Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T27812 | ||||
Target Name | Serotonin transporter (SERT) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Drug Info | IC50 = 1.5 nM | [74] | ||
Drug Info | IC50 = 39 nM | [74] | |||
Drug Info | IC50 = 1.8 nM | [74] | |||
Drug Info | IC50 = 2700 nM | [65] | |||
Drug Info | Ki = 22000 nM | [71] | |||
Amfepramone | Drug Info | IC50 = 311000 nM | [63] | ||
Cocaine | Drug Info | IC50 = 480 nM | [73] | ||
Dexfenfluramine | Drug Info | pKi = 5.41 | [68] | ||
Escitalopram | Drug Info | IC50 = 1.5 nM | [69] | ||
Fluoxetine | Drug Info | IC50 = 6.8 nM | [74] | ||
Fluvoxamine | Drug Info | IC50 = 3.8 nM | [74] | ||
Paroxetine | Drug Info | IC50 = 0.29 nM | [74] | ||
Sertraline | Drug Info | IC50 = 0.19 nM | [74] | ||
Sibutramine | Drug Info | IC50 = 477000 nM | [62] | ||
Tianeptine | Drug Info | IC50 = 11320 nM | |||
Trazodone | Drug Info | IC50 = 0.58 mM | [70] | ||
Venlafaxine | Drug Info | IC50 = 210 nM | |||
Drug Info | Ki = 12 nM | [67] | |||
Drug Info | IC50 = 0.5 nM | [61] | |||
Bicifadine | Drug Info | IC50 = 120 nM | [28] | ||
DOV-216303 | Drug Info | Ki = 13.8 nM | [7] | ||
OPC-14523 | Drug Info | IC50 = 80 nM | [64] | ||
R-sibutramine metabolite | Drug Info | Ki = 5100 nM | [72] | ||
YM-992 | Drug Info | Ki = 21 nM | [61] | ||
Drug Info | Ki = 60.03 nM | [4] | |||
Drug Info | IC50 = 14000 nM | [56] | |||
Drug Info | Ki = 11216 nM | [27] | |||
Drug Info | Ki = 150 nM | [15] | |||
Drug Info | Ki = 2.8 nM | [48] | |||
Drug Info | IC50 = 27 nM | [28] | |||
Drug Info | Ki = 129 nM | [48] | |||
Drug Info | Ki = 1.82 nM | [4] | |||
Drug Info | IC50 = 664 nM | [43] | |||
Drug Info | Ki = 3750 nM | [15] | |||
Drug Info | IC50 = 2000 nM | [59] | |||
Drug Info | Ki = 1.9 nM | [2] | |||
Drug Info | Ki = 3260 nM | [16] | |||
Drug Info | Ki = 364 nM | [47] | |||
Drug Info | Ki = 1140 nM | [47] | |||
Drug Info | IC50 = 5.4 nM | [13] | |||
Drug Info | Ki = 1260 nM | [50] | |||
Drug Info | IC50 = 14000 nM | [56] | |||
Drug Info | Ki = 3260 nM | [16] | |||
Drug Info | Ki = 17 nM | [47] | |||
Drug Info | IC50 = 6900 nM | [52] | |||
Drug Info | IC50 = 46 nM | [11] | |||
Drug Info | IC50 = 6.8 nM | [45] | |||
Drug Info | IC50 = 88 nM | [40] | |||
Drug Info | IC50 = 664 nM | [43] | |||
Drug Info | Ki = 1.82 nM | [4] | |||
Drug Info | IC50 = 13 nM | [13] | |||
Drug Info | Ki = 60.03 nM | [4] | |||
Drug Info | IC50 = 230 nM | [14] | |||
Drug Info | IC50 = 24 nM | [39] | |||
Drug Info | Ki = 2.8 nM | [48] | |||
Drug Info | IC50 = 27 nM | [28] | |||
Drug Info | IC50 = 10000 nM | [29] | |||
Drug Info | Ki = 150 nM | [15] | |||
Drug Info | IC50 = 23 nM | [14] | |||
Drug Info | IC50 = 20 nM | [40] | |||
Drug Info | Ki = 10 nM | [53] | |||
Drug Info | Ki = 1.9 nM | [2] | |||
Drug Info | Ki = 3750 nM | [15] | |||
Drug Info | Ki = 129 nM | [48] | |||
Drug Info | IC50 = 660 nM | [26] | |||
Drug Info | IC50 = 3 nM | [44] | |||
Drug Info | Ki = 11216 nM | [27] | |||
Drug Info | IC50 = 2710 nM | [21] | |||
Drug Info | IC50 = 2000 nM | [59] | |||
Drug Info | IC50 = 10 nM | [44] | |||
((3R,4R)-4-(o-tolyloxy)chroman-3-yl)methanamine | Drug Info | IC50 = 3800 nM | [32] | ||
(+/-)-3-((naphthalen-2-yloxy)methyl)pyrrolidine | Drug Info | IC50 = 25 nM | [40] | ||
(+/-)-nantenine | Drug Info | Ki = 244 nM | [49] | ||
(2R,3R)-iodoreboxetine | Drug Info | Ki = 646 nM | [33] | ||
(2R,3R)-iodoreboxetine | Drug Info | Ki = 646 nM | [33] | ||
(2R,3S)-2-[(2-Iodophenoxy)phenylmethyl]morpholine | Drug Info | Ki = 51.5 nM | [42] | ||
(2R,3S)-2-[(2-Iodophenoxy)phenylmethyl]morpholine | Drug Info | Ki = 51.5 nM | [42] | ||
(2R,3S)-2-[(3-Iodophenoxy)phenylmethyl]morpholine | Drug Info | Ki = 154 nM | [42] | ||
(2R,3S)-2-[(3-Iodophenoxy)phenylmethyl]morpholine | Drug Info | Ki = 154 nM | [42] | ||
(2R,3S)-2-[(4-Iodophenoxy)phenylmethyl]morpholine | Drug Info | Ki = 34.5 nM | [42] | ||
(2R,3S)-2-[(4-Iodophenoxy)phenylmethyl]morpholine | Drug Info | Ki = 34.5 nM | [42] | ||
(2S,3S)-iodoreboxetine | Drug Info | Ki = 2793 nM | [33] | ||
(2S,3S)-iodoreboxetine | Drug Info | Ki = 2793 nM | [33] | ||
(cis)-1,6-diphenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | IC50 = 240 nM | [28] | ||
(cis)-1,6-diphenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | IC50 = 240 nM | [28] | ||
(R)-2-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol | Drug Info | Ki = 8 nM | [53] | ||
(R)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile | Drug Info | IC50 = 42 nM | [40] | ||
(R)-DULOXETINE | Drug Info | Ki = 8.8 nM | [37] | ||
(R)-DULOXETINE | Drug Info | Ki = 8.8 nM | [37] | ||
(R)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide | Drug Info | IC50 = 5 nM | [44] | ||
(R)-N-isopropyl-N-(pyrrolidin-3-yl)-2-naphthamide | Drug Info | IC50 = 15 nM | [44] | ||
(R)-Norfluoxetine | Drug Info | IC50 = 13 nM | [36] | ||
(S)-3-(naphthalen-2-ylmethoxy)pyrrolidine | Drug Info | IC50 = 23 nM | [40] | ||
(S)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile | Drug Info | IC50 = 37 nM | [40] | ||
(S)-NORDULOXETINE | Drug Info | IC50 = 25.6 nM | [45] | ||
(S)-Norfluoxetine | Drug Info | IC50 = 46 nM | [36] | ||
1-(1,2-diphenylethyl)piperazine | Drug Info | IC50 = 14 nM | [13] | ||
1-(1,4-diphenylbutan-2-yl)piperazine | Drug Info | IC50 = 23 nM | [14] | ||
1-(1-(2-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) | Drug Info | Ki = 24 nM | [53] | ||
1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) | Drug Info | Ki = 24 nM | [53] | ||
1-(1-phenyl-2-(2-propoxyphenyl)ethyl)piperazine | Drug Info | Ki = 18 nM | [53] | ||
1-(1-phenyl-2-(pyridin-4-yl)ethyl)piperazine | Drug Info | IC50 = 38 nM | [14] | ||
1-(1-phenyl-2-o-tolylethyl)piperazine | Drug Info | IC50 = 12 nM | [13] | ||
1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX) | Drug Info | Ki = 27 nM | [53] | ||
1-(2-(2-bromophenyl)-1-phenylethyl)piperazine | Drug Info | IC50 = 15 nM | [13] | ||
1-(2-(2-ethylphenyl)-1-phenylethyl)piperazine | Drug Info | IC50 = 16 nM | [13] | ||
1-(2-(2-fluorobenzyloxy)phenyl)piperazine | Drug Info | Ki = 978 nM | [47] | ||
1-(2-(2-methoxyphenyl)-1-phenylethyl)piperazine | Drug Info | Ki = 4 nM | [53] | ||
1-(2-(3-chlorophenyl)-1-phenylethyl)piperazine | Drug Info | IC50 = 9.4 nM | [13] | ||
1-(2-(3-fluorophenoxy)phenyl)piperazine | Drug Info | Ki = 3100 nM | [47] | ||
1-(2-(3-methoxyphenyl)-1-phenylethyl)piperazine | Drug Info | IC50 = 25 nM | [13] | ||
1-(2-(4-fluorophenoxy)phenyl)piperazine | Drug Info | Ki = 994 nM | [47] | ||
1-(2-(6-fluoronaphthalen-2-yl)ethyl)piperazine | Drug Info | IC50 = 11 nM | [40] | ||
1-(2-(naphthalen-1-yl)-1-phenylethyl)piperazine | Drug Info | IC50 = 12 nM | [14] | ||
1-(2-(naphthalen-2-yl)-1-phenylethyl)piperazine | Drug Info | IC50 = 17 nM | [14] | ||
1-(2-(phenoxymethyl)phenyl)piperazine | Drug Info | Ki = 780 nM | [47] | ||
1-(2-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | IC50 = 2020 nM | [11] | ||
1-(2-phenoxyphenyl)piperazine | Drug Info | Ki = 1880 nM | [47] | ||
1-(3,4-Dichloro-phenyl)-3-diethylamino-indan-5-ol | Drug Info | Ki = 0.7 nM | [6] | ||
1-(3,4-Dichloro-phenyl)-3-diethylamino-indan-5-ol | Drug Info | Ki = 0.7 nM | [6] | ||
1-(3,4-Dichloro-phenyl)-3-methylamino-indan-5-ol | Drug Info | Ki = 3 nM | [6] | ||
1-(3,4-Dichloro-phenyl)-3-methylamino-indan-5-ol | Drug Info | Ki = 3 nM | [6] | ||
1-(3-chlorophenyl)-2-(piperidin-1-yl)propan-1-one | Drug Info | Ki = 5479 nM | [46] | ||
1-(3-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | IC50 = 1070 nM | [11] | ||
1-(3-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | IC50 = 4400 nM | [11] | ||
1-(4-Benzylsulfanyl-phenyl)-propylamine | Drug Info | IC50 = 679 nM | [43] | ||
1-(4-Benzylsulfanyl-phenyl)-propylamine | Drug Info | IC50 = 679 nM | [43] | ||
1-(4-bromophenyl)-2-(tert-butylamino)propan-1-one | Drug Info | IC50 = 4508 nM | [52] | ||
1-(4-bromophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | IC50 = 1050 nM | [11] | ||
1-(4-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | IC50 = 197 nM | [11] | ||
1-(4-nitrophenyl)-2-pyrrolidin-1-yl-pentan-1-one | Drug Info | IC50 = 1110 nM | [11] | ||
1-(benzofuran-2-yl)-3-aza-bicyclo[3.1.0]hexane | Drug Info | IC50 = 140 nM | [28] | ||
1-(benzofuran-2-yl)-3-aza-bicyclo[3.1.0]hexane | Drug Info | IC50 = 140 nM | [28] | ||
1-(naphthalen-2-yl)-3-aza-bicyclo[3.1.0]hexane | Drug Info | IC50 = 50 nM | [28] | ||
1-(naphthalen-2-yl)-3-aza-bicyclo[3.1.0]hexane | Drug Info | IC50 = 50 nM | [28] | ||
1-(thiophen-2-yl)-3-aza-bicyclo[3.1.0]hexane | Drug Info | IC50 = 4500 nM | [28] | ||
1-(thiophen-2-yl)-3-aza-bicyclo[3.1.0]hexane | Drug Info | IC50 = 4500 nM | [28] | ||
1-Biphenyl-4-yl-3-aza-bicyclo[3.1.0]hexane | Drug Info | IC50 = 160 nM | [28] | ||
1-Biphenyl-4-yl-3-aza-bicyclo[3.1.0]hexane | Drug Info | IC50 = 160 nM | [28] | ||
1-fluoro-5-phenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | IC50 = 2900 nM | [28] | ||
1-fluoro-5-phenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | IC50 = 2900 nM | [28] | ||
1-Methyl-2-(4-phenylsulfanyl-phenyl)-ethylamine | Drug Info | IC50 = 14330 nM | [43] | ||
1-Methyl-2-(4-phenylsulfanyl-phenyl)-ethylamine | Drug Info | IC50 = 14330 nM | [43] | ||
1-Methyl-4-p-tolyl-piperidine-4-carbonitrile | Drug Info | Ki = 13700 nM | [1] | ||
1-Methyl-4-p-tolyl-piperidine-4-carbonitrile | Drug Info | Ki = 13700 nM | [1] | ||
1-phenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | IC50 = 5200 nM | [28] | ||
1-phenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | IC50 = 5200 nM | [28] | ||
10R-hydroxylobel-7-ene | Drug Info | Ki = 7500 nM | [15] | ||
10R-hydroxylobel-7-ene | Drug Info | Ki = 7500 nM | [15] | ||
10R-hydroxylobelane | Drug Info | Ki = 7300 nM | [15] | ||
10R-hydroxylobelane | Drug Info | Ki = 7300 nM | [15] | ||
10S-hydroxylobel-7-ene | Drug Info | Ki = 19000 nM | [15] | ||
10S-hydroxylobel-7-ene | Drug Info | Ki = 19000 nM | [15] | ||
10S-hydroxylobelane | Drug Info | Ki = 4270 nM | [15] | ||
10S-hydroxylobelane | Drug Info | Ki = 4270 nM | [15] | ||
1S,2R-milnacipran | Drug Info | IC50 = 28 nM | [35] | ||
1S,2R-milnacipran | Drug Info | IC50 = 28 nM | [35] | ||
2-(2'-Aminoethyl)-5-benzyltetrahydrofuran | Drug Info | IC50 = 2260 nM | [39] | ||
2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | Ki = 57 nM | [50] | ||
2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | Ki = 728 nM | [50] | ||
2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine | Drug Info | Ki = 610 nM | [50] | ||
2-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile | Drug Info | IC50 = 87 nM | [13] | ||
2-(3-Methyl-piperazin-1-yl)-6-nitro-quinoline | Drug Info | Ki = 22.19 nM | [2] | ||
2-(3-Methyl-piperazin-1-yl)-6-nitro-quinoline | Drug Info | Ki = 22.19 nM | [2] | ||
2-(Aminomethyl)-5-(1'-naphthethyl)tetrahydrofuran | Drug Info | IC50 = 23 nM | [39] | ||
2-(Aminomethyl)-5-(2'-naphthyl)tetrahydrofuran | Drug Info | IC50 = 4 nM | [39] | ||
2-(Aminomethyl)-5-phenethyltetrahydrofuran | Drug Info | IC50 = 129 nM | [39] | ||
2-(N-Cyclopropylamino)-3-chloropropiophenone | Drug Info | Ki = 3420 nM | [46] | ||
2-(N-tert-Butylamino)-3',4'-dichloropropiophenone | Drug Info | Ki = 1480 nM | [46] | ||
2-(tert-butylamino)-1-(3-chlorophenyl)butan-1-one | Drug Info | IC50 = 16000 nM | [52] | ||
2-(tert-Butylamino)-3',4'-dichlorobutyrophenone | Drug Info | IC50 = 790 nM | [46] | ||
2-(tert-Butylamino)-3',4'-dichloropentanophenone | Drug Info | Ki = 842 nM | [46] | ||
2-Amino-1-(4-ethylthiophenyl)butane | Drug Info | IC50 = 1290 nM | [43] | ||
2-Amino-1-(4-ethylthiophenyl)butane | Drug Info | IC50 = 1290 nM | [43] | ||
2-Amino-1-(4-ethylthiophenyl)propane | Drug Info | IC50 = 1403 nM | [43] | ||
2-Amino-1-(4-ethylthiophenyl)propane | Drug Info | IC50 = 1403 nM | [43] | ||
2-Amino-1-(4-methylthiophenyl)butane | Drug Info | IC50 = 611 nM | [43] | ||
2-Amino-1-(4-methylthiophenyl)butane | Drug Info | IC50 = 611 nM | [43] | ||
2-Amino-1-(4-methylthiophenyl)propane | Drug Info | IC50 = 74 nM | [43] | ||
2-Amino-1-(4-methylthiophenyl)propane | Drug Info | IC50 = 74 nM | [43] | ||
2-Aminomethyl-5-(p-bromophenyl)tetrahydrofuran | Drug Info | IC50 = 50 nM | [39] | ||
2-Aminomethyl-5-(p-chlorophenyl)tetrahydrofuran | Drug Info | IC50 = 32 nM | [39] | ||
2-Aminomethyl-5-(p-methoxyphenyl)tetrahydrofuran | Drug Info | IC50 = 617 nM | [39] | ||
2-Aminomethyl-5-(p-t-butylphenyl)tetrahydrofuran | Drug Info | IC50 = 636 nM | [39] | ||
2-Aminomethyl-5-(phenyl)tetrahydrofuran | Drug Info | IC50 = 1714 nM | [39] | ||
2-N,N-Dimethylamino-1-(4-methylthiophenyl)propane | Drug Info | IC50 = 520 nM | [43] | ||
2-N,N-Dimethylamino-1-(4-methylthiophenyl)propane | Drug Info | IC50 = 520 nM | [43] | ||
2-N-(Isopropyl)amino-1-(4-methylthiophenyl)butane | Drug Info | IC50 = 1939 nM | [43] | ||
2-N-(Isopropyl)amino-1-(4-methylthiophenyl)butane | Drug Info | IC50 = 1939 nM | [43] | ||
2-N-(n-Propyl)amino-1-(4-methylthiophenyl)butane | Drug Info | IC50 = 621 nM | [43] | ||
2-N-(n-Propyl)amino-1-(4-methylthiophenyl)butane | Drug Info | IC50 = 621 nM | [43] | ||
2-N-Allylamino-1-(4-methylthiophenyl)propan | Drug Info | IC50 = 524 nM | [43] | ||
2-N-Allylamino-1-(4-methylthiophenyl)propan | Drug Info | IC50 = 524 nM | [43] | ||
2-N-Cyclopropylamino-1-(4-methylthiophenyl)butane | Drug Info | IC50 = 872 nM | [43] | ||
2-N-Cyclopropylamino-1-(4-methylthiophenyl)butane | Drug Info | IC50 = 872 nM | [43] | ||
2-N-Ethylamino-1-(4-ethylthiophenyl)butane | Drug Info | IC50 = 1804 nM | [43] | ||
2-N-Ethylamino-1-(4-ethylthiophenyl)butane | Drug Info | IC50 = 1804 nM | [43] | ||
2-N-Ethylamino-1-(4-ethylthiophenyl)propane | Drug Info | IC50 = 478 nM | [43] | ||
2-N-Ethylamino-1-(4-ethylthiophenyl)propane | Drug Info | IC50 = 478 nM | [43] | ||
2-N-Ethylamino-1-(4-methylthiophenyl)butane | Drug Info | IC50 = 823 nM | [43] | ||
2-N-Ethylamino-1-(4-methylthiophenyl)butane | Drug Info | IC50 = 823 nM | [43] | ||
2-N-Ethylamino-1-(4-methylthiophenyl)propane | Drug Info | IC50 = 963 nM | [43] | ||
2-N-Ethylamino-1-(4-methylthiophenyl)propane | Drug Info | IC50 = 963 nM | [43] | ||
2-N-Hydroxyamino-1-(4-ethylthiophenyl)butane | Drug Info | IC50 = 1446 nM | [43] | ||
2-N-Hydroxyamino-1-(4-ethylthiophenyl)butane | Drug Info | IC50 = 1446 nM | [43] | ||
2-N-Hydroxyamino-1-(4-ethylthiophenyl)propane | Drug Info | IC50 = 625 nM | [43] | ||
2-N-Hydroxyamino-1-(4-ethylthiophenyl)propane | Drug Info | IC50 = 625 nM | [43] | ||
2-N-Hydroxyamino-1-(4-methylthiophenyl)butane | Drug Info | IC50 = 598 nM | [43] | ||
2-N-Hydroxyamino-1-(4-methylthiophenyl)butane | Drug Info | IC50 = 598 nM | [43] | ||
2-N-Hydroxyamino-1-(4-methylthiophenyl)propane | Drug Info | IC50 = 436 nM | [43] | ||
2-N-Hydroxyamino-1-(4-methylthiophenyl)propane | Drug Info | IC50 = 436 nM | [43] | ||
2-N-Methylamino-1-(4-ethylthiophenyl)propane | Drug Info | IC50 = 724 nM | [43] | ||
2-N-Methylamino-1-(4-ethylthiophenyl)propane | Drug Info | IC50 = 724 nM | [43] | ||
2-N-Methylamino-1-(4-methylthiophenyl)butane | Drug Info | IC50 = 437 nM | [43] | ||
2-N-Methylamino-1-(4-methylthiophenyl)butane | Drug Info | IC50 = 437 nM | [43] | ||
2-N-Methylamino-1-(4-methylthiophenyl)propane | Drug Info | IC50 = 417 nM | [43] | ||
2-N-Methylamino-1-(4-methylthiophenyl)propane | Drug Info | IC50 = 417 nM | [43] | ||
2-N-Propargylamino-1-(4-methylthiophenyl)butane | Drug Info | IC50 = 399 nM | [43] | ||
2-N-Propargylamino-1-(4-methylthiophenyl)butane | Drug Info | IC50 = 399 nM | [43] | ||
2-N-Propargylamino-1-(4-methylthiophenyl)propane | Drug Info | IC50 = 688 nM | [43] | ||
2-N-Propargylamino-1-(4-methylthiophenyl)propane | Drug Info | IC50 = 688 nM | [43] | ||
2-Naphthalen-2-ylmethyl-4,5-dihydro-1H-imidazole | Drug Info | IC50 = 887 nM | [60] | ||
2-Naphthalen-2-ylmethyl-4,5-dihydro-1H-imidazole | Drug Info | IC50 = 887 nM | [60] | ||
2-phenoxy-3-(piperidin-4-yl)pyridine | Drug Info | Ki = 1890 nM | [50] | ||
3-(1H-indol-1-yl)-N-methyl-3-phenylpropan-1-amine | Drug Info | IC50 = 327 nM | [34] | ||
3-(1H-indol-3-yl)-N,N-dimethylpropan-1-amine | Drug Info | IC50 = 58 nM | [22] | ||
3-(2-phenyl-2-(piperazin-1-yl)ethyl)benzamide | Drug Info | IC50 = 210 nM | [13] | ||
3-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile | Drug Info | IC50 = 4 nM | [13] | ||
3-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol | Drug Info | IC50 = 9.5 nM | [13] | ||
3-(3,4-dichlorophenyl)-2-nortropene | Drug Info | Ki = 0.3 nM | [48] | ||
3-(3,4-dichlorophenyl)-2-nortropene | Drug Info | Ki = 0.3 nM | [48] | ||
3-(3-aminocyclopentyl)-1H-indole-5-carbonitrile | Drug Info | IC50 = 32 nM | [55] | ||
3-(4-Trifluoromethylphenyl)-2-nortropene | Drug Info | Ki = 1.8 nM | [48] | ||
3-(4-Trifluoromethylphenyl)-2-nortropene | Drug Info | Ki = 1.8 nM | [48] | ||
3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine | Drug Info | Ki = 292 nM | [50] | ||
3-alpha-Phenylmethoxy-3-beta-phenyl-nortropane | Drug Info | Ki = 247 nM | [48] | ||
3-alpha-Phenylmethoxy-3-beta-phenyl-nortropane | Drug Info | Ki = 247 nM | [48] | ||
3-Bromo-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | Ki = 12.62 nM | [2] | ||
3-Bromo-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | Ki = 12.62 nM | [2] | ||
3-p-Tolyl-8-aza-bicyclo[3.2.1]octane | Drug Info | Ki = 46 nM | [3] | ||
3-p-Tolyl-8-aza-bicyclo[3.2.1]octane | Drug Info | Ki = 46 nM | [3] | ||
3-Phenyl-2-nortropene | Drug Info | Ki = 176 nM | [48] | ||
3-Phenyl-2-nortropene | Drug Info | Ki = 176 nM | [48] | ||
3alpha-(bis-chloro-phenylmethoxy)tropane | Drug Info | Ki = 1640 nM | [16] | ||
3alpha-(bis-chloro-phenylmethoxy)tropane | Drug Info | Ki = 1640 nM | [16] | ||
4-((naphthalen-2-yloxy)methyl)piperidine | Drug Info | IC50 = 8 nM | [40] | ||
4-(1H-indol-3-yl)-N,N-dimethylcyclohex-3-enamine | Drug Info | IC50 = 3.1 nM | [18] | ||
4-(2-((3-fluorophenoxy)methyl)phenyl)piperidine | Drug Info | Ki = 49 nM | [47] | ||
4-(2-((dimethylamino)methyl)phenoxy)benzonitrile | Drug Info | IC50 = 60 nM | [30] | ||
4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine | Drug Info | Ki = 26 nM | [47] | ||
4-(2-(2-fluorobenzyloxy)phenyl)piperidine | Drug Info | Ki = 56 nM | [47] | ||
4-(2-(3-chlorophenoxy)phenyl)piperidine | Drug Info | Ki = 211 nM | [47] | ||
4-(2-(3-fluorophenoxy)-4-methylphenyl)piperidine | Drug Info | Ki = 2 nM | [47] | ||
4-(2-(3-fluorophenoxy)phenyl)piperidine | Drug Info | Ki = 901 nM | [47] | ||
4-(2-(4-fluorobenzyloxy)phenyl)piperidine | Drug Info | Ki = 274 nM | [47] | ||
4-(2-(4-fluorophenoxy)-4-methylphenyl)piperidine | Drug Info | Ki = 427 nM | [47] | ||
4-(2-(4-fluorophenoxy)phenyl)piperidine | Drug Info | Ki = 319 nM | [47] | ||
4-(2-(benzyloxy)-3-fluorophenyl)piperidine | Drug Info | Ki = 2970 nM | [47] | ||
4-(2-(benzyloxy)-6-fluorophenyl)piperidine | Drug Info | Ki = 28 nM | [47] | ||
4-(2-(benzyloxy)phenyl)piperidine | Drug Info | Ki = 74 nM | [47] | ||
4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine | Drug Info | Ki = 1040 nM | [47] | ||
4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine | Drug Info | Ki = 157 nM | [47] | ||
4-(2-fluoro-6-phenoxyphenyl)piperidine | Drug Info | Ki = 706 nM | [47] | ||
4-(2-phenoxyphenyl)piperidine | Drug Info | Ki = 1760 nM | [47] | ||
4-(3-fluoro-2-phenoxyphenyl)piperidine | Drug Info | Ki = 2330 nM | [47] | ||
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | Ki < 1000 nM | [54] | ||
4-Allyl-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | Ki = 1.67 nM | [4] | ||
4-Allyl-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | Ki = 1.67 nM | [4] | ||
4-Benzyl-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | Ki = 126.86 nM | [4] | ||
4-Benzyl-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | Ki = 126.86 nM | [4] | ||
4-Bromo-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | Ki = 0.37 nM | [4] | ||
4-Bromo-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | Ki = 0.37 nM | [4] | ||
4-Furan-2-yl-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | Ki = 5.23 nM | [4] | ||
4-Furan-2-yl-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | Ki = 5.23 nM | [4] | ||
4-Iodo-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | Ki = 1.73 nM | [4] | ||
4-Iodo-6-nitro-2-piperazin-1-yl-quinoline | Drug Info | Ki = 1.73 nM | [4] | ||
6,6-dimethyl-1-phenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | IC50 = 1800 nM | [28] | ||
6,6-dimethyl-1-phenyl-3-aza-bicyclo[3.1.0]hexane | Drug Info | IC50 = 1800 nM | [28] | ||
6,8-Dinitro-2-piperazin-1-yl-quinoline | Drug Info | Ki = 312.85 nM | [2] | ||
6,8-Dinitro-2-piperazin-1-yl-quinoline | Drug Info | Ki = 312.85 nM | [2] | ||
6-(3-aza-bicyclo[3.1.0]hexan-1-yl)quinoline | Drug Info | IC50 = 640 nM | [28] | ||
6-(3-aza-bicyclo[3.1.0]hexan-1-yl)quinoline | Drug Info | IC50 = 640 nM | [28] | ||
6-(piperidin-4-ylmethoxy)-2-naphthonitrile | Drug Info | IC50 = 15 nM | [40] | ||
6-Bromo-2-piperazin-1-yl-quinoline | Drug Info | Ki = 0.91 nM | [2] | ||
6-Bromo-2-piperazin-1-yl-quinoline | Drug Info | Ki = 0.91 nM | [2] | ||
6-Chloro-2-piperazin-1-yl-quinoline | Drug Info | Ki = 1.68 nM | [2] | ||
6-Chloro-2-piperazin-1-yl-quinoline | Drug Info | Ki = 1.68 nM | [2] | ||
6-Iodo-2-piperazin-1-yl-quinoline | Drug Info | Ki = 6.6 nM | [2] | ||
6-Iodo-2-piperazin-1-yl-quinoline | Drug Info | Ki = 6.6 nM | [2] | ||
6-nitroquipazine | Drug Info | Ki = 0.24 nM | [17] | ||
6-nitroquipazine | Drug Info | Ki = 0.24 nM | [17] | ||
7-(piperidin-4-ylmethoxy)-2-naphthonitrile | Drug Info | IC50 = 3 nM | [40] | ||
8-Methyl-3-p-tolyl-8-aza-bicyclo[3.2.1]octane | Drug Info | Ki = 390 nM | [3] | ||
8-Methyl-3-p-tolyl-8-aza-bicyclo[3.2.1]octane | Drug Info | Ki = 390 nM | [3] | ||
8R-hydroxylobel-9-ene | Drug Info | Ki = 860 nM | [51] | ||
8R-hydroxylobel-9-ene | Drug Info | Ki = 860 nM | [51] | ||
8S-hydroxylobelane | Drug Info | Ki = 2220 nM | [15] | ||
8S-hydroxylobelane | Drug Info | Ki = 2220 nM | [15] | ||
A-80426 | Drug Info | IC50 = 13.1 nM | [60] | ||
A-80426 | Drug Info | IC50 = 13.1 nM | [60] | ||
Beta-methoxyamphetamine | Drug Info | IC50 = 173 nM | [43] | ||
Beta-methoxyamphetamine | Drug Info | IC50 = 173 nM | [43] | ||
Biphenyl-2-ylmethyl-(S)-pyrrolidin-3-yl-amine | Drug Info | Ki = 1070 nM | [31] | ||
COCAINE.HCL | Drug Info | Ki = 306 nM | [20] | ||
COCAINE.HCL | Drug Info | Ki = 306 nM | [20] | ||
Cyclohexyl-(3,4-dichloro-phenyl)-acetonitrile | Drug Info | IC50 = 8000 nM | [5] | ||
Cyclohexyl-(3,4-dichloro-phenyl)-acetonitrile | Drug Info | IC50 = 8000 nM | [5] | ||
Cyclopentyl-(3,4-dichloro-phenyl)-acetonitrile | Drug Info | IC50 = 10000 nM | [5] | ||
Cyclopentyl-(3,4-dichloro-phenyl)-acetonitrile | Drug Info | IC50 = 10000 nM | [5] | ||
D-211A | Drug Info | Ki = 11884 nM | [27] | ||
D-211A | Drug Info | Ki = 11884 nM | [27] | ||
D-211B | Drug Info | Ki = 1484 nM | [27] | ||
D-211B | Drug Info | Ki = 1484 nM | [27] | ||
D-254C | Drug Info | Ki = 1391 nM | [27] | ||
D-254C | Drug Info | Ki = 1391 nM | [27] | ||
D-257A | Drug Info | Ki = 12904 nM | [27] | ||
D-257A | Drug Info | Ki = 12904 nM | [27] | ||
D-257C | Drug Info | Ki = 7414 nM | [27] | ||
D-257C | Drug Info | Ki = 7414 nM | [27] | ||
Erythro-3,4-dichloromethylphenidate hydrochloride | Drug Info | Ki = 2570 nM | [20] | ||
Erythro-3,4-dichloromethylphenidate hydrochloride | Drug Info | Ki = 2570 nM | [20] | ||
Isobutyl-(4-methyl-benzyl)-piperidin-4-yl-amine | Drug Info | Ki = 0.99 nM | [12] | ||
JNJ-28583867 | Drug Info | Ki = 3.7 nM | [24] | ||
KF-A5 | Drug Info | IC50 = 7800 nM | [23] | ||
KF-A6 | Drug Info | IC50 = 3500 nM | [23] | ||
LITOXETINE | Drug Info | IC50 = 5.9 nM | [44] | ||
MDL-28618 | Drug Info | IC50 = 190 nM | [32] | ||
METHYLENEDIOXYAMPHETAMINE | Drug Info | IC50 = 478 nM | [43] | ||
METHYLENEDIOXYAMPHETAMINE | Drug Info | IC50 = 478 nM | [43] | ||
METHYLENEDIOXYMETHAMPHETAMINE | Drug Info | IC50 = 1060 nM | [43] | ||
METHYLENEDIOXYMETHAMPHETAMINE | Drug Info | IC50 = 1060 nM | [43] | ||
N*1*-(6-Nitro-quinolin-2-yl)-ethane-1,2-diamine | Drug Info | Ki = 164.3 nM | [2] | ||
N*1*-(6-Nitro-quinolin-2-yl)-ethane-1,2-diamine | Drug Info | Ki = 164.3 nM | [2] | ||
N-(2-oxazolemethyl)milnacipran | Drug Info | IC50 = 1600 nM | [25] | ||
N-(piperidin-4-yl)-N-propyl-2-naphthamide | Drug Info | IC50 = 28.3 nM | [44] | ||
N-benzyl-N-isobutylpiperidin-4-amine | Drug Info | Ki = 8.4 nM | [12] | ||
NISOXETINE | Drug Info | Ki = 277 nM | [37] | ||
NISOXETINE | Drug Info | Ki = 277 nM | [37] | ||
O-DESMETHYL TRAMADOL | Drug Info | IC50 = 4600 nM | [10] | ||
Para-chloroamphetamine | Drug Info | IC50 = 182 nM | [43] | ||
Para-chloroamphetamine | Drug Info | IC50 = 182 nM | [43] | ||
PF-18298 | Drug Info | Ki = 6 nM | [53] | ||
PF-3409409 | Drug Info | Ki = 224 nM | [41] | ||
PYROVALERONE | Drug Info | IC50 = 2780 nM | [11] | ||
QUIPAZINE | Drug Info | Ki = 63 nM | [2] | ||
QUIPAZINE | Drug Info | Ki = 63 nM | [2] | ||
R-226161 | Drug Info | Ki = 1.2 nM | [19] | ||
Reboxetine | Drug Info | Ki = 661 nM | [38] | ||
S-34324 | Drug Info | Ki = 77 nM | [9] | ||
TEFLUDAZINE | Drug Info | IC50 = 7000 nM | [57] | ||
TEFLUDAZINE | Drug Info | IC50 = 7000 nM | [57] | ||
Threo-1-aza-5-phenyl[4.4.0]decane hydrochloride | Drug Info | Ki = 5140 nM | [20] | ||
Threo-1-aza-5-phenyl[4.4.0]decane hydrochloride | Drug Info | Ki = 5140 nM | [20] | ||
Threo-3,4-dichlororitalinol hydrochloride | Drug Info | Ki = 276 nM | [20] | ||
Threo-3,4-dichlororitalinol hydrochloride | Drug Info | Ki = 276 nM | [20] | ||
WIN-35065 | Drug Info | Ki = 1900 nM | [21] | ||
WIN-35065 | Drug Info | Ki = 1900 nM | [21] | ||
WIN-35066-2 | Drug Info | Ki = 178 nM | [8] | ||
ZIMELIDINE | Drug Info | IC50 = 4500 nM | [58] | ||
ZIMELIDINE | Drug Info | IC50 = 4500 nM | [58] | ||
[3-(3,4-Dichloro-phenyl)-indan-1-yl]-methyl-amine | Drug Info | Ki = 3 nM | [6] | ||
[3-(3,4-Dichloro-phenyl)-indan-1-yl]-methyl-amine | Drug Info | Ki = 3 nM | [6] | ||
[3H]WIN35428 | Drug Info | IC50 = 5060 nM | [59] | ||
[3H]WIN35428 | Drug Info | IC50 = 5060 nM | [59] | ||
Action against Disease Model | Drug Info | EMD 68843 (vilazodone) is a novel compound with combined high affinity and selectivity for the 5-hydroxytryptamine (5-HT) transporter and 5-HT(1A) receptors. In Sf9 cells, EMD 68843 increased guanosine 5'-O-(3-[(35)S]thiotriphosphate) binding to 69% of the magnitude of the full 5-HT(1A) receptor agonist R-(1)-trans-8-hydroxy-2-[N-n-propyl-N-(39-iodo-29-propenyl)] aminotetralin (8-OH-PIPAT), indicating that it is a partial agonist at 5-HT(1A) receptors. Acute, systemic administration of EMD 68843 produced a larger maximal increase of extracellular 5-HT than the SSRI fluoxetine in both the ventral hippocampus (HPv) (558 versus 274%) and the frontal cortex (FC) (527 versus 165%). Regional differences in the response to the two drugs were also observed. These effects maybe attributed to the differential regulation of 5-HT release in the HPv and FC by 5-HT(1A) autoreceptors. When challenged with the 5-HT(1A) receptor agonist 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT), EMD 68843-induced increases in extracellular 5-HT were greatly reduced in the HPv but to a lesser extent in the FC. In behavioral studies, EMD 68843 produced antidepressant-like effects in the forced swimming test in both rats and mice but only within a narrow dosage range. Like fluoxetine, | [66] | ||
References | |||||
REF 1 | Synthesis, dopamine and serotonin transporter binding affinities of novel analogues of meperidine. Bioorg Med Chem Lett. 1999 Dec 6;9(23):3273-6. | ||||
REF 2 | Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 1. Bioorg Med Chem Lett. 2000 Jul 17;10(14):1559-62. | ||||
REF 3 | 3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter. Bioorg Med Chem Lett. 2000 Nov 6;10(21):2445-7. | ||||
REF 4 | Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 2: 4-substituted 6-nitroquipazines. Bioorg Med Chem Lett. 2002 Mar 11;12(5):811-5. | ||||
REF 5 | Synthesis and evaluation of dopamine and serotonin transporter inhibition by oxacyclic and carbacyclic analogues of methylphenidate. J Med Chem. 2003 Apr 10;46(8):1538-45. | ||||
REF 6 | Synthesis and pharmacological evaluation of 3-(3,4-dichlorophenyl)-1-indanamine derivatives as nonselective ligands for biogenic amine transporters. J Med Chem. 2004 May 6;47(10):2624-34. | ||||
REF 7 | DOV 216,303, a "triple" reuptake inhibitor: safety, tolerability, and pharmacokinetic profile. J Clin Pharmacol. 2004 Dec;44(12):1360-7. | ||||
REF 8 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl e... J Med Chem. 2004 Dec 2;47(25):6401-9. | ||||
REF 9 | Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking... J Med Chem. 2005 Mar 24;48(6):2054-71. | ||||
REF 10 | Derivatives of tramadol for increased duration of effect. Bioorg Med Chem Lett. 2006 Feb;16(3):691-4. | ||||
REF 11 | 1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors. J Med Chem. 2006 Feb 23;49(4):1420-32. | ||||
REF 12 | N-Alkyl-N-arylmethylpiperidin-4-amines: novel dual inhibitors of serotonin and norepinephrine reuptake. Bioorg Med Chem Lett. 2006 May 15;16(10):2714-8. | ||||
REF 13 | N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4345-8. | ||||
REF 14 | Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4349-53. | ||||
REF 15 | Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5018-21. | ||||
REF 16 | Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogue... J Med Chem. 2006 Oct 19;49(21):6391-9. | ||||
REF 17 | Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 5: 2'-Substituted 6-nitroquipazines. Bioorg Med Chem. 2007 May 15;15(10):3499-504. | ||||
REF 18 | Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3099-104. | ||||
REF 19 | Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-a... Bioorg Med Chem. 2007 Jun 1;15(11):3649-60. | ||||
REF 20 | Synthesis and pharmacology of site-specific cocaine abuse treatment agents: restricted rotation analogues of methylphenidate. J Med Chem. 2007 May 31;50(11):2718-31. | ||||
REF 21 | Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-... J Med Chem. 2007 Jul 26;50(15):3686-95. | ||||
REF 22 | Conformationally restricted homotryptamines. Part 4: Heterocyclic and naphthyl analogs of a potent selective serotonin reuptake inhibitor. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5647-51. | ||||
REF 23 | Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. Antimicrob Agents Chemother. 2007 Nov;51(11):4133-40. | ||||
REF 24 | Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors. Bioorg Med Chem Lett. 2008 Jan 1;18(1):39-43. | ||||
REF 25 | Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1346-9. | ||||
REF 26 | 1-(2-Phenoxyphenyl)methanamines: SAR for dual serotonin/noradrenaline reuptake inhibition, metabolic stability and hERG affinity. Bioorg Med Chem Lett. 2008 Jan 15;18(2):596-9. | ||||
REF 27 | Further structural optimization of cis-(6-benzhydryl-piperidin-3-yl)-benzylamine and 1,4-diazabicyclo[3.3.1]nonane derivatives by introducing an ex... Bioorg Med Chem. 2008 Mar 15;16(6):2769-78. | ||||
REF 28 | Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3682-6. | ||||
REF 29 | Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI). Bioorg Med Chem Lett. 2008 Jul 15;18(14):4224-7. | ||||
REF 30 | Designing rapid onset selective serotonin re-uptake inhibitors. 2: structure-activity relationships of substituted (aryl)benzylamines. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4018-21. | ||||
REF 31 | Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modu... Bioorg Med Chem Lett. 2008 Aug 1;18(15):4355-9. | ||||
REF 32 | Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4495-8. | ||||
REF 33 | New iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter. Bioorg Med Chem Lett. 2008 Sep 15;18(18):4940-3. | ||||
REF 34 | Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6067-70. | ||||
REF 35 | Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropath... J Med Chem. 2008 Nov 27;51(22):7265-72. | ||||
REF 36 | Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression. Bioorg Med Chem. 2009 Jan 1;17(1):337-43. | ||||
REF 37 | 1-Naphthyl and 4-indolyl arylalkylamines as selective monoamine reuptake inhibitors. Bioorg Med Chem Lett. 2009 Jan 1;19(1):58-61. | ||||
REF 38 | Synthesis, radiosynthesis, and biological evaluation of carbon-11 and fluorine-18 labeled reboxetine analogues: potential positron emission tomogra... J Med Chem. 2009 Jan 8;52(1):62-73. | ||||
REF 39 | 2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors. Bioorg Med Chem. 2009 Mar 1;17(5):2047-68. | ||||
REF 40 | Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2329-32. | ||||
REF 41 | Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more po... Bioorg Med Chem Lett. 2009 Aug 15;19(16):4579-83. | ||||
REF 42 | Design and synthesis of (2R,3S)-iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter. Bioorg Med Chem Lett. 2009 Sep 1;19(17):4996-8. | ||||
REF 43 | Synthesis and serotonin transporter activity of sulphur-substituted alpha-alkyl phenethylamines as a new class of anticancer agents. Eur J Med Chem. 2009 Dec;44(12):4862-88. | ||||
REF 44 | Bioorg Med Chem Lett. 2009 Oct 15;19(20):5893-7. Epub 2009 Aug 21.Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2. | ||||
REF 45 | Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression. Bioorg Med Chem. 2009 Oct 1;17(19):6890-7. | ||||
REF 46 | Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction. J Med Chem. 2009 Nov 12;52(21):6768-81. | ||||
REF 47 | Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1... Bioorg Med Chem Lett. 2009 Dec 1;19(23):6604-7. | ||||
REF 48 | Synthesis and monoamine transporter affinity of 3alpha-arylmethoxy-3beta-arylnortropanes. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6865-8. | ||||
REF 49 | Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. | ||||
REF 50 | Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agon... Bioorg Med Chem Lett. 2010 Feb 1;20(3):1114-7. | ||||
REF 51 | Lobeline esters as novel ligands for neuronal nicotinic acetylcholine receptors and neurotransmitter transporters. Bioorg Med Chem. 2010 Jan 15;18(2):640-9. | ||||
REF 52 | Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation. J Med Chem. 2010 Mar 11;53(5):2204-14. | ||||
REF 53 | Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reduc... Bioorg Med Chem Lett. 2010 Jun 15;20(12):3788-92. | ||||
REF 54 | Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97. | ||||
REF 55 | Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors. J Med Chem. 2010 Nov 11;53(21):7564-72. | ||||
REF 56 | Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity. J Med Chem. 1988 Dec;31(12):2247-56. | ||||
REF 57 | Neuroleptic activity and dopamine-uptake inhibition in 1-piperazino-3-phenylindans. J Med Chem. 1983 Jul;26(7):935-47. | ||||
REF 58 | Nontricyclic antidepressant agents derived from cis- and trans-1-amino-4-aryltetralins. J Med Chem. 1984 Nov;27(11):1508-15. | ||||
REF 59 | 3 alpha-(4'-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters: novel ligands with high affinity and selectivity at the dopamine trans... J Med Chem. 1996 Oct 11;39(21):4139-41. | ||||
REF 60 | Structure-activity studies for a novel series of N-(arylethyl)-N-(1,2,3,4-tetrahydronaphthalen-1-ylmethyl)-N-methylamine s possessing dual 5-HT upt... J Med Chem. 1997 Mar 28;40(7):1049-62. | ||||
REF 61 | Serotonin reuptake inhibitors: the corner stone in treatment of depression for half a century--a medicinal chemistry survey. Curr Top Med Chem. 2006;6(17):1801-23. | ||||
REF 62 | Sibutramine, a serotonin uptake inhibitor, increases dopamine concentrations in rat striatal and hypothalamic extracellular fluid. Neuropharmacology. 2000 Sep;39(12):2352-9. | ||||
REF 63 | Uptake and release effects of diethylpropion and its metabolites with biogenic amine transporters. Bioorg Med Chem. 2000 Dec;8(12):2689-92. | ||||
REF 64 | Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523. Neuropharmacology. 2001 Dec;41(8):976-88. | ||||
REF 65 | Block of volume-regulated anion channels by selective serotonin reuptake inhibitors. Naunyn Schmiedebergs Arch Pharmacol. 2002 Aug;366(2):158-65. | ||||
REF 66 | Behavioral and neurochemical effects of 5-(4-[4-(5-Cyano-3-indolyl)-butyl)-butyl]-1-piperazinyl)-benzofuran-2-carboxamide (EMD 68843): a combined selective inhibitor of serotonin reuptake and 5-hydroxytryptamine(1A) receptor partial agonist. J Pharmacol Exp Ther. 2002 Sep;302(3):1220-7. | ||||
REF 67 | Antidepressant-like actions of DOV 21,947: a "triple" reuptake inhibitor. Eur J Pharmacol. 2003 Feb 14;461(2-3):99-104. | ||||
REF 68 | 5-HT2C receptor agonists as potential drugs for the treatment of obesity. Curr Top Med Chem. 2003;3(8):885-97. | ||||
REF 69 | Stereoisomers in Psychiatry: The Case of Escitalopram. Prim Care Companion J Clin Psychiatry. 2002 Feb;4(1):20-24. | ||||
REF 70 | Synthesis and biological evaluation of 2-(4-fluorophenoxy)-2-phenyl-ethyl piperazines as serotonin-selective reuptake inhibitors with a potentially improved adverse reaction profile. Bioorg Med Chem. 2004 Mar 15;12(6):1483-91. | ||||
REF 71 | BCL-2 family antagonists for cancer therapy. Nat Rev Drug Discov. 2008 Dec;7(12):989-1000. | ||||
REF 72 | The contribution of metabolites to the rapid and potent down-regulation of rat cortical beta-adrenoceptors by the putative antidepressant sibutramine hydrochloride. Neuropharmacology. 1989 Feb;28(2):129-34. | ||||
REF 73 | Novel 2-substituted cocaine analogs: uptake and ligand binding studies at dopamine, serotonin and norepinephrine transport sites in the rat brain. J Pharmacol Exp Ther. 1995 Mar;272(3):1176-86. | ||||
REF 74 | Selective serotonin reuptake inhibitors in affective disorders--I. Basic pharmacology. J Psychopharmacol. 1998;12(3 Suppl B):S5-20. | ||||
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