Target Validation Information
Target ID T08910
Target Name Gamma-aminobutyric acid receptor subunit gamma-2
Target Type
Successful
Drug Potency against Target 4-(biphenyl-3-yl)-5-(piperidin-4-yl)isoxazol-3-ol Drug Info IC50 = 78 nM [530818]
Beta-Carboline-3-carboxylic acid t-butyl ester Drug Info Ki = 1000 nM [531188]
6-Nitro-2-(4-nitro-phenyl)-chromen-4-one Drug Info Ki = 17000 nM
MRK016 Drug Info Ki = 0.2 nM [527853]
Ro-4938581 Drug Info Ki = 14 nM [530391]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine Drug Info IC50 = 7000 nM [528408]
3-demethoxy-3-D-mannopyranosylaminothiocolchicine Drug Info IC50 = 11300 nM [528408]
4-Methyl-5-(4-piperidyl)isothiazol-3-ol Drug Info Ki = 2200 nM [528034]
3-butoxy-9H-pyrido[3,4-b]indole Drug Info Ki = 1000 nM [531188]
2-Oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 810 nM [533975]
6-ethyl-3-i-propoxycarbonyl-4-quinolone Drug Info Ki = 214 nM [528134]
6-ethyl-3-(2-methylbutoxycarbonyl)-4-quinolone Drug Info Ki = 28 nM [528134]
5-(piperidin-4-yl)isothiazol-3-ol Drug Info Ki = 1870 nM [528034]
3-butoxycarbonyl-4-quinolone Drug Info Ki = 54 nM [528134]
N-benzyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide Drug Info Ki = 65 nM [528709]
6,6-Dimethyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 360 nM [533975]
2-(4-chlorophenyl)-5-phenyl-4-isoxazolin-3-one Drug Info Ki = 1120 nM [528080]
3,3-Diisopropyl-dihydro-furan-2-one Drug Info IC50 = 220 nM [533975]
2-Thiophen-2-yl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 1.7 nM [534155]
6-bromo-3-ethoxycarbonyl-4-quinolone Drug Info Ki = 16 nM [528134]
3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 10000 nM [531188]
3-Methyl-1-phenyl-1H-chromeno[4,3-c]pyrazol-4-one Drug Info IC50 = 300 nM [533354]
6-Nitro-2-(3-nitro-phenyl)-chromen-4-one Drug Info Ki = 12 nM
RO-145974 Drug Info Ki = 45 nM [534008]
6-ethyl-3-pentoxycarbonyl-4-quinolone Drug Info Ki = 35 nM [528134]
RY-066 Drug Info Ki = 48 nM [534718]
2-(1H-Indol-3-yl)-2-oxo-N-phenethyl-acetamide Drug Info Ki = 380 nM [526738]
(4R)-4-ammoniopentanoate Drug Info IC50 = 2500 nM [533514]
(4S)-4-ammoniopentanoate Drug Info IC50 = 2900 nM [533514]
3-(isopentyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 10000 nM [531188]
3-isobutoxy-9H-pyrido[3,4-b]indole Drug Info Ki = 10000 nM [531188]
3-ethoxy-9H-pyrido[3,4-b]indole Drug Info Ki = 1000 nM [531188]
RO-145975 Drug Info Ki = 53 nM [534008]
RO-147437 Drug Info Ki = 1.3 nM [534008]
ALLOPREGNANOLONE Drug Info IC50 = 74 nM [527511]
1,1-Dimethyl-5-oxa-spiro[2.4]heptan-4-one Drug Info IC50 = 1140 nM [533975]
3-ethoxycarbonyl-4-quinolone Drug Info Ki = 78 nM [528134]
6-bromo-3-ethoxycarbonyl-2-methyl-4-quinolone Drug Info Ki = 4200 nM [528134]
6-ethyl-3-(3-methylbutoxycarbonyl)-4-quinolone Drug Info Ki = 28 nM [528134]
4-Phenyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 220 nM [527382]
N-Indan-1-yl-2-(1H-indol-3-yl)-2-oxo-acetamide Drug Info Ki = 2160 nM [526094]
3-amino-3-demethoxythiocolchicine Drug Info IC50 = 5400 nM [528408]
N-Benzyl-2-(1H-indol-3-yl)-2-oxo-acetamide Drug Info Ki = 346 nM [528709]
N-butyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide Drug Info Ki = 943 nM [528709]
Ro-154513 Drug Info Ki = 15 nM [533912]
3-carboxy-6-ethyl-4-quinolone Drug Info Ki = 208 nM [528134]
6-ethyl-3-(3-pentoxycarbonyl)-4-quinolone Drug Info Ki = 2600 nM [528134]
(beta-CCE)9H-beta-Carboline-3-carboxylic acid Drug Info Ki = 1.2 nM [526738]
CI-218872 Drug Info Ki = 160 nM [533745]
GNF-PF-4421 Drug Info Ki = 20 nM [528134]
1-Methyl-5-oxa-spiro[2.4]heptan-4-one Drug Info IC50 = 3410 nM [533975]
Ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 1000 nM [531188]
Ridine-5-carboxylic acid ethyl ester Drug Info IC50 = 79 nM [533164]
3-Isopropyl-3-methyl-dihydro-furan-2-one Drug Info IC50 = 740 nM [533975]
3-butylaminocarbonyl-6-ethyl-4-quinolone Drug Info Ki = 0.54 nM [528134]
6-ethyl-3-propoxycarbonyl-4-quinolone Drug Info Ki = 1.8 nM [528134]
3-cyclopentoxycarbonyl-6-ethyl-4-quinolone Drug Info Ki = 19 nM [528134]
5-(4-piperidyl)-4-propylisothiazol-3-ol Drug Info Ki = 440 nM [528034]
3-tert-Butyl-3-ethyl-dihydro-furan-2-one Drug Info IC50 = 310 nM [533975]
5-[(1R)-1-ammonioethyl]isoxazol-3-olate Drug Info IC50 = 9500 nM [533514]
6-benzyl-3-propoxycarbonyl-4-quinolone Drug Info Ki = 0.17 nM [528134]
4-Naphthalen-1-yl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 820 nM [527382]
3,3-Diethyl-dihydro-furan-2-one Drug Info IC50 = 750 nM [533975]
GNF-PF-3645 Drug Info Ki = 15 nM [528134]
6,9-Dimethyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 780 nM [533975]
3-(benzyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 10000 nM [531188]
3-butoxycarbonyl-6-ethyl-4-quinolone Drug Info Ki = 13 nM [528134]
3-Methyl-2-phenyl-2H-chromeno[4,3-c]pyrazol-4-one Drug Info IC50 = 3100 nM [533354]
1-(4-chlorophenyl)-4-phenyl-1H-imidazole Drug Info Ki = 3290 nM [528080]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine Drug Info IC50 = 9700 nM [528408]
1,3-Diphenyl-1H-chromeno[4,3-c]pyrazol-4-one Drug Info IC50 = 16000 nM [533354]
4-benzyl-5-(4-piperidyl)isothiazol-3-ol Drug Info Ki = 331 nM [528034]
RO-194603 Drug Info Ki = 0.2 nM [534008]
3-Ethoxy-9H-beta-carboline Drug Info Ki = 25.1 nM [534660]
CGS-9896 Drug Info Ki = 2.4 nM [528080]
CGS-13767 Drug Info IC50 = 4 nM [529466]
Ro-4938581 Drug Info Ki = 80 nM [530391]
U-78875 Drug Info Ki = 1.6 nM [534209]
3-Isothiocyanato-9H-beta-carboline Drug Info IC50 = 4 nM [531518]
U-89267 Drug Info Ki = 0.65 nM [533912]
ZK-93423 Drug Info IC50 = 1 nM [530319]
3-Methyl-9H-beta-carboline Drug Info Ki = 1.1 nM [533745]
3-demethoxy-3-L-fucopyranosylaminothiocolchicine Drug Info IC50 = 10500 nM [528408]
THIOCOLCHICOSIDE Drug Info IC50 = 3400 nM [528408]
3-demethoxy-3D-glucopyranosylaminothiocolchicine Drug Info IC50 = 18000 nM [528408]
5-(piperidin-4-yl)isoxazol-3-ol Drug Info Ki = 9100 nM [527382]
Ro-151310 Drug Info Ki = 5.4 nM [534008]
ELTANOLONE Drug Info IC50 = 71 nM [527511]
5-[(1S)-1-ammonioethyl]isoxazol-3-olate Drug Info IC50 = 5800 nM [533514]
GAMMA-AMINO-BUTANOIC ACID Drug Info IC50 = 24 nM [528408]
6-Methyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 680 nM [533975]
4-Benzyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 3800 nM [527382]
6-ethyl-3-propylaminocarbonyl-4-quinolone Drug Info Ki = 0.26 nM [528134]
3-Ethyl-3-methyl-dihydro-furan-2-one Drug Info IC50 = 2280 nM [533975]
3-Ethyl-3-isopropyl-dihydro-furan-2-one Drug Info IC50 = 240 nM [533975]
4-(4-chlorophenyl)-1-pyrid-2-yl-pyrazole Drug Info Ki = 4480 nM [528080]
6-benzyl-3-ethoxycarbonyl-4-quinolone Drug Info Ki = 1.4 nM [528134]
2-Isoxazol-5-yl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 1 nM [534155]
AMENTOFLAVONE Drug Info IC50 = 14.9 nM [526653]
(2E,4S)-4-ammoniopent-2-enoate Drug Info IC50 = 2600 nM [533514]
Sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 216 nM [531188]
3-ethoxycarbonyl-6-propyl-4-quinolone Drug Info Ki = 17 nM [528134]
3-propoxy-9H-pyrido[3,4-b]indole Drug Info Ki = 1000 nM [531188]
Ethyl 9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 2700 nM [531188]
3-ethoxycarbonyl-6-ethyl-2-methyl-4-quinolone Drug Info Ki = 6580 nM [528134]
6-ethyl-3-(2-ethylbutoxycarbonyl)-4-quinolone Drug Info Ki = 92 nM [528134]
N-butyl-2-(1H-indol-3-yl)-2-oxoacetamide Drug Info Ki = 1175 nM [528709]
N-(p-methylbenzyl)-5-nitroindol-3-ylglyoxylamide Drug Info Ki = 31.3 nM [528709]
CGS-9895 Drug Info IC50 = 100 nM [533348]
4-(2-aminoethyl)-1,2,5-oxadiazol-3-ol Drug Info Ki = 13000 nM [528295]
4-Naphthalen-2-yl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 36 nM [527382]
CGS-17867A Drug Info Ki = 0.77 nM [527100]
L-655708 Drug Info Ki = 0.4 nM [527005]
References
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Ref 528408J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
Ref 528408J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
Ref 528034J Med Chem. 2006 Feb 23;49(4):1388-96.Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.
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Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
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Ref 528709J Med Chem. 2007 Apr 5;50(7):1627-34. Epub 2007 Mar 3.Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 528080J Med Chem. 2006 Mar 23;49(6):1855-66.Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 534155J Med Chem. 1996 Jul 5;39(14):2844-51.Synthesis and structure--activity relationships of fused imidazopyridines: a new series of benzodiazepine receptor ligands.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
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Ref 533354J Med Chem. 1988 Jan;31(1):1-3.Synthesis, binding studies, and structure-activity relationships of 1-aryl-and 2-aryl[1]benzopyranopyrazol-4-ones, central benzodiazepine receptor ligands.
Ref 534008J Med Chem. 1993 Apr 16;36(8):1001-6.Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepine receptors.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 534718J Med Chem. 1998 Oct 8;41(21):4130-42.Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparative molecular field analysis.
Ref 526738J Med Chem. 1992 Jun 12;35(12):2214-20.Benzodiazepine receptor affinity and interaction of some N-(indol-3-ylglyoxylyl)amine derivatives.
Ref 533514J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects.
Ref 533514J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects.
Ref 531188Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted |A-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
Ref 531188Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted |A-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
Ref 531188Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted |A-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
Ref 534008J Med Chem. 1993 Apr 16;36(8):1001-6.Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepine receptors.
Ref 534008J Med Chem. 1993 Apr 16;36(8):1001-6.Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepine receptors.
Ref 527511J Med Chem. 2005 Apr 21;48(8):3051-9.Neurosteroid analogues. 10. The effect of methyl group substitution at the C-6 and C-7 positions on the GABA modulatory and anesthetic actions of (3alpha,5alpha)-and (3alpha,5beta)-3-hydroxypregnan-20-one.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 527382J Med Chem. 2005 Jan 27;48(2):427-39.Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
Ref 526094J Med Chem. 2001 Jul 5;44(14):2286-97.Novel N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular modeling analysis of the structure-activity relationships.
Ref 528408J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
Ref 528709J Med Chem. 2007 Apr 5;50(7):1627-34. Epub 2007 Mar 3.Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands.
Ref 528709J Med Chem. 2007 Apr 5;50(7):1627-34. Epub 2007 Mar 3.Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands.
Ref 533912J Med Chem. 1994 Mar 18;37(6):758-68.Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 526738J Med Chem. 1992 Jun 12;35(12):2214-20.Benzodiazepine receptor affinity and interaction of some N-(indol-3-ylglyoxylyl)amine derivatives.
Ref 533745J Med Chem. 1994 Dec 23;37(26):4576-80.Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 531188Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted |A-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
Ref 533164J Med Chem. 1989 Dec;32(12):2561-73.Synthesis and structure-activity relationships of a series of anxioselective pyrazolopyridine ester and amide anxiolytic agents.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 528034J Med Chem. 2006 Feb 23;49(4):1388-96.Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 533514J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 527382J Med Chem. 2005 Jan 27;48(2):427-39.Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 531188Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted |A-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 533354J Med Chem. 1988 Jan;31(1):1-3.Synthesis, binding studies, and structure-activity relationships of 1-aryl-and 2-aryl[1]benzopyranopyrazol-4-ones, central benzodiazepine receptor ligands.
Ref 528080J Med Chem. 2006 Mar 23;49(6):1855-66.Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors.
Ref 528408J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
Ref 533354J Med Chem. 1988 Jan;31(1):1-3.Synthesis, binding studies, and structure-activity relationships of 1-aryl-and 2-aryl[1]benzopyranopyrazol-4-ones, central benzodiazepine receptor ligands.
Ref 528034J Med Chem. 2006 Feb 23;49(4):1388-96.Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.
Ref 534008J Med Chem. 1993 Apr 16;36(8):1001-6.Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepine receptors.
Ref 534660J Med Chem. 1998 Jul 2;41(14):2537-52.Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) at wild type and recombinant GABAA receptors.
Ref 528080J Med Chem. 2006 Mar 23;49(6):1855-66.Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors.
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