Target Validation Information
Target ID T58992
Target Name Delta-type opioid receptor
Target Type
Successful
Drug Potency against Target DPDPE Drug Info Ki = 2.72 nM
3,6-bis(Dmt-Tic-NH-methyl)-2(1H)-pyrazinone Drug Info Ki = 0.163 nM [527916]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo Drug Info IC50 = 16 nM [528606]
6-(4-((phenethylamino)methyl)phenoxy)nicotinamide Drug Info Ki = 1.16 nM [529132]
D-Phe-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2(CTP) Drug Info IC50 = 8400 nM [533376]
4-(p-Tolyl)spiro[chromene-2,4'-piperidine] Drug Info Ki = 72 nM [529689]
H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]-OH Drug Info IC50 = 3.4 nM [528875]
H-Tyr-Pro-Dap(6DMN)-Phe-NH2 Drug Info IC50 = 500 nM [528238]
17-(Cyclopropylmethyl)-N-phenylmorphinan-3-amine Drug Info Ki = 5.4 nM [530529]
N-(4-Iodophenyl)-N'-(17-methylmorphinan-3-yl)urea Drug Info Ki = 300 nM [530529]
1-benzhydryl-4-o-tolylpiperidin-4-ol Drug Info Ki = 1668 nM [528781]
1-benzhydryl-4-(3-phenylpropyl)piperidin-4-ol Drug Info Ki = 13750 nM [528781]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-Bzl Drug Info IC50 = 41 nM [529306]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Trp-D-Nle-D-Asp-D-Phe-H Drug Info IC50 = 25 nM [528606]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-Boc Drug Info IC50 = 24 nM [528058]
Trans-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH Drug Info IC50 = 0.76 nM [528875]
Cis-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH Drug Info IC50 = 0.59 nM [528875]
1-benzhydryl-4-cyclohexylpiperidin-4-ol Drug Info Ki = 8105 nM [528781]
1-benzhydryl-4-(furan-2-yl)piperidin-4-ol Drug Info Ki = 14455 nM [528781]
4-phenyl-1-(1-phenylheptyl)piperidin-4-ol Drug Info Ki = 550 nM [528785]
1-benzhydryl-4-benzylpiperidin-4-ol Drug Info Ki = 15010 nM [528781]
1-benzhydryl-4-phenyl-4-propoxypiperidine Drug Info Ki = 2767 nM [528785]
1-benzhydryl-4-p-tolylpiperidin-4-ol Drug Info Ki = 12115 nM [528781]
1-benzhydryl-4-(thiophen-2-yl)piperidin-4-ol Drug Info Ki = 8446 nM [528781]
1-benzhydryl-4-(2-methoxyphenyl)piperidin-4-ol Drug Info Ki = 4392 nM [528781]
1-benzhydryl-4-butylpiperidin-4-ol Drug Info Ki = 18800 nM [528781]
1-benzhydryl-4-ethoxy-4-phenylpiperidine Drug Info Ki = 898 nM [528785]
Deprotected cogener of M6G Drug Info Ki = 266.3 nM [527461]
SN-23 Drug Info Ki = 0.19 nM [530073]
H-Tyr-c[D-Orn-Aic-Glu]-NH2 Drug Info Ki = 209 nM [528093]
Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info IC50 = 310 nM [528193]
Tyr-(R)-Aba-Gly-Phe-NH2 Drug Info Ki = 2.965 nM [529202]
LOFENTANIL Drug Info IC50 = 0.25 nM [533543]
Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info IC50 = 1300 nM [528193]
Tyr-(S)-spiro-Aba-Gly-Phe-NH2 Drug Info Ki = 2.312 nM [529202]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-3,5-Bzl(CF3)2 Drug Info IC50 = 150 nM [529306]
Nalbuphine Drug Info Ki = 1.4 nM [552189]
Tyr-Pro-Tmp-Phe-NH Drug Info Ki = 1358 nM [528832]
H-Tyr-NMe-D-Ala-Phe-Sar-NH2 Drug Info IC50 = 7100 nM [529395]
H-Dmt-Tic-NH-CH2-ImidPh Drug Info Ki = 0.443 nM [529246]
CARBOXYFENTANYL Drug Info Ki = 9400 nM [529088]
H-D-Tic-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 Drug Info IC50 = 1270 nM [525699]
N-methylstephisoferulin Drug Info IC50 = 2500 nM [530876]
SB-213698 Drug Info Ki = 1.44 nM [530073]
MCL-447 Drug Info Ki = 160 nM [528787]
MCL-117 Drug Info Ki = 0.62 nM [527951]
MCL-458 Drug Info Ki = 360 nM [528787]
(-)-isoelaeocarpiline Drug Info IC50 = 9900 nM [528442]
PERIPENTADENINE Drug Info IC50 = 11400 nM [529173]
MCL-428 Drug Info Ki = 3.9 nM [528655]
DELTORPHIN-II Drug Info IC50 = 0.53 nM [531038]
MCL-443 Drug Info Ki = 15 nM [528655]
MCL-450 Drug Info IC50 = 3.9 nM [528412]
MCL-429 Drug Info Ki = 1.6 nM [528655]
Tyr-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 1500 nM [528193]
PROSTEPHABYSSINE Drug Info IC50 = 5500 nM [530876]
RTI-5989-25 Drug Info Ki = 142 nM [534631]
MCL-153 Drug Info Ki = 730 nM [530707]
Grandisine C Drug Info IC50 = 14600 nM [528442]
8-azabicyclo[3.2.1]octan-3-yloxy-benzamide Drug Info IC50 = 8306 nM [531109]
Dmt-Pro-Tmp-Phe-NH2 Drug Info Ki = 1.83 nM [528832]
Tyr-Pro-Imp-Phe-NH2 Drug Info Ki = 543 nM [528832]
H-Dmt-Aba-Gly-NH-CH2-Bid Drug Info IC50 = 2700 nM [528269]
Dmt-Pro-Emp-Phe-NH2 Drug Info IC50 = 0.51 nM [528832]
MCL-451 Drug Info IC50 = 10 nM [528412]
Dmt-Pro-Phe-Phe-NH2 Drug Info IC50 = 0.59 nM [528832]
Dmt-Pro-Dmp-Phe-NH2 Drug Info Ki = 2.27 nM [528832]
Tyr-Pro-Emp-Phe-NH2 Drug Info IC50 = 277 nM [528832]
Tyr-Pro-Mmp-Phe-NH Drug Info IC50 = 15.7 nM [528832]
H-Tyr-Tic-OH Drug Info Ki = 242 nM [530447]
Tyr-Pro-Phe-Phe-OCH2CH3 Drug Info Ki = 2940 nM [529480]
Tyr-Pro-Phe-Phe-N(CH3)2 Drug Info IC50 = 2723 nM [529480]
H-Dmt-Tic-NH-CH2-Indn Drug Info IC50 = 129 nM [529246]
N-methylstephuline Drug Info IC50 = 2100 nM [530876]
H-Dmt-Tic-NH-CH2-Boa Drug Info Ki = 0.283 nM [529246]
3-desoxy-3-carboxamidonaltrexone Drug Info Ki = 550 nM [530013]
H-Dmt-Tic-NH-(S)CH(CH2-COOH)-Bid(N1-Me) Drug Info IC50 = 2886 nM [529630]
H-Dmt-Tic-NH-CH[(CH2)4-NH2]-Bid Drug Info Ki = 0.49 nM [528411]
H-Dmt-Tic-Gly-NH-Bzl Drug Info IC50 = 2.69 nM [529630]
H-Dmt-Aba-Gly-NH-Ph Drug Info IC50 = 650 nM [528269]
Tyr-Pro-Phe-Phe-OCH2OH Drug Info IC50 = 29.17 nM [529480]
H-Dmt-Tic-NH-CH2-Imid Drug Info IC50 = 3.63 nM [529246]
Tyr-Pro-Phe-Phe-NHCH3 Drug Info Ki = 8474 nM [529480]
Tyr-Pro-L-(NMe)Phe-D-Pro-NH2 Drug Info IC50 = 1250 nM [534004]
LONGANINE Drug Info IC50 = 700 nM [530876]
H-Cpa-Gly-Gly-Phe-Met-NH2 Drug Info Ki = 1.3 nM [528724]
H-Poa-ser-Gly-Phe-Leu-Thr-OH Drug Info Ki = 360 nM [528724]
H-mCpa-ala-Gly-Phe-leu-OH Drug Info Ki = 170 nM [528724]
H-Cpa-c[pen-Gly-Phe-pen]OH Drug Info Ki = 19 nM [528724]
H-Tyr-Gly-Gly-Phe-Met-OH Drug Info Ki = 2 nM [528724]
H-Cdp-Gly-Gly-Phe-Leu-OH Drug Info Ki = 1 nM [528724]
H-mCpa-Gly-Gly-Phe-Leu-OH Drug Info Ki = 475 nM [528724]
H-Cxp-ala-Gly-Phe-leu-OH Drug Info Ki = 1100 nM [528724]
H-Tyr-c[D-Orn-(D or L)Atc-Glu]-NH2 Drug Info Ki = 3510 nM [528093]
Tyr-Pro-D-Phe-D-Pro-NH2 Drug Info IC50 = 4810 nM [534004]
H-Cdp-ser-Gly-Phe-Leu-Thr-OH Drug Info Ki = 1.2 nM [528724]
H-Dmt-Tic-NH-(CH2)6-NH-Dmt-H Drug Info Ki = 0.23 nM [527758]
H-Cdp-ala-Gly-Phe-leu-OH Drug Info Ki = 0.78 nM [528724]
1,10-bis-(Dmt-Tic-amino)decane Drug Info Ki = 1.53 nM [527916]
H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-OH Drug Info IC50 = 682 nM [527693]
H-Dmt-Tic-Gly-NH-Ph Drug Info IC50 = 2.57 nM [529630]
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info IC50 = 63 nM [528193]
H-Apa-ala-Gly-Phe-leu-OH Drug Info Ki = 19 nM [528724]
BIO-306 Drug Info IC50 = 130 nM [552753]
N-Benzyl-17-(cyclobutylmethyl)morphinan-3-amine Drug Info Ki = 130 nM [530529]
AKNADILACTAM Drug Info IC50 = 17000 nM [530876]
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info IC50 = 24 nM [528193]
H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-NH2 Drug Info Ki = 4 nM [528621]
[Dcp1]Dyn A(1-11)-NH2 Drug Info Ki = 129 nM [528376]
Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info IC50 = 220 nM [528193]
H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-NH2 Drug Info Ki = 13 nM [528621]
H-Dmt-Tic-NH-CH[(CH2)4-NH-Z]-Bid Drug Info IC50 = 9049 nM [528411]
Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info IC50 = 890 nM [528193]
4-phenyl-1-(1-phenylhexyl)piperidin-4-ol Drug Info Ki = 184 nM [528785]
1-benzhydryl-4-(benzyloxy)-4-phenylpiperidine Drug Info Ki = 3741 nM [528785]
SOMATOSTATIN Drug Info IC50 = 2000 nM [533376]
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info IC50 = 700 nM [528193]
Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info IC50 = 66 nM [528193]
Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info IC50 = 9 nM [528193]
SNF-9007 Drug Info IC50 = 29 nM [528193]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc Drug Info IC50 = 230 nM [528058]
N-(17-Methylmorphinan-3-yl)-N'-phenylurea Drug Info Ki = 320 nM [530529]
Dhp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 Drug Info Ki = 11.6 nM [528376]
1-benzhydryl-4-(2-fluorophenyl)piperidin-4-ol Drug Info Ki = 5610 nM [528781]
1-(2-ethoxy-1-phenylethyl)-4-phenylpiperidin-4-ol Drug Info Ki = 15250 nM [528785]
1-benzhydryl-4-methoxy-4-phenylpiperidine Drug Info Ki = 2651 nM [528785]
1-benzhydryl-4-(4-fluorophenyl)piperidin-4-ol Drug Info Ki = 3325 nM [528781]
Loperamide Drug Info IC50 = 6.9 nM [552192]
1-benzhydryl-4-(3-methoxyphenyl)piperidin-4-ol Drug Info Ki = 9585 nM [528781]
1-benzhydryl-4-hexylpiperidin-4-ol Drug Info Ki = 17865 nM [528781]
1-benzhydryl-4-(3-fluorophenyl)piperidin-4-ol Drug Info Ki = 5610 nM [528781]
6-(4-(3-(benzylamino)propyl)phenoxy)nicotinamide Drug Info Ki = 495.99 nM [528996]
N-Benzyl-17-(cyclopropylmethyl)morphinan-3-amine Drug Info Ki = 29 nM [530529]
4-(4-((phenethylamino)methyl)phenoxy)benzamide Drug Info Ki = 1.88 nM [528996]
CYCLORPHAN Drug Info Ki = 1.9 nM [530529]
Codeine Drug Info Ki > 1000 nM
H-Dmt-Tic-Glu-NH2 Drug Info IC50 = 2.58 nM [527332]
Tyr-D-Ala-Gly-Phe-Met-Pro-Leu-Trp-NH-Bzl Drug Info IC50 = 4.8 nM [529724]
MC-CAM Drug Info Ki = 4.79 nM [530461]
MCL-144 Drug Info Ki = 4.2 nM [530279]
1-benzhydryl-4-phenylpiperidin-4-ol Drug Info Ki = 1666 nM [530052]
6-(4-(2-(benzylamino)ethyl)phenoxy)nicotinamide Drug Info Ki = 70.21 nM [529132]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)phenol Drug Info Ki = 59 nM [529689]
BIPHALIN Drug Info IC50 = 2.7 nM [530392]
4-phenyl-4-[1H-imidazol-2-yl]-piperidine Drug Info Ki = 81 nM [527810]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H Drug Info IC50 = 12 nM [528606]
Tyr-D-Ala-Gly-Phe-Met-NH2 Drug Info IC50 = 36 nM [530392]
ISOELAEOCARPINE Drug Info IC50 = 13600 nM [528801]
Tyr-(NMe)Ala-L-Phe-D-Pro-NH2 Drug Info IC50 = 202 nM [534004]
AMINOFENTANYL Drug Info IC50 = 13000 nM [528300]
H-D-Tca-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 Drug Info IC50 = 211 nM [525699]
H-Dmt-Tic-Glu-Dap(6DMN)-NH(2) Drug Info Ki = 7.8 nM [528238]
H-Dmt-Tic-NH-(D)-CH[(CH2)4-NH-Z]-Bid Drug Info Ki = 0.4 nM [528411]
8-carboxamidocyclazocine Drug Info Ki = 5.2 nM [529429]
H-Tyr-Pro-Phe-Phe-NH-CH2-CH2-NH Tic Dmt-H Drug Info Ki = 1.45 nM [529041]
6-cinnamoylhernandine Drug Info IC50 = 5100 nM [530876]
MCL-448 Drug Info Ki = 23 nM [528787]
MCL-182 Drug Info Ki = 180 nM [528787]
BUTORPHAN Drug Info Ki = 5.9 nM [530707]
MCL-147 Drug Info Ki = 29 nM [528787]
MCL-445 Drug Info Ki = 270 nM [528787]
MCL-446 Drug Info Ki = 50 nM [528787]
MCL-434 Drug Info Ki = 42 nM [528655]
MCL-432 Drug Info Ki = 27 nM [528655]
RTI-5989-23 Drug Info Ki = 168 nM [534631]
SALVINORIN A Drug Info Ki = 3990 nM [529401]
14-O-phenylpropylnaltrexone Drug Info Ki = 0.48 nM [529991]
Naltrexone-6-alpha-ol Drug Info Ki = 56 nM [529816]
Naltrexone-6-beta-ol Drug Info Ki = 53 nM [529816]
6-(Allyl-methyl-amino)-4,4-diphenyl-heptan-3-ol Drug Info Ki = 150 nM [533539]
Tyr-Pro-Dmp-Phe-NH2 Drug Info IC50 = 1.39 nM [528832]
Dmt-Pro-3,5Dmp-Phe-NH2 Drug Info Ki = 11.6 nM [528832]
Tyr-Pro-Dmt-Phe-NH2 Drug Info IC50 = 978 nM [528832]
METAZOCINE Drug Info Ki = 140 nM [529816]
PHENAZOCINE Drug Info Ki = 5 nM [529816]
H-Tyr-c[pen-Gly-Phe-pen]OH Drug Info Ki = 3.2 nM [528724]
Benzyl derivative of M6G Drug Info Ki = 7.2 nM [527461]
C[L-mTyr-D-pro-L-Phe-D-trp] Drug Info Ki = 670 nM [530160]
C[L-Phe-D-pro-L-mTyr-D-trp] Drug Info Ki = 3400 nM [530160]
MCL-149 Drug Info Ki = 150 nM [528787]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Phe-D-Asp-D-Nle-Trp-H Drug Info IC50 = 15 nM [528606]
Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc Drug Info IC50 = 42 nM [528058]
D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2(CTAP) Drug Info IC50 = 4500 nM [533376]
1-benzhydryl-4-(4-chlorophenyl)piperidin-4-ol Drug Info Ki = 6364 nM [528781]
(-)-cyclorphan Drug Info Ki = 1.9 nM [527951]
H-Tyr-Pro-Phe-Phe-NH-(CH2)5-(C=O)-Dap(6DMN)-NH2 Drug Info IC50 = 300 nM [528238]
17-Methylmorphinan-3-yl 4-Iodophenyl Carbamate Drug Info Ki = 160 nM [530529]
6-(2-phenethylisoindolin-5-yloxy)nicotinamide Drug Info Ki = 2274 nM [529132]
Tyr-D-Ala-Phe-Gly-Tyr-Pro-Thr(Beta-D-Glc)-Gly-NH2 Drug Info Ki = 67 nM [534460]
4-phenyl-1-(1-phenylbutyl)piperidin-4-ol Drug Info Ki = 4126 nM [528785]
4-phenyl-1-(phenyl(p-tolyl)methyl)piperidin-4-ol Drug Info Ki = 9365 nM [528785]
Tyr-D-Ala-Phe-Asp-Val-Val-Thr[Beta-D-Glc]-Gly-NH2 Drug Info Ki = 1.55 nM [534460]
Tyr-D-Ala-Phe-Thr(-D-Glc)-Tyr-Pro-Ser-NH2 Drug Info Ki = 1760 nM [534460]
5-(4-((phenethylamino)methyl)phenoxy)picolinamide Drug Info Ki = 8.54 nM [528996]
1-(dio-tolylmethyl)-4-phenylpiperidin-4-ol Drug Info Ki = 5791 nM [528785]
DAMGO Drug Info Ki = 2670 nM
LY-255582 Drug Info Ki = 198 nM [534631]
Dmt-Pro-Mmp-Phe-NH2 Drug Info Ki = 4.61 nM [528832]
Grandisine F Drug Info IC50 = 1550 nM [528442]
GUANIDINONALTRINDOLE Drug Info Ki = 70 nM [526656]
17-methyl-4'-methyldihydromorphinone Drug Info Ki = 4 nM [528375]
H-Tyr-D-Ala-Gly-Phe-D-Leu Drug Info IC50 = 0.27 nM [528853]
H-Dmt-Aba-Gly-NH-CH2-Ph Drug Info IC50 = 830 nM [528269]
UFP-512 Drug Info IC50 = 0.12 nM [531038]
HTyr-Gly-Gly-Phe-Leu-Arg-Arg-lle-Arg-Pro-LysNH2 Drug Info Ki = 6.18 nM [530428]
N-alpha-amidino-Tyr(Me)-Pro-Trp-Phe-NH2 Drug Info IC50 = 1343 nM [528594]
MCL-435 Drug Info Ki = 30 nM [528655]
MCL-183 Drug Info Ki = 230 nM [528787]
MCL-145 Drug Info Ki = 9.4 nM [527951]
MCL-431 Drug Info Ki = 78 nM [528655]
MCL-139 Drug Info Ki = 9.4 nM [527951]
MCL-433 Drug Info Ki = 53 nM [528655]
MCL-154 Drug Info Ki = 2500 nM [530707]
MCL-449 Drug Info Ki = 2.8 nM [528655]
H-D-Phe-c[Cys-Tyr-DTrp-Orn-Thr-Pen]-Thr-NH2 Drug Info IC50 = 13500 nM [529704]
Antanal 2 Drug Info Ki = 7.74 nM [529704]
1-[3-(4-biphenyl)-(1,2,4-triazol-4-yl) ]-3-phenol Drug Info Ki = 1500 nM [528288]
RTI-5989-31 Drug Info Ki = 270 nM [528947]
3,6-bis(Dmt-Tic-NH-propyl)-2(1H)-pyrazinone Drug Info Ki = 0.155 nM [527916]
O-DESMETHYL TRAMADOL Drug Info Ki = 2900 nM [529816]
Dimepheptanol Drug Info Ki = 230 nM [533539]
Hydrocodone Drug Info Ki = 1021 nM
SN-11 Drug Info Ki = 0.19 nM [530073]
Dmt-Pro-Dmt-Phe-NH2 Drug Info Ki = 80.8 nM [528832]
Dmt-Pro-Imp-Phe-NH2 Drug Info IC50 = 5.56 nM [528832]
H-Dmt-Tic-Lys-NH-Ph Drug Info Ki = 0.42 nM [528411]
H-Dmt-Tic-Asp-NH-Ph Drug Info IC50 = 265 nM [529630]
H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-OH Drug Info Ki = 0.48 nM [528621]
H-2',6'-dimethyltyrosine-Tic-Phe-Phe-OH Drug Info Ki = 0.248 nM [530447]
Tyr-Pro-D-Phg-Phe-NH2 Drug Info Ki = 2100 nM [528190]
Dcp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 Drug Info Ki = 25.8 nM [528376]
6-desoxonaltrexone Drug Info Ki = 79 nM [530013]
H-Dmt-Tic-NH-CH2-Bta Drug Info Ki = 0.145 nM [529246]
Tyr-Pro-3,5Dmp-Phe-NH2 Drug Info Ki = 3451 nM [528832]
H-Dmt-Tic-Asp-N(Me)-Ph Drug Info Ki = 0.186 nM [529630]
H-Dmt-Tic-D-Asp-NH-Ph Drug Info IC50 = 2655 nM [529630]
Dmt-Pro-Phe-D-1-Nal-NH2 Drug Info Ki = 27.1 nM [528646]
Tyr-Pro-L-Phe-D-Pro-NH2 Drug Info IC50 = 1508 nM [534004]
Tyr-(S)-Aba-Gly-Phe-NH2 Drug Info Ki = 0.778 nM [529202]
Dmt-Pro-Phe-D-2-Nal-NH2 Drug Info Ki = 7.74 nM [528646]
M6G thiosaccharide analogue Drug Info Ki = 31.4 nM [527461]
H-mCpa-ser-Gly-Phe-Leu-Thr-OH Drug Info Ki = 42 nM [528724]
H-Aba-ala-Gly-Phe-Met-OH Drug Info Ki = 1 nM [528724]
H-Dmt-Tic-Gly-NH-CH2-Bid Drug Info IC50 = 0.13 nM [528269]
H-Cpa-Gly-Gly-Phe-Met-OH Drug Info Ki = 1.8 nM [528724]
H-Tyr-Gly-Gly-Phe-Met-NH2 Drug Info Ki = 10 nM [528724]
H-Aba-ala-Gly-Phe-leu-OH Drug Info Ki = 10 nM [528724]
H-Aba-Gly-Gly-Phe-Leu-OH Drug Info Ki = 19 nM [528724]
H-Dmt-Tic-Lys-NH-CH2-Ph Drug Info Ki = 0.5 nM [528411]
Tyr-Pro-D-Phe-Pro-NH2 Drug Info IC50 = 594 nM [534004]
C[L-Phe-D-pro-L-Phe-L-trp] Drug Info Ki = 2000 nM [530160]
H-Dmt-Tic-Lys(Z)-NH-Ph Drug Info Ki = 0.57 nM [528411]
Clocinnamox Drug Info Ki = 2.7 nM [529991]
Tyr-Pro-L-Phe-Pro-NH2 Drug Info IC50 = 3690 nM [534004]
Tyr-Pro-L-(NMe)Phe-Pro-NH2 Drug Info IC50 = 1790 nM [534004]
1,6-bis-(Dmt-Tic-amino)hexane Drug Info Ki = 0.129 nM [527916]
(H-Dmt-Tic-Glu-NH-(CH(2))(5)-CO-Dap(6DMN)-NH(2) Drug Info Ki = 0.158 nM [528238]
3,6-bis(Dmt-Tic-NH-butyl)-2(1H)-pyrazinone Drug Info Ki = 0.323 nM [527916]
H-Tyr-c[D-Cys-Gly-Phe-L-Cys]NH2 Drug Info Ki = 1.61 nM [528692]
H-Dmt-Tic-Gly-N(Me)-Ph Drug Info IC50 = 1466 nM [529630]
H-Dmt-Tic-NH-CH[(CH2)4-NH-Ac]-Bid Drug Info Ki = 0.18 nM [528411]
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info IC50 = 170 nM [528193]
Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2 Drug Info IC50 = 0.28 nM [533971]
H-Dmt-Tic-Lys(Z)-NH-CH2-Ph Drug Info Ki = 0.31 nM [528411]
17-(Cyclobutylmethyl)-N-phenylmorphinan-3-amine Drug Info Ki = 39 nM [530529]
H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-NH2 Drug Info Ki = 7 nM [528621]
H-Tyr-Tic-Cha-Phe-OH Drug Info Ki = 0.61 nM [528621]
H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-NH2 Drug Info Ki = 4.1 nM [528621]
H-Dmt-Tic-Lys(Ac)-NH-Ph Drug Info Ki = 0.13 nM [528411]
H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-OH Drug Info Ki = 2 nM [528621]
H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-OH Drug Info Ki = 2 nM [528621]
Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info IC50 = 23 nM [528193]
H-Dmt-Tic-Glu-NH-(CH2)5-NH2 Drug Info Ki = 0.22 nM [527332]
1-benzhydryl-4-(4-methoxyphenyl)piperidin-4-ol Drug Info Ki = 19220 nM [528781]
H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid Drug Info IC50 = 179 nM [529630]
H-Tyr-D-Ala-Gly Phe-Pro-Leu-Trp-O-3,5-Bzl(CF3)2 Drug Info IC50 = 400 nM [529306]
1-benzhydryl-4-(4-bromophenyl)piperidin-4-ol Drug Info Ki = 15240 nM [528781]
2-Hydroxymethyl-3-hydroxymorphinan Drug Info Ki = 1400 nM [530529]
1-(1,2-diphenylethyl)-4-phenylpiperidin-4-ol Drug Info Ki = 187 nM [528785]
H-Tyr-c[D-Cys-Gly-Phe-D-Cys]NH2 Drug Info Ki = 0.822 nM [528692]
4-phenyl-1-(1-phenylpentyl)piperidin-4-ol Drug Info Ki = 441 nM [528785]
Antanal 1 Drug Info Ki = 17.4 nM [529704]
N-alpha-amidino-Tyr(Me)-Pro-Trp-p-Cl-Phe-NH2 Drug Info IC50 = 1288 nM [528594]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac Drug Info IC50 = 36 nM [528058]
H-D-Trp-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 Drug Info IC50 = 3530 nM [525699]
4-phenyl-1-(phenyl(m-tolyl)methyl)piperidin-4-ol Drug Info Ki = 2437 nM [528785]
1-benzhydryl-4-m-tolylpiperidin-4-ol Drug Info Ki = 7796 nM [528781]
H-Dmt-Tic-NH-(CH2)6-NH-Tic-H Drug Info Ki = 0.13 nM [527758]
Tyr-Pro-Phe-Phe-OCH3 Drug Info IC50 = 37.2 nM [529480]
Tyr-Pro-Phe-Phe-OC(CH3)3 Drug Info Ki = 247 nM [529480]
H-2',6'-dimethyltyrosine-Tic-OH Drug Info Ki = 1.84 nM [530447]
ENDOMORPHIN-1 Drug Info Ki = 1909 nM [529556]
H-Dmt-Tic-NH-(CH2)6-NH-Phe-H Drug Info Ki = 0.89 nM [527758]
Tyr-Pro-Phe-Phe-NHNH2 Drug Info IC50 = 185 nM [529480]
CCDC 710249, HCl salt Drug Info IC50 = 6.9 nM [530013]
H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-OH Drug Info Ki = 1.5 nM [528621]
D-PhGly-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2 Drug Info IC50 = 2800 nM [533376]
DERMORPHIN Drug Info IC50 = 15.2 nM [527931]
UFP-502 Drug Info IC50 = 0.13 nM [531038]
H-Dmt-Tic-NH-CH2-CH2-NH2 Drug Info Ki = 1.81 nM [529041]
H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-NH2 Drug Info IC50 = 1.69 nM [527693]
H-Tyr-D-Ala-Gly-Phe-NH-NH-(NMe)Phe-Asp-Nle-Trp-Ac Drug Info IC50 = 5.1 nM [528058]
H-Aba-ser-Gly-Phe-Leu-Thr-OH Drug Info Ki = 3.8 nM [528724]
H-Tyr-c[cys-Gly-Phe(p-NO2)-cys]NH2 Drug Info IC50 = 0.232 nM [528724]
SN-28 Drug Info Ki = 0.14 nM [531165]
4-Phenylspiro[chromene-2,4'-piperidine] Drug Info Ki = 71 nM [529689]
6-cinnamoyl-N-methylstephasunoline Drug Info IC50 = 11300 nM [530876]
D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2(CTOP) Drug Info IC50 = 13500 nM [533376]
(-)-eseroline Drug Info IC50 = 10000 nM
Grandisine D Drug Info IC50 = 1650 nM [528442]
[Leu5]enkephalin Drug Info Ki = 2.53 nM [530780]
SB-0304 Drug Info IC50 = 17800 nM [529395]
Tyr-Gly-Gly-Phe-leu-c(Cys-Arg-Ile-Arg-Cys)-lys Drug Info IC50 = 92.6 nM [533889]
OXYMORPHINDOLE Drug Info Ki = 0.8 nM [529414]
Tyr-Gly-Gly-Phe-c(Cys-Arg-Arg-Ile-Cys)-Arg-lys Drug Info IC50 = 6262 nM [533889]
ANALOG OF DYNORPHIN A Drug Info IC50 = 9.1 nM [533889]
ELAEOCARPENINE Drug Info Ki = 14000 nM [530705]
Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2 Drug Info IC50 = 0.67 nM [533971]
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info IC50 = 45 nM [528193]
Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info IC50 = 65 nM [528193]
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info IC50 = 12 nM [528193]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H Drug Info IC50 = 26 nM [528058]
CYCLAZOCINE Drug Info Ki = 2 nM [529871]
ETONITAZENE Drug Info Ki = 0.6 nM [531519]
ICI-174864 Drug Info IC50 = 83 nM [528410]
Dmt-Pro-Trp-D-2-Nal-NH2 Drug Info Ki = 17.4 nM [528646]
6-(4-((benzylamino)methyl)phenoxy)nicotinamide Drug Info Ki = 54.15 nM [528996]
1,4-bis-(Dmt-Tic-amino)butane Drug Info Ki = 0.124 nM [527916]
MCL-444 Drug Info Ki = 2.7 nM [528655]
6beta-naltrexol HCl Drug Info Ki = 213 nM [530077]
Butorphanol Drug Info Ki = 0.5 nM [552189]
NORBINALTORPHIMINE Drug Info Ki = 86 nM [526656]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide Drug Info Ki = 17 nM [530324]
HERKINORIN Drug Info Ki = 1170 nM [529401]
Bis-((-)-N-propargylmorphinan-3-yl) sebacoylate Drug Info Ki = 190 nM [527951]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-O-Bzl Drug Info IC50 = 40 nM [529306]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-3,5-Bzl(CF3)2 Drug Info IC50 = 45 nM [529306]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-Bzl Drug Info IC50 = 50 nM [529306]
FALCARINDIOL Drug Info Ki = 1096 nM [529238]
ENDOMORPHIN 2 Drug Info IC50 = 510 nM [531092]
Action against Disease Model Hydromorphone HEK-deltaCells IC50: 54 nM Drug Info
Butorphanol HEK-delta Cells IC50: 61 nM Drug Info
Nalbuphine HEK-delta Cells IC50: 545 nM Drug Info
References
Ref 527916J Med Chem. 2005 Dec 15;48(25):8035-44.Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists.
Ref 528606J Med Chem. 2007 Jan 11;50(1):165-8.Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
Ref 529132Bioorg Med Chem Lett. 2007 Dec 15;17(24):6841-6. Epub 2007 Oct 17.Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
Ref 533376J Med Chem. 1986 Nov;29(11):2370-5.Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for mu opioid receptors.
Ref 529689J Med Chem. 2008 Oct 9;51(19):5893-6. Epub 2008 Sep 13.Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
Ref 528875J Med Chem. 2007 Jun 28;50(13):3138-42. Epub 2007 Jun 1.Synthesis of stable and potent delta/mu opioid peptides: analogues of H-Tyr-c[D-Cys-Gly-Phe-D-Cys]-OH by ring-closing metathesis.
Ref 528238J Med Chem. 2006 Jun 15;49(12):3653-8.6-N,N-dimethylamino-2,3-naphthalimide: a new environment-sensitive fluorescent probe in delta- and mu-selective opioid peptides.
Ref 530529J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Ref 530529J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 529306J Med Chem. 2008 Mar 13;51(5):1369-76. Epub 2008 Feb 12.A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
Ref 528606J Med Chem. 2007 Jan 11;50(1):165-8.Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
Ref 528058J Med Chem. 2006 Mar 9;49(5):1773-80.Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
Ref 528875J Med Chem. 2007 Jun 28;50(13):3138-42. Epub 2007 Jun 1.Synthesis of stable and potent delta/mu opioid peptides: analogues of H-Tyr-c[D-Cys-Gly-Phe-D-Cys]-OH by ring-closing metathesis.
Ref 528875J Med Chem. 2007 Jun 28;50(13):3138-42. Epub 2007 Jun 1.Synthesis of stable and potent delta/mu opioid peptides: analogues of H-Tyr-c[D-Cys-Gly-Phe-D-Cys]-OH by ring-closing metathesis.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 527461Bioorg Med Chem Lett. 2005 Mar 15;15(6):1583-6.Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide.
Ref 530073Bioorg Med Chem Lett. 2009 May 15;19(10):2792-5. Epub 2009 Mar 26.Design and synthesis of novel delta opioid receptor agonists and their pharmacologies.
Ref 528093J Med Chem. 1991 Oct;34(10):3125-32.Conformational restriction of the phenylalanine residue in a cyclic opioid peptide analogue: effects on receptor selectivity and stereospecificity.
Ref 528193J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Ref 529202J Med Chem. 2008 Jan 10;51(1):173-7. Epub 2007 Dec 7.Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties.
Ref 533543J Med Chem. 1982 Aug;25(8):913-9.Potential affinity labels for the opiate receptor based on fentanyl and related compounds.
Ref 528193J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Ref 529202J Med Chem. 2008 Jan 10;51(1):173-7. Epub 2007 Dec 7.Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties.
Ref 529306J Med Chem. 2008 Mar 13;51(5):1369-76. Epub 2008 Feb 12.A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
Ref 552189kappa-Opioid receptor effects of butorphanol in rhesus monkeys. J Pharmacol Exp Ther. 1999 Jul;290(1):259-65.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 529395J Med Chem. 2008 Apr 24;51(8):2571-4. Epub 2008 Mar 28.Blood-brain barrier penetration by two dermorphin tetrapeptide analogues: role of lipophilicity vs structural flexibility.
Ref 529246Bioorg Med Chem. 2008 Mar 15;16(6):3032-8. Epub 2007 Dec 23.Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).
Ref 529088J Med Chem. 2007 Nov 1;50(22):5528-32. Epub 2007 Oct 10.Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.
Ref 525699J Med Chem. 2000 Feb 24;43(4):569-80.Opiate aromatic pharmacophore structure-activity relationships in CTAP analogues determined by topographical bias, two-dimensional NMR, and biological activity assays.
Ref 530876J Nat Prod. 2010 May 28;73(5):988-91.Hasubanan alkaloids with delta-opioid binding affinity from the aerial parts of Stephania japonica.
Ref 530073Bioorg Med Chem Lett. 2009 May 15;19(10):2792-5. Epub 2009 Mar 26.Design and synthesis of novel delta opioid receptor agonists and their pharmacologies.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 527951J Med Chem. 2006 Jan 12;49(1):256-62.Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 528442J Nat Prod. 2006 Sep;69(9):1295-9.Grandisines C-G, indolizidine alkaloids from the Australian rainforest tree Elaeocarpus grandis.
Ref 529173J Nat Prod. 2007 Dec;70(12):1946-50. Epub 2007 Nov 27.Alkaloids with human delta-opioid receptor binding affinity from the Australian rainforest tree Peripentadenia mearsii.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 531038Bioorg Med Chem. 2010 Aug 15;18(16):6024-30. Epub 2010 Jun 25.Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 528412J Med Chem. 2006 Sep 7;49(18):5640-3.New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 528193J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Ref 530876J Nat Prod. 2010 May 28;73(5):988-91.Hasubanan alkaloids with delta-opioid binding affinity from the aerial parts of Stephania japonica.
Ref 534631J Med Chem. 1998 May 21;41(11):1980-90.Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
Ref 530707Bioorg Med Chem Lett. 2010 Mar 1;20(5):1507-9. Epub 2010 Jan 25.Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.
Ref 528442J Nat Prod. 2006 Sep;69(9):1295-9.Grandisines C-G, indolizidine alkaloids from the Australian rainforest tree Elaeocarpus grandis.
Ref 531109Bioorg Med Chem Lett. 2010 Sep 15;20(18):5405-10. Epub 2010 Aug 3.SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 528269J Med Chem. 2006 Jun 29;49(13):3990-3.New 2',6'-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 528412J Med Chem. 2006 Sep 7;49(18):5640-3.New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 530447J Med Chem. 2009 Nov 12;52(21):6941-5.Agonist vs antagonist behavior of delta opioid peptides containing novel phenylalanine analogues in place of Tyr(1).
Ref 529480Bioorg Med Chem. 2008 Jun 15;16(12):6415-22. Epub 2008 May 3.Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling.
Ref 529480Bioorg Med Chem. 2008 Jun 15;16(12):6415-22. Epub 2008 May 3.Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling.
Ref 529246Bioorg Med Chem. 2008 Mar 15;16(6):3032-8. Epub 2007 Dec 23.Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).
Ref 530876J Nat Prod. 2010 May 28;73(5):988-91.Hasubanan alkaloids with delta-opioid binding affinity from the aerial parts of Stephania japonica.
Ref 529246Bioorg Med Chem. 2008 Mar 15;16(6):3032-8. Epub 2007 Dec 23.Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).
Ref 530013Bioorg Med Chem Lett. 2009 Apr 15;19(8):2289-94. Epub 2009 Feb 25.Syntheses of novel high affinity ligands for opioid receptors.
Ref 529630J Med Chem. 2008 Aug 28;51(16):5109-17. Epub 2008 Aug 5.Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
Ref 528411J Med Chem. 2006 Sep 7;49(18):5610-7.Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
Ref 529630J Med Chem. 2008 Aug 28;51(16):5109-17. Epub 2008 Aug 5.Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
Ref 528269J Med Chem. 2006 Jun 29;49(13):3990-3.New 2',6'-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands.
Ref 529480Bioorg Med Chem. 2008 Jun 15;16(12):6415-22. Epub 2008 May 3.Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling.
Ref 529246Bioorg Med Chem. 2008 Mar 15;16(6):3032-8. Epub 2007 Dec 23.Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).
Ref 529480Bioorg Med Chem. 2008 Jun 15;16(12):6415-22. Epub 2008 May 3.Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling.
Ref 534004J Med Chem. 1993 Mar 19;36(6):708-19.A topochemical approach to explain morphiceptin bioactivity.
Ref 530876J Nat Prod. 2010 May 28;73(5):988-91.Hasubanan alkaloids with delta-opioid binding affinity from the aerial parts of Stephania japonica.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528093J Med Chem. 1991 Oct;34(10):3125-32.Conformational restriction of the phenylalanine residue in a cyclic opioid peptide analogue: effects on receptor selectivity and stereospecificity.
Ref 534004J Med Chem. 1993 Mar 19;36(6):708-19.A topochemical approach to explain morphiceptin bioactivity.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 527758Bioorg Med Chem Lett. 2005 Dec 15;15(24):5517-20. Epub 2005 Sep 23.New series of potent delta-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 527916J Med Chem. 2005 Dec 15;48(25):8035-44.Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists.
Ref 527693J Med Chem. 2005 Aug 25;48(17):5608-11.From the potent and selective mu opioid receptor agonist H-Dmt-d-Arg-Phe-Lys-NH(2) to the potent delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH.
Ref 529630J Med Chem. 2008 Aug 28;51(16):5109-17. Epub 2008 Aug 5.Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
Ref 528193J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 552753Progress in developing cholecystokinin (CCK)/gastrin receptor ligands that have therapeutic potential. Curr Opin Pharmacol. 2007 Dec;7(6):583-92. Epub 2007 Nov 9.
Ref 530529J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Ref 530876J Nat Prod. 2010 May 28;73(5):988-91.Hasubanan alkaloids with delta-opioid binding affinity from the aerial parts of Stephania japonica.
Ref 528193J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Ref 528621J Med Chem. 2007 Jan 25;50(2):328-33.Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.
Ref 528376J Med Chem. 2006 Aug 24;49(17):5382-5.Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opioid antagonists.
Ref 528193J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Ref 528621J Med Chem. 2007 Jan 25;50(2):328-33.Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.
Ref 528411J Med Chem. 2006 Sep 7;49(18):5610-7.Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
Ref 528193J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 533376J Med Chem. 1986 Nov;29(11):2370-5.Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for mu opioid receptors.
Ref 528193J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Ref 528193J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Ref 528193J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Ref 528193J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Ref 528058J Med Chem. 2006 Mar 9;49(5):1773-80.Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
Ref 530529J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Ref 528376J Med Chem. 2006 Aug 24;49(17):5382-5.Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opioid antagonists.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 552192Loperamide binding to opiate receptor sites of brain and myenteric plexus. J Pharmacol Exp Ther. 1976 Oct;199(1):131-40.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528996Bioorg Med Chem Lett. 2007 Oct 1;17(19):5349-52. Epub 2007 Aug 11.Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
Ref 530529J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Ref 528996Bioorg Med Chem Lett. 2007 Oct 1;17(19):5349-52. Epub 2007 Aug 11.Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
Ref 530529J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Ref 527332J Med Chem. 2004 Dec 16;47(26):6541-6.Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic.
Ref 529724J Med Chem. 2008 Oct 23;51(20):6334-47. Epub 2008 Sep 27.The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
Ref 530461J Med Chem. 2009 Nov 12;52(21):6926-30.14beta-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and related opioids. Further examples of pseudoirreversible mu opioid receptor antagonists.
Ref 530279J Med Chem. 2009 Dec 10;52(23):7389-96.Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands.
Ref 530052Bioorg Med Chem Lett. 2009 May 1;19(9):2519-23. Epub 2009 Mar 14.The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety.
Ref 529132Bioorg Med Chem Lett. 2007 Dec 15;17(24):6841-6. Epub 2007 Oct 17.Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
Ref 529689J Med Chem. 2008 Oct 9;51(19):5893-6. Epub 2008 Sep 13.Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
Ref 530392Bioorg Med Chem. 2009 Oct 15;17(20):7337-43. Epub 2009 Aug 21.The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.
Ref 527810Bioorg Med Chem Lett. 2006 Jan 1;16(1):146-9. Epub 2005 Oct 19.4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives, a novel class of selective delta-opioid agonists.
Ref 528606J Med Chem. 2007 Jan 11;50(1):165-8.Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
Ref 530392Bioorg Med Chem. 2009 Oct 15;17(20):7337-43. Epub 2009 Aug 21.The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.
Ref 528801J Nat Prod. 2007 May;70(5):872-5. Epub 2007 Apr 24.Indolizidine alkaloids with delta-opioid receptor binding affinity from the leaves of Elaeocarpus fuscoides.
Ref 534004J Med Chem. 1993 Mar 19;36(6):708-19.A topochemical approach to explain morphiceptin bioactivity.
Ref 528300Bioorg Med Chem Lett. 2006 Sep 15;16(18):4946-50. Epub 2006 Jul 7.Synthesis and evaluation of 3-aminopropionyl substituted fentanyl analogues for opioid activity.
Ref 525699J Med Chem. 2000 Feb 24;43(4):569-80.Opiate aromatic pharmacophore structure-activity relationships in CTAP analogues determined by topographical bias, two-dimensional NMR, and biological activity assays.
Ref 528238J Med Chem. 2006 Jun 15;49(12):3653-8.6-N,N-dimethylamino-2,3-naphthalimide: a new environment-sensitive fluorescent probe in delta- and mu-selective opioid peptides.
Ref 528411J Med Chem. 2006 Sep 7;49(18):5610-7.Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
Ref 529429Bioorg Med Chem. 2008 May 15;16(10):5653-64. Epub 2008 Mar 30.Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine.
Ref 529041Bioorg Med Chem. 2007 Nov 15;15(22):6876-81. Epub 2007 Aug 29.A new opioid designed multiple ligand derived from the micro opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic.
Ref 530876J Nat Prod. 2010 May 28;73(5):988-91.Hasubanan alkaloids with delta-opioid binding affinity from the aerial parts of Stephania japonica.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 530707Bioorg Med Chem Lett. 2010 Mar 1;20(5):1507-9. Epub 2010 Jan 25.Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 534631J Med Chem. 1998 May 21;41(11):1980-90.Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
Ref 529401J Med Chem. 2008 Apr 24;51(8):2421-31. Epub 2008 Apr 2.Herkinorin analogues with differential beta-arrestin-2 interactions.
Ref 529991J Med Chem. 2009 Mar 26;52(6):1553-7.14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
Ref 529816Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8. Epub 2008 Nov 7.Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Ref 529816Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8. Epub 2008 Nov 7.Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Ref 533539J Med Chem. 1981 Jul;24(7):903-6.Synthesis of analogues of acetylmethadol and methadol as potential narcotic antagonists.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 529816Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8. Epub 2008 Nov 7.Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Ref 529816Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8. Epub 2008 Nov 7.Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 527461Bioorg Med Chem Lett. 2005 Mar 15;15(6):1583-6.Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide.
Ref 530160Bioorg Med Chem Lett. 2009 Jul 1;19(13):3647-50. Epub 2009 May 3.Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
Ref 530160Bioorg Med Chem Lett. 2009 Jul 1;19(13):3647-50. Epub 2009 May 3.Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 528606J Med Chem. 2007 Jan 11;50(1):165-8.Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
Ref 528058J Med Chem. 2006 Mar 9;49(5):1773-80.Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
Ref 533376J Med Chem. 1986 Nov;29(11):2370-5.Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for mu opioid receptors.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 527951J Med Chem. 2006 Jan 12;49(1):256-62.Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
Ref 528238J Med Chem. 2006 Jun 15;49(12):3653-8.6-N,N-dimethylamino-2,3-naphthalimide: a new environment-sensitive fluorescent probe in delta- and mu-selective opioid peptides.
Ref 530529J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Ref 529132Bioorg Med Chem Lett. 2007 Dec 15;17(24):6841-6. Epub 2007 Oct 17.Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
Ref 534460J Med Chem. 1997 Aug 29;40(18):2948-52.Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 534460J Med Chem. 1997 Aug 29;40(18):2948-52.Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides.
Ref 534460J Med Chem. 1997 Aug 29;40(18):2948-52.Synthesis and pharmacological activity of deltorphin and dermorphin-related glycopeptides.
Ref 528996Bioorg Med Chem Lett. 2007 Oct 1;17(19):5349-52. Epub 2007 Aug 11.Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 534631J Med Chem. 1998 May 21;41(11):1980-90.Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 528442J Nat Prod. 2006 Sep;69(9):1295-9.Grandisines C-G, indolizidine alkaloids from the Australian rainforest tree Elaeocarpus grandis.
Ref 526656J Med Chem. 2003 Jul 3;46(14):3127-37.Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist.
Ref 528375J Med Chem. 2006 Aug 24;49(17):5333-8.Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
Ref 528853J Med Chem. 2007 Jun 14;50(12):2779-86. Epub 2007 May 22.Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
Ref 528269J Med Chem. 2006 Jun 29;49(13):3990-3.New 2',6'-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands.
Ref 531038Bioorg Med Chem. 2010 Aug 15;18(16):6024-30. Epub 2010 Jun 25.Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.
Ref 530428J Med Chem. 2009 Nov 12;52(21):6814-21.The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues.
Ref 528594Bioorg Med Chem. 2007 Feb 15;15(4):1694-702. Epub 2006 Dec 12.Endomorphin-1 analogs with enhanced metabolic stability and systemic analgesic activity: design, synthesis, and pharmacological characterization.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 527951J Med Chem. 2006 Jan 12;49(1):256-62.Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 527951J Med Chem. 2006 Jan 12;49(1):256-62.Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 530707Bioorg Med Chem Lett. 2010 Mar 1;20(5):1507-9. Epub 2010 Jan 25.Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 529704J Med Chem. 2008 Sep 25;51(18):5866-70.Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp].
Ref 529704J Med Chem. 2008 Sep 25;51(18):5866-70.Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp].
Ref 528288J Med Chem. 2006 Jul 13;49(14):4044-7.Discovery of novel triazole-based opioid receptor antagonists.
Ref 528947J Med Chem. 2007 Aug 9;50(16):3765-76. Epub 2007 Jul 11.Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorphan series.
Ref 527916J Med Chem. 2005 Dec 15;48(25):8035-44.Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists.
Ref 529816Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8. Epub 2008 Nov 7.Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Ref 533539J Med Chem. 1981 Jul;24(7):903-6.Synthesis of analogues of acetylmethadol and methadol as potential narcotic antagonists.
Ref 530073Bioorg Med Chem Lett. 2009 May 15;19(10):2792-5. Epub 2009 Mar 26.Design and synthesis of novel delta opioid receptor agonists and their pharmacologies.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 528411J Med Chem. 2006 Sep 7;49(18):5610-7.Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
Ref 529630J Med Chem. 2008 Aug 28;51(16):5109-17. Epub 2008 Aug 5.Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
Ref 528621J Med Chem. 2007 Jan 25;50(2):328-33.Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.
Ref 530447J Med Chem. 2009 Nov 12;52(21):6941-5.Agonist vs antagonist behavior of delta opioid peptides containing novel phenylalanine analogues in place of Tyr(1).
Ref 528190Bioorg Med Chem Lett. 2006 Jul 15;16(14):3688-92. Epub 2006 May 8.Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics inthe position 3 or 4.
Ref 528376J Med Chem. 2006 Aug 24;49(17):5382-5.Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opioid antagonists.
Ref 530013Bioorg Med Chem Lett. 2009 Apr 15;19(8):2289-94. Epub 2009 Feb 25.Syntheses of novel high affinity ligands for opioid receptors.
Ref 529246Bioorg Med Chem. 2008 Mar 15;16(6):3032-8. Epub 2007 Dec 23.Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 529630J Med Chem. 2008 Aug 28;51(16):5109-17. Epub 2008 Aug 5.Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
Ref 529630J Med Chem. 2008 Aug 28;51(16):5109-17. Epub 2008 Aug 5.Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
Ref 528646J Med Chem. 2007 Feb 8;50(3):512-20.Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).
Ref 534004J Med Chem. 1993 Mar 19;36(6):708-19.A topochemical approach to explain morphiceptin bioactivity.
Ref 529202J Med Chem. 2008 Jan 10;51(1):173-7. Epub 2007 Dec 7.Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties.
Ref 528646J Med Chem. 2007 Feb 8;50(3):512-20.Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).
Ref 527461Bioorg Med Chem Lett. 2005 Mar 15;15(6):1583-6.Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528269J Med Chem. 2006 Jun 29;49(13):3990-3.New 2',6'-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528411J Med Chem. 2006 Sep 7;49(18):5610-7.Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
Ref 534004J Med Chem. 1993 Mar 19;36(6):708-19.A topochemical approach to explain morphiceptin bioactivity.
Ref 530160Bioorg Med Chem Lett. 2009 Jul 1;19(13):3647-50. Epub 2009 May 3.Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
Ref 528411J Med Chem. 2006 Sep 7;49(18):5610-7.Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
Ref 529991J Med Chem. 2009 Mar 26;52(6):1553-7.14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
Ref 534004J Med Chem. 1993 Mar 19;36(6):708-19.A topochemical approach to explain morphiceptin bioactivity.
Ref 534004J Med Chem. 1993 Mar 19;36(6):708-19.A topochemical approach to explain morphiceptin bioactivity.
Ref 527916J Med Chem. 2005 Dec 15;48(25):8035-44.Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists.
Ref 528238J Med Chem. 2006 Jun 15;49(12):3653-8.6-N,N-dimethylamino-2,3-naphthalimide: a new environment-sensitive fluorescent probe in delta- and mu-selective opioid peptides.
Ref 527916J Med Chem. 2005 Dec 15;48(25):8035-44.Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists.
Ref 528692J Med Chem. 2007 Mar 22;50(6):1414-7. Epub 2007 Feb 22.Dicarba analogues of the cyclic enkephalin peptides H-Tyr-c[D-Cys-Gly-Phe-D(or L)-Cys]NH(2) retain high opioid activity.
Ref 529630J Med Chem. 2008 Aug 28;51(16):5109-17. Epub 2008 Aug 5.Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
Ref 528411J Med Chem. 2006 Sep 7;49(18):5610-7.Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
Ref 528193J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Ref 533971J Med Chem. 1994 Jan 7;37(1):141-5.Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors.
Ref 528411J Med Chem. 2006 Sep 7;49(18):5610-7.Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
Ref 530529J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Ref 528621J Med Chem. 2007 Jan 25;50(2):328-33.Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.
Ref 528621J Med Chem. 2007 Jan 25;50(2):328-33.Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.
Ref 528621J Med Chem. 2007 Jan 25;50(2):328-33.Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.
Ref 528411J Med Chem. 2006 Sep 7;49(18):5610-7.Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
Ref 528621J Med Chem. 2007 Jan 25;50(2):328-33.Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.
Ref 528621J Med Chem. 2007 Jan 25;50(2):328-33.Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.
Ref 528193J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Ref 527332J Med Chem. 2004 Dec 16;47(26):6541-6.Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 529630J Med Chem. 2008 Aug 28;51(16):5109-17. Epub 2008 Aug 5.Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
Ref 529306J Med Chem. 2008 Mar 13;51(5):1369-76. Epub 2008 Feb 12.A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 530529J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 528692J Med Chem. 2007 Mar 22;50(6):1414-7. Epub 2007 Feb 22.Dicarba analogues of the cyclic enkephalin peptides H-Tyr-c[D-Cys-Gly-Phe-D(or L)-Cys]NH(2) retain high opioid activity.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 529704J Med Chem. 2008 Sep 25;51(18):5866-70.Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp].
Ref 528594Bioorg Med Chem. 2007 Feb 15;15(4):1694-702. Epub 2006 Dec 12.Endomorphin-1 analogs with enhanced metabolic stability and systemic analgesic activity: design, synthesis, and pharmacological characterization.
Ref 528058J Med Chem. 2006 Mar 9;49(5):1773-80.Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
Ref 525699J Med Chem. 2000 Feb 24;43(4):569-80.Opiate aromatic pharmacophore structure-activity relationships in CTAP analogues determined by topographical bias, two-dimensional NMR, and biological activity assays.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 527758Bioorg Med Chem Lett. 2005 Dec 15;15(24):5517-20. Epub 2005 Sep 23.New series of potent delta-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif.
Ref 529480Bioorg Med Chem. 2008 Jun 15;16(12):6415-22. Epub 2008 May 3.Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling.
Ref 529480Bioorg Med Chem. 2008 Jun 15;16(12):6415-22. Epub 2008 May 3.Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling.
Ref 530447J Med Chem. 2009 Nov 12;52(21):6941-5.Agonist vs antagonist behavior of delta opioid peptides containing novel phenylalanine analogues in place of Tyr(1).
Ref 529556J Med Chem. 2008 Jul 24;51(14):4270-9. Epub 2008 Jun 24.New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile.
Ref 527758Bioorg Med Chem Lett. 2005 Dec 15;15(24):5517-20. Epub 2005 Sep 23.New series of potent delta-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif.
Ref 529480Bioorg Med Chem. 2008 Jun 15;16(12):6415-22. Epub 2008 May 3.Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling.
Ref 530013Bioorg Med Chem Lett. 2009 Apr 15;19(8):2289-94. Epub 2009 Feb 25.Syntheses of novel high affinity ligands for opioid receptors.
Ref 528621J Med Chem. 2007 Jan 25;50(2):328-33.Beta-methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.
Ref 533376J Med Chem. 1986 Nov;29(11):2370-5.Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for mu opioid receptors.
Ref 527931J Med Chem. 2005 Dec 29;48(26):8112-4.Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
Ref 531038Bioorg Med Chem. 2010 Aug 15;18(16):6024-30. Epub 2010 Jun 25.Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.
Ref 529041Bioorg Med Chem. 2007 Nov 15;15(22):6876-81. Epub 2007 Aug 29.A new opioid designed multiple ligand derived from the micro opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic.
Ref 527693J Med Chem. 2005 Aug 25;48(17):5608-11.From the potent and selective mu opioid receptor agonist H-Dmt-d-Arg-Phe-Lys-NH(2) to the potent delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH.
Ref 528058J Med Chem. 2006 Mar 9;49(5):1773-80.Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 531165Bioorg Med Chem Lett. 2010 Nov 1;20(21):6302-5. Epub 2010 Aug 21.Design and synthesis of KNT-127, a |A-opioid receptor agonist effective by systemic administration.
Ref 529689J Med Chem. 2008 Oct 9;51(19):5893-6. Epub 2008 Sep 13.Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
Ref 530876J Nat Prod. 2010 May 28;73(5):988-91.Hasubanan alkaloids with delta-opioid binding affinity from the aerial parts of Stephania japonica.
Ref 533376J Med Chem. 1986 Nov;29(11):2370-5.Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for mu opioid receptors.
Ref 528442J Nat Prod. 2006 Sep;69(9):1295-9.Grandisines C-G, indolizidine alkaloids from the Australian rainforest tree Elaeocarpus grandis.
Ref 530780J Med Chem. 2010 Apr 8;53(7):2875-81."Carba"-analogues of fentanyl are opioid receptor agonists.
Ref 529395J Med Chem. 2008 Apr 24;51(8):2571-4. Epub 2008 Mar 28.Blood-brain barrier penetration by two dermorphin tetrapeptide analogues: role of lipophilicity vs structural flexibility.
Ref 533889J Med Chem. 1993 Mar 19;36(6):750-7.Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
Ref 529414Eur J Med Chem. 2008 Nov;43(11):2307-15. Epub 2008 Feb 29.Ligand binding to nucleic acids and proteins: Does selectivity increase with strength?.
Ref 533889J Med Chem. 1993 Mar 19;36(6):750-7.Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
Ref 533889J Med Chem. 1993 Mar 19;36(6):750-7.Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
Ref 530705Bioorg Med Chem Lett. 2010 Mar 1;20(5):1601-3. Epub 2010 Jan 22.Synthesis and evaluation of opioid receptor-binding affinity of elaeocarpenine and its analogs.
Ref 533971J Med Chem. 1994 Jan 7;37(1):141-5.Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors.
Ref 528193J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Ref 528193J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Ref 528193J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Ref 528058J Med Chem. 2006 Mar 9;49(5):1773-80.Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
Ref 529871Bioorg Med Chem Lett. 2009 Jan 15;19(2):365-8. Epub 2008 Nov 24.Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine.
Ref 531519J Med Chem. 1990 Sep;33(9):2456-64.Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.
Ref 528410J Med Chem. 2006 Sep 7;49(18):5597-609.Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.
Ref 528646J Med Chem. 2007 Feb 8;50(3):512-20.Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).
Ref 528996Bioorg Med Chem Lett. 2007 Oct 1;17(19):5349-52. Epub 2007 Aug 11.Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
Ref 527916J Med Chem. 2005 Dec 15;48(25):8035-44.Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 530077Bioorg Med Chem Lett. 2009 May 15;19(10):2811-4. Epub 2009 Mar 26.Design, synthesis, and characterization of 6beta-naltrexol analogs, and their selectivity for in vitro opioid receptor subtypes.
Ref 552189kappa-Opioid receptor effects of butorphanol in rhesus monkeys. J Pharmacol Exp Ther. 1999 Jul;290(1):259-65.
Ref 526656J Med Chem. 2003 Jul 3;46(14):3127-37.Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist.
Ref 530324J Med Chem. 2009 Sep 24;52(18):5685-702.Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747).
Ref 529401J Med Chem. 2008 Apr 24;51(8):2421-31. Epub 2008 Apr 2.Herkinorin analogues with differential beta-arrestin-2 interactions.
Ref 527951J Med Chem. 2006 Jan 12;49(1):256-62.Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
Ref 529306J Med Chem. 2008 Mar 13;51(5):1369-76. Epub 2008 Feb 12.A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
Ref 529306J Med Chem. 2008 Mar 13;51(5):1369-76. Epub 2008 Feb 12.A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
Ref 529306J Med Chem. 2008 Mar 13;51(5):1369-76. Epub 2008 Feb 12.A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
Ref 529238Bioorg Med Chem. 2008 Mar 15;16(6):3218-23. Epub 2007 Dec 31.Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors.
Ref 531092Eur J Med Chem. 2010 Oct;45(10):4594-600. Epub 2010 Jul 21.Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2.

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