Target General Infomation
Target ID
T64382
Former ID
TTDS00018
Target Name
Gamma-aminobutyric acid receptor
Synonyms
GABA receptor
Target Type
Successful
Disease Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Ascariasis; Enterobiasis [ICD9: 127.0, 127.4; ICD10: B77, B80]
Alcohol use disorders [ICD9: 303; ICD10: F10.2]
Bipolar disorder [ICD9: 296.0, 296.1, 296.4, 296.5, 296.6, 296.7, 296.8, 300; ICD10: F31, F40-F42]
Epilepsy [ICD10: G40]
Epileptic seizures [ICD9: 345.9, 780.3; ICD10: G40, P90, R56]
Inflammation [ICD10: E08-E13, E10.2, E11, E11.2, E13.2, I73.9, I80-I82, N00-N29, G89]
Irritable bowel syndrome [ICD9: 564.1, 787.91; ICD10: A09, K58, K59.1]
Muscle spasm [ICD10: M62.838]
Obesity [ICD9: 278; ICD10: E66]
Premenstrual syndrome [ICD10: N94.3]
Schizophrenia [ICD9: 295; ICD10: F20]
Seizures [ICD9: 345.9, 780.3; ICD10: G40, P90, R56]
Urea cycle disorders [ICD9: 270.6; ICD10: E72.2]
BioChemical Class
Chloride channel
Target Validation
T64382
Drugs and Mode of Action
Drug(s) ALPIDEM Drug Info Approved Anxiety disorder [551871]
Clonazepam Drug Info Approved Epilepsy [538277], [541998]
DP-VPA Drug Info Approved Bipolar disorder [546558]
Phenobarbital Drug Info Approved Seizures [539845], [550627]
Piperazine Drug Info Approved Ascariasis; Enterobiasis [538341], [551871]
THIOCOLCHICOSIDE Drug Info Approved Muscle spasm [551871]
ANDROSTERONE Drug Info Phase 3 Discovery agent [524778]
Phentermine+topiramate Drug Info Phase 3 Obesity [536869]
ZK-93423 Drug Info Phase 3 Epileptic seizures [467683], [533661]
ALLOPREGNANOLONE Drug Info Phase 2 Discovery agent [467451], [524035]
BL-1020 Drug Info Phase 2 Schizophrenia [536463]
BNC-210 Drug Info Phase 2 Anxiety disorder [548927]
Clonazepam Drug Info Phase 2 Seizures [529439], [534170], [541998]
Dextofisopam Drug Info Phase 2 Irritable bowel syndrome [536224]
Phenylbutyrate Drug Info Phase 2 Urea cycle disorders [536447], [543164]
PIKAMILONE Drug Info Phase 2 Anxiety disorder [522726]
Muscimol Drug Info Phase 1 Discovery agent [467594], [522693]
ELTANOLONE Drug Info Discontinued in Phase 3 Premenstrual syndrome [546011]
Dezinamide Drug Info Discontinued in Phase 2 Epileptic seizures [544536]
Gedocarnil Drug Info Discontinued in Phase 1 Anxiety disorder [545942]
U-78875 Drug Info Discontinued in Phase 1 Anxiety disorder [544810]
C-202 Drug Info Terminated Epilepsy [548090]
CGS-17867A Drug Info Terminated Alcohol use disorders [544711]
CGS-9896 Drug Info Terminated Discovery agent [544687]
Divaplon Drug Info Terminated Discovery agent [544692]
U-90042 Drug Info Terminated Anxiety disorder [544907]
XR-368 Drug Info Terminated Anxiety disorder [545635]
Inhibitor ((E)-3-Amino-propenyl)-methyl-phosphinic acid Drug Info [529517]
(2-Amino-4,5-dihydro-thiazol-4-yl)-acetic acid Drug Info [551228]
(2E,4S)-4-ammoniopent-2-enoate Drug Info [533514]
(4R)-4-ammoniopentanoate Drug Info [533514]
(4S)-4-ammoniopentanoate Drug Info [533514]
(6-Benzylamino-9H-beta-carbolin-3-yl)-methanol Drug Info [533414]
(9-Benzyl-9H-purin-6-yl)-cyclopropyl-amine Drug Info [533033]
(9H-beta-Carbolin-3-yl)-carbamic acid ethyl ester Drug Info [533400]
(9H-beta-Carbolin-3-yl)-ethyl-amine Drug Info [533400]
(9H-beta-Carbolin-3-yl)-methanol Drug Info [533414]
(beta-CCE)9H-beta-Carboline-3-carboxylic acid Drug Info [526738]
(R)-4-amino-2-methylbutanoic acid Drug Info [529135]
1,1-Dimethyl-5-oxa-spiro[2.4]heptan-4-one Drug Info [533975]
1,3-Diphenyl-1H-chromeno[4,3-c]pyrazol-4-one Drug Info [533354]
1-(4-chlorophenyl)-4-phenyl-1H-imidazole Drug Info [528080]
1-(9H-beta-Carbolin-3-yl)-butan-1-one Drug Info [526755]
1-(9H-beta-Carbolin-3-yl)-ethanone Drug Info [533414]
1-Methyl-5-oxa-spiro[2.4]heptan-4-one Drug Info [533975]
2,4-Diamino-butyric acid(GABA) Drug Info [533404]
2,6-Diisopropyl-4-nitro-phenol Drug Info [534629]
2-(1H-Indol-3-yl)-2-oxo-N-phenethyl-acetamide Drug Info [526738]
2-(2-Amino-phenyl)-6-methyl-chromen-4-one Drug Info [526416]
2-(2-Hydroxy-phenyl)-6-methyl-chromen-4-one Drug Info [526416]
2-(2-Methoxy-phenyl)-6-methyl-chromen-4-one Drug Info [526416]
2-(3-Amino-phenyl)-6-methyl-chromen-4-one Drug Info [526416]
2-(3-Bromo-phenyl)-6-methyl-chromen-4-one Drug Info [526416]
2-(3-Bromo-phenyl)-6-nitro-chromen-4-one Drug Info [551323]
2-(3-Bromo-phenyl)-chromen-4-one Drug Info [551323]
2-(3-Butoxy-phenyl)-6-methyl-chromen-4-one Drug Info [526416]
2-(3-Chloro-phenyl)-chromen-4-one Drug Info [551323]
2-(3-Hydroxy-phenyl)-6-methyl-chromen-4-one Drug Info [526416]
2-(3-Methoxy-phenyl)-6-methyl-chromen-4-one Drug Info [526416]
2-(4-Amino-phenyl)-6-methyl-chromen-4-one Drug Info [526416]
2-(4-Chloro-phenyl)-3H-imidazo[4,5-c]quinoline Drug Info [534155]
2-(4-chlorophenyl)-5-phenyl-4-isoxazolin-3-one Drug Info [528080]
2-(9-Benzyl-9H-purin-6-ylamino)-ethanol Drug Info [533033]
2-Furan-2-yl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info [534157]
2-Isoxazol-3-yl-3H-imidazo[4,5-c]quinoline Drug Info [534155]
2-Isoxazol-5-yl-3H-imidazo[4,5-c]quinoline Drug Info [534155]
2-Oxa-spiro[4.4]nonan-1-one Drug Info [533975]
2-p-Tolyl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info [534157]
2-Phenyl-3H-imidazo[4,5-c]quinoline Drug Info [534155]
2-Phenyl-5,6-dihydro-pyrazolo[1,5-c]quinazoline Drug Info [534157]
2-Phenyl-6-propyl-chromen-4-one Drug Info [526416]
2-Phenyl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info [534157]
2-Pyridin-2-yl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info [534157]
2-Thiophen-2-yl-3H-imidazo[4,5-c]quinoline Drug Info [534155]
3,3-Diethyl-dihydro-furan-2-one Drug Info [533975]
3,3-Diisopropyl-dihydro-furan-2-one Drug Info [533975]
3,3-Dimethyl-dihydro-furan-2-one Drug Info [533975]
3-(2,2-Dimethyl-propoxy)-9H-beta-carboline Drug Info [526755]
3-(3-Methyl-butoxy)-9H-beta-carboline Drug Info [526755]
3-(benzyloxy)-9H-pyrido[3,4-b]indole Drug Info [531188]
3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole Drug Info [531188]
3-(isopentyloxy)-9H-pyrido[3,4-b]indole Drug Info [531188]
3-amino-3-demethoxythiocolchicine Drug Info [528408]
3-Amino-propane-1-sulfonic acid Drug Info [551302]
3-ammoniopropane-1-sulfinate Drug Info [551302]
3-Butoxy-9H-beta-carboline Drug Info [526755]
3-butoxy-9H-pyrido[3,4-b]indole Drug Info [531188]
3-butoxycarbonyl-4-quinolone Drug Info [528134]
3-butoxycarbonyl-6-ethyl-4-quinolone Drug Info [528134]
3-butylaminocarbonyl-6-ethyl-4-quinolone Drug Info [528134]
3-carboxy-6-ethyl-4-quinolone Drug Info [528134]
3-Chloro-9H-beta-carboline Drug Info [533363]
3-cyclopentoxycarbonyl-6-ethyl-4-quinolone Drug Info [528134]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine Drug Info [528408]
3-demethoxy-3-D-mannopyranosylaminothiocolchicine Drug Info [528408]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine Drug Info [528408]
3-demethoxy-3-L-fucopyranosylaminothiocolchicine Drug Info [528408]
3-demethoxy-3D-glucopyranosylaminothiocolchicine Drug Info [528408]
3-Ethoxy-9H-beta-carboline Drug Info [534660]
3-ethoxy-9H-pyrido[3,4-b]indole Drug Info [531188]
3-ethoxycarbonyl-4-quinolone Drug Info [528134]
3-ethoxycarbonyl-6-ethyl-2-methyl-4-quinolone Drug Info [528134]
3-ethoxycarbonyl-6-propyl-4-quinolone Drug Info [528134]
3-Ethyl-3-isopropyl-dihydro-furan-2-one Drug Info [533975]
3-Ethyl-3-methyl-dihydro-furan-2-one Drug Info [533975]
3-Hydroxy-piperidine-4-carboxylic acid Drug Info [533544]
3-Isobutoxy-9H-beta-carboline Drug Info [526755]
3-isobutoxy-9H-pyrido[3,4-b]indole Drug Info [531188]
3-Isopropoxy-9H-beta-carboline Drug Info [526755]
3-Isopropyl-3-methyl-dihydro-furan-2-one Drug Info [533975]
3-Isothiocyanato-9H-beta-carboline Drug Info [531518]
3-Methoxy-9H-beta-carboline Drug Info [533363]
3-Methoxycarbonyl-2-methyl-9H-beta-carbolin-2-ium Drug Info [551248]
3-Methyl-1-phenyl-1H-chromeno[4,3-c]pyrazol-4-one Drug Info [533354]
3-Methyl-2-phenyl-2H-chromeno[4,3-c]pyrazol-4-one Drug Info [533354]
3-Methyl-9H-beta-carboline Drug Info [533745]
3-Nitro-9H-beta-carboline Drug Info [533363]
3-Propoxy-9H-beta-carboline Drug Info [533363]
3-propoxy-9H-pyrido[3,4-b]indole Drug Info [531188]
3-sec-Butoxy-9H-beta-carboline Drug Info [526755]
3-tert-Butyl-3-ethyl-dihydro-furan-2-one Drug Info [533975]
4-(2-aminoethyl)-1,2,5-oxadiazol-3-ol Drug Info [528295]
4-(4-chlorophenyl)-1-pyrid-2-yl-pyrazole Drug Info [528080]
4-(5-tert-Butyl-[1,3]dithian-2-yl)-benzonitrile Drug Info [533668]
4-Amino-3-hydroxy-butyric acid Drug Info [533403]
4-benzyl-5-(4-piperidyl)isothiazol-3-ol Drug Info [528034]
4-Benzyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info [527382]
4-Bromo-2,6-diisopropyl-phenol Drug Info [534629]
4-Chloro-2,6-diisopropyl-phenol Drug Info [534629]
4-Dimethylamino-2,6-diisopropyl-phenol Drug Info [534629]
4-Ethyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info [525949]
4-Hydroxy-3,5-diisopropyl-benzaldehyde Drug Info [534629]
4-Iodo-2,6-diisopropyl-phenol Drug Info [534629]
4-Methoxymethyl-3,6-dipropoxy-9H-beta-carboline Drug Info [534660]
4-Methyl-5-(4-piperidyl)isothiazol-3-ol Drug Info [528034]
4-Methyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info [525949]
4-Naphthalen-1-yl-5-piperidin-4-yl-isoxazol-3-ol Drug Info [527382]
4-Naphthalen-2-yl-5-piperidin-4-yl-isoxazol-3-ol Drug Info [527382]
4-Phenyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info [528744]
5-(4-piperidyl)-4-propylisothiazol-3-ol Drug Info [528034]
5-(piperidin-4-yl)isothiazol-3-ol Drug Info [528034]
5-(piperidin-4-yl)isoxazol-3-ol Drug Info [528744]
5-Aminomethyl-4,5-dihydro-isoxazol-3-ol Drug Info [533403]
5-tert-Butyl-2-(4-ethynyl-phenyl)-[1,3]dithiane Drug Info [533668]
5-tert-Butyl-2-(4-fluoro-phenyl)-[1,3]dithiane Drug Info [533668]
5-[(1R)-1-ammonioethyl]isoxazol-3-olate Drug Info [533514]
5-[(1S)-1-ammonioethyl]isoxazol-3-olate Drug Info [533514]
6,6-Dimethyl-2-oxa-spiro[4.4]nonan-1-one Drug Info [533975]
6,9-Dimethyl-2-oxa-spiro[4.4]nonan-1-one Drug Info [533975]
6-benzyl-3-ethoxycarbonyl-4-quinolone Drug Info [528134]
6-benzyl-3-propoxycarbonyl-4-quinolone Drug Info [528134]
6-benzyl-3-propylaminocarbonyl-4-quinolone Drug Info [528134]
6-Bromo-2-(2-nitro-phenyl)-chromen-4-one Drug Info [551336]
6-Bromo-2-(3-bromo-phenyl)-chromen-4-one Drug Info [551323]
6-Bromo-2-(3-nitro-phenyl)-chromen-4-one Drug Info [551336]
6-Bromo-2-(4-nitro-phenyl)-chromen-4-one Drug Info [551336]
6-Bromo-2-phenyl-chromen-4-one Drug Info [551323]
6-bromo-3-ethoxycarbonyl-2-methyl-4-quinolone Drug Info [528134]
6-bromo-3-ethoxycarbonyl-4-quinolone Drug Info [528134]
6-Chloro-2-(3-nitro-phenyl)-chromen-4-one Drug Info [551323]
6-Chloro-2-phenyl-chromen-4-one Drug Info [551323]
6-Ethyl-2-phenyl-chromen-4-one Drug Info [526416]
6-ethyl-3-(2-ethylbutoxycarbonyl)-4-quinolone Drug Info [528134]
6-ethyl-3-(2-methylbutoxycarbonyl)-4-quinolone Drug Info [528134]
6-ethyl-3-(3-methylbutoxycarbonyl)-4-quinolone Drug Info [528134]
6-ethyl-3-(3-pentoxycarbonyl)-4-quinolone Drug Info [528134]
6-ethyl-3-i-propoxycarbonyl-4-quinolone Drug Info [528134]
6-ethyl-3-pentoxycarbonyl-4-quinolone Drug Info [528134]
6-ethyl-3-propoxycarbonyl-4-quinolone Drug Info [528134]
6-ethyl-3-propylaminocarbonyl-4-quinolone Drug Info [528134]
6-Fluoro-2-(3-nitro-phenyl)-chromen-4-one Drug Info [551323]
6-Isopropyl-2-phenyl-chromen-4-one Drug Info [526416]
6-Methyl-2-oxa-spiro[4.4]nonan-1-one Drug Info [533975]
6-Methyl-2-p-tolyl-chromen-4-one Drug Info [526416]
6-Methyl-2-phenyl-chromen-4-one Drug Info [526416]
6-Methyl-2-pyridin-3-yl-chromen-4-one Drug Info [526416]
6-Nitro-2-(3-nitro-phenyl)-chromen-4-one Drug Info [551290]
6-Nitro-2-(4-nitro-phenyl)-chromen-4-one Drug Info [551290]
6-Nitro-2-phenyl-chromen-4-one Drug Info [551323]
7,12-Dihydro-5,7,12-triaza-indeno[1,2-a]fluorene Drug Info [533412]
7,12-Dihydro-7,12-diaza-indeno[1,2-a]fluorene Drug Info [533363]
7-Diazonium-naphthalene-1-sulfonic acid anion Drug Info [533352]
8-Diazonium-naphthalene-1-sulfonic acid anion Drug Info [533352]
9H-beta-Carbolin-3-ol Drug Info [533363]
9H-beta-Carbolin-6-ylamine Drug Info [533414]
9H-beta-Carboline-3-carboxylic acid butyl ester Drug Info [533546]
9H-beta-Carboline-3-carboxylic acid ethyl ester Drug Info [533546]
9H-beta-Carboline-3-carboxylic acid propyl ester Drug Info [533546]
Acetic acid 2,6-diisopropyl-phenyl ester Drug Info [534629]
AFLATREME Drug Info [551293]
ALFAXALONE Drug Info [534629]
ALLOPREGNANOLONE Drug Info [528321]
ALPIDEM Drug Info [534470]
AMENTOFLAVONE Drug Info [526653]
ANDROSTERONE Drug Info [528321]
Benzoic acid 2,6-diisopropyl-phenyl ester Drug Info [534629]
Benzyl-(9H-beta-carbolin-6-yl)-amine Drug Info [533363]
Beta-Carboline-3-carboxylic acid t-butyl ester Drug Info [531188]
BETA-CCM Drug Info [533763]
BRL-54504AX Drug Info [551288]
CGP-27492 Drug Info [533678]
CGS-13767 Drug Info [529466]
CGS-17867A Drug Info [527100]
CGS-8216 Drug Info [529466]
CGS-9895 Drug Info [533348]
CGS-9896 Drug Info [528080]
CI-218872 Drug Info [531188]
Divaplon Drug Info [533379]
ELTANOLONE Drug Info [528321]
Ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate Drug Info [531188]
Ethyl 9H-pyrido[3,4-b]indole-3-carboxylate Drug Info [531188]
ETIOCHOLANOLONE Drug Info [528321]
GABAZINE Drug Info [528034]
GAMMA-AMINO-BUTANOIC ACID Drug Info [528408]
GNF-PF-3645 Drug Info [528134]
GNF-PF-4421 Drug Info [528134]
Isoquinoline-3-carboxylic acid methyl ester Drug Info [533363]
L-655708 Drug Info [527005]
N-(9H-beta-Carbolin-3-yl)-acetamide Drug Info [533400]
N-(9H-beta-Carbolin-3-yl)-formamide Drug Info [533400]
N-Benzyl-2-(1H-indol-3-yl)-2-oxo-acetamide Drug Info [534710]
N-butyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide Drug Info [528709]
N-Indan-1-yl-2-(1H-indol-3-yl)-2-oxo-acetamide Drug Info [526094]
NIPECOTIC ACID Drug Info [533396]
NORHARMANE Drug Info [533363]
NSC-19028 Drug Info [526416]
NSC-73613 Drug Info [551323]
NSC-93394 Drug Info [551323]
Piperidine-4-carboxylic acid Drug Info [533544]
PITRAZEPINE Drug Info [526735]
Pyrrolidin-3-yl-acetic acid Drug Info [533396]
Ridine-5-carboxylic acid ethyl ester Drug Info [533164]
RIPAZEPAM Drug Info [533397]
RO-054520 Drug Info [533368]
RO-145974 Drug Info [534008]
RO-145975 Drug Info [534008]
RO-147437 Drug Info [534008]
Ro-151310 Drug Info [531044]
Ro-154513 Drug Info [534122]
RO-194603 Drug Info [534008]
Ro-4938581 Drug Info [530391]
RWJ-16979 Drug Info [533762]
RY-066 Drug Info [534718]
Sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate Drug Info [531188]
THIOCOLCHICOSIDE Drug Info [528408]
Toluene-1-diazonium-3-sulfonic acid anion Drug Info [533352]
U-78875 Drug Info [525465]
U-89267 Drug Info [533912]
WEDELOLACTONE Drug Info [525981]
ZK-93423 Drug Info [530319]
Antagonist Bicuculline Drug Info [534920]
Phenobarbital Drug Info [536555], [537706]
Piperazine Drug Info [535818]
SR95531 Drug Info [534920]
Agonist BL-1020 Drug Info [536463]
Clonazepam Drug Info [535248], [536166]
Dextofisopam Drug Info [536224]
Muscimol Drug Info [537788]
Phenylbutyrate Drug Info [536447]
Modulator BNC-210 Drug Info [525395]
C-202 Drug Info [551657]
Dezinamide Drug Info [534194]
DP-VPA Drug Info [526386]
Gedocarnil Drug Info [551901]
Phentermine+topiramate Drug Info [536710]
PIKAMILONE Drug Info [551871]
U-90042 Drug Info [533584]
XR-368 Drug Info [534442]
References
Ref 467451(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4108).
Ref 467594(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4259).
Ref 467683(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4346).
Ref 522693ClinicalTrials.gov (NCT00921128) Convection-Enhanced Delivery to Study the Pathophysiology Underlying the Clinical Features of Parkinson s Disease. U.S. National Institutes of Health.
Ref 522726ClinicalTrials.gov (NCT00940186) Clinical Pharmacokinetics Study on Pikamilone. U.S. National Institutes of Health.
Ref 524035ClinicalTrials.gov (NCT01673828) Allopregnanolone for the Treatment of Traumatic Brain Injury. U.S. National Institutes of Health.
Ref 524778ClinicalTrials.gov (NCT02151006) Does Dehydro Epiandrosterone (DHEA) Improve Pregnancy Rate in Women Undergoing IVF/ICSI With Expected Poor Ovarian Response?. U.S. National Institutes of Health.
Ref 529439Residual effect of a 7-amino metabolite of clonazepam on GABAA receptor function in the nucleus reticularis thalami of the rat. Epilepsia. 2008 Oct;49(10):1803-8.
Ref 533661Abecarnil enhances GABA-induced currents in acutely isolated cerebellar Purkinje cells. Neuropharmacology. 1995 Feb;34(2):157-63.
Ref 534170Characterization of GABAA receptor function in human temporal cortical neurons. J Neurophysiol. 1996 Apr;75(4):1458-71.
Ref 536224Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
Ref 536447Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52.
Ref 536463The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
Ref 536869Adjunctive topiramate enhances the risk of hypothermia associated with valproic acid therapy. J Clin Pharm Ther. 2008 Oct;33(5):513-9.
Ref 538277FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074569.
Ref 538341FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 080671.
Ref 539845(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2804).
Ref 541998(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6963).
Ref 543164(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8480).
Ref 544536Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000082)
Ref 544687Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000585)
Ref 544692Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000631)
Ref 544711Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000696)
Ref 544810Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001194)
Ref 544907Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001470)
Ref 545635Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004007)
Ref 545942Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005436)
Ref 546011Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005875)
Ref 546558Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008928)
Ref 548090Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021837)
Ref 548927Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030421)
Ref 550627Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 52539550 years of hurdles and hope in anxiolytic drug discovery. Nat Rev Drug Discov. 2013 Sep;12(9):667-87. doi: 10.1038/nrd4075.
Ref 525465J Med Chem. 1999 Apr 8;42(7):1123-44.Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality.
Ref 525949J Med Chem. 2000 Dec 28;43(26):4930-3.A novel class of potent 3-isoxazolol GABA(A) antagonists: design, synthesis, and pharmacology.
Ref 525981Bioorg Med Chem Lett. 2001 Feb 12;11(3):283-6.Synthesis and preliminary pharmacological evaluation of coumestans with different patterns of oxygenation.
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 526386DP-VPA D-Pharm. Curr Opin Investig Drugs. 2002 Jun;3(6):921-3.
Ref 526416J Med Chem. 2002 Sep 12;45(19):4188-201.Refinement and evaluation of a pharmacophore model for flavone derivatives binding to the benzodiazepine site of the GABA(A) receptor.
Ref 526653Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors.
Ref 526735J Med Chem. 1992 May 29;35(11):1969-77.Structure and molecular modeling of GABAA receptor antagonists.
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 526755J Med Chem. 1992 Oct 30;35(22):4001-10.Predictive binding of beta-carboline inverse agonists and antagonists via the CoMFA/GOLPE approach.
Ref 527005J Med Chem. 2004 Mar 25;47(7):1807-22.3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.
Ref 527100Bioorg Med Chem Lett. 2004 Jul 5;14(13):3441-4.2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor.
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 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 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 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 528295J Med Chem. 2006 Jul 13;49(14):4442-6.Hydroxy-1,2,5-oxadiazolyl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and pharmacological characterization of gamma-aminobutyric acid (GABA) related compounds.
Ref 528321J Med Chem. 2006 Jul 27;49(15):4595-605.Neurosteroid analogues. 11. Alternative ring system scaffolds: gamma-aminobutyric acid receptor modulation and anesthetic actions of benz[f]indenes.
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 528744J Med Chem. 2007 Apr 19;50(8):1988-92. Epub 2007 Mar 22.4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships.
Ref 529135Bioorg Med Chem Lett. 2008 Jan 1;18(1):402-4. Epub 2007 Oct 17.Enantioselective actions of 4-amino-3-hydroxybutanoic acid and (3-amino-2-hydroxypropyl)methylphosphinic acid at recombinant GABA(C) receptors.
Ref 529466J Med Chem. 1991 Jan;34(1):281-90.Synthesis and benzodiazepine binding activity of a series of novel [1,2,4]triazolo[1,5-c]quinazolin-5(6H)-ones.
Ref 529517J Med Chem. 2008 Jul 10;51(13):3825-40. Epub 2008 Jun 5.Novel gamma-aminobutyric acid rho1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships.
Ref 530319J Med Chem. 1990 Mar;33(3):1062-9.Structural requirements for agonist actions at the benzodiazepine receptor: studies with analogues of 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester.
Ref 530391Bioorg Med Chem Lett. 2009 Oct 15;19(20):5940-4. Epub 2009 Aug 15.The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction.
Ref 531044Bioorg Med Chem. 2010 Nov 15;18(22):7731-8. Epub 2010 Jun 1.The GABA(A) receptor as a target for photochromic molecules.
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 531518J Med Chem. 1990 Sep;33(9):2343-57.Synthetic and computer-assisted analyses of the pharmacophore for the benzodiazepine receptor inverse agonist site.
Ref 533033J Med Chem. 1989 May;32(5):1020-4.Benzodiazepine receptor binding activity of 6,9-disubstituted purines.
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 533348J Med Chem. 1987 Oct;30(10):1737-42.1,3-Diarylpyrazolo[4,5-c]- and -[5,4-c]quinolin-4-ones. 4. Synthesis and specific inhibition of benzodiazepine receptor binding.
Ref 533352J Med Chem. 1987 Dec;30(12):2222-7.Aryl diazo compounds and diazonium salts as potential irreversible probes of the gamma-aminobutyric acid receptor.
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 533363J Med Chem. 1988 Sep;31(9):1854-61.Synthesis of novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore.
Ref 533368J Med Chem. 1988 Dec;31(12):2235-46.Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.
Ref 533379J Med Chem. 1988 Jun;31(6):1220-6.(Imidazo[1,2-a]pyrimidin-2-yl)phenylmethanones and related compounds as potential nonsedative anxiolytics.
Ref 533396J Med Chem. 1985 May;28(5):653-60.Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
Ref 533397J Med Chem. 1985 May;28(5):683-5.Synthesis and interaction of 5-(substituted-phenyl)-3-methyl-6,7-dihydropyrazolo[4,3-e] [1,4]diazepin-8(7H)-ones with benzodiazepine receptors in rat cerebral cortex.
Ref 533400J Med Chem. 1985 Jun;28(6):824-8.3-Amino-beta-carboline derivatives and the benzodiazepine receptor. Synthesis of a selective antagonist of the sedative action of diazepam.
Ref 533403J Med Chem. 1985 Nov;28(11):1612-7.GABA agonists. Resolution, absolute stereochemistry, and enantioselectivity of (S)-(+)- and (R)-(-)-dihydromuscimol.
Ref 533404J Med Chem. 1986 Feb;29(2):224-9.Glycine antagonists. Synthesis, structure, and biological effects of some bicyclic 5-isoxazolol zwitterions.
Ref 533412J Med Chem. 1987 Mar;30(3):456-8.Synthesis of 7,12-dihydropyrido[3,4-b:5,4-b']diindoles. A novel class of rigid, planar benzodiazepine receptor ligands.
Ref 533414J Med Chem. 1987 Apr;30(4):750-3.Synthesis of 6-substituted beta-carbolines that behave as benzodiazepine receptor antagonists or inverse agonists.
Ref 533514J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects.
Ref 533544J Med Chem. 1982 Oct;25(10):1157-62.Hydroxy- and amino-substituted piperidinecarboxylic acids as gamma-aminobutyric acid agonists and uptake inhibitors.
Ref 533546J Med Chem. 1983 Apr;26(4):499-503.beta-Carbolines as benzodiazepine receptor ligands. 1. Synthesis and benzodiazepine receptor interaction of esters of beta-carboline-3-carboxylic acid.
Ref 533584U-90042, a sedative/hypnotic compound that interacts differentially with the GABAA receptor subtypes. J Pharmacol Exp Ther. 1995 Nov;275(2):761-7.
Ref 533668J Med Chem. 1995 Jul 7;38(14):2663-71.Synthesis of carbon-11-, fluorine-18-, and iodine-125-labeled GABAA-gated chloride ion channel blockers: substituted 5-tert-butyl-2-phenyl-1,3-dithianes and -dithiane oxides.
Ref 533678J Med Chem. 1995 Aug 18;38(17):3297-312.Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
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 533762J Med Chem. 1995 Jan 6;38(1):16-20.Potential anxiolytic agents. Pyrido[1,2-a]benzimidazoles: a new structural class of ligands for the benzodiazepine binding site on GABA-A receptors.
Ref 533763J Med Chem. 1995 Jan 6;38(1):189-98.Synthetic routes to 4-amino-3-carboxy-beta-carboline derivatives: incidental formation of novel furo[3,4-c]-beta-carbolin-2-ones displaying high affinities for thebenzodiazepine receptor.
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 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 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 534122J Med Chem. 1996 Apr 26;39(9):1928-34.Synthesis and pharmacological properties of novel 8-substituted imidazobenzodiazepines: high-affinity, selective probes for alpha 5-containing GABAA receptors.
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 534157J Med Chem. 1996 Jul 19;39(15):2915-21.Synthesis and binding activity of some pyrazolo[1,5-c]quinazolines as tools to verify an optional binding site of a benzodiazepine receptor ligand.
Ref 534194Clobazam, oxcarbazepine, tiagabine, topiramate, and other new antiepileptic drugs. Epilepsia. 1995;36 Suppl 2:S105-14.
Ref 534442Regulation of neuronal and recombinant GABA(A) receptor ion channels by xenovulene A, a natural product isolated from Acremonium strictum. J Pharmacol Exp Ther. 1997 Aug;282(2):513-20.
Ref 534470J Med Chem. 1997 Sep 12;40(19):3109-18.Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new series of high-affinity and selective ligands for the peripheral type.
Ref 534629J Med Chem. 1998 May 21;41(11):1846-54.Propofol analogues. Synthesis, relationships between structure and affinity at GABAA receptor in rat brain, and differential electrophysiological profile at recombinant human GABAA 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 534710J Med Chem. 1998 Sep 24;41(20):3821-30.N'-Phenylindol-3-ylglyoxylohydrazide derivatives: synthesis, structure-activity relationships, molecular modeling studies, and pharmacological action on brain benzodiazepine receptors.
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 534920GABA receptors inhibited by benzodiazepines mediate fast inhibitory transmission in the central amygdala. J Neurosci. 1999 Nov 15;19(22):9698-704.
Ref 535248Hyperekplexia in neonates. Postgrad Med J. 2001 Sep;77(911):570-2.
Ref 535818Cyclooctadepsipeptides--an anthelmintically active class of compounds exhibiting a novel mode of action. Int J Antimicrob Agents. 2003 Sep;22(3):318-31.
Ref 536166Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17.
Ref 536224Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
Ref 536447Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52.
Ref 536463The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
Ref 536555DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6. Epub 2007 Nov 29.
Ref 536710Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
Ref 537706Anticonvulsant drugs: mechanisms of action. Adv Neurol. 1986;44:713-36.
Ref 537788THIP treatment of Huntington's disease. Neurology. 1983 May;33(5):637-9.
Ref 551228(?)-2-amino-2-thiazoline-4-ethanoic acid; a novel, specific GABAA receptor agonist. Bioorg. Med. Chem. Lett. 1(5):247-248 (1991).
Ref 551248N-2 methylated quaternary derivatives of beta-carboline-3-carboxylates inhibit acetylcholinesterase in vitroO, Bioorg. Med. Chem. Lett. 3(12):2831-2836 (1993).
Ref 551288Isosteric replacement of the indole nucleus by benzothiophene in a series of pyrido[2,3-b]indoles with potential anxiolytic activity, Bioorg. Med. Chem. Lett. 5(22):2589-2592 (1995).
Ref 5512906,3'-Dinitroflavone, a novel high affinity ligand for the benzodiazepine receptor with potent anxiolytic properties, Bioorg. Med. Chem. Lett. 5(22):2717-2720 (1995).
Ref 551293Partial structures of the fungal toxin aflatrem, methyl-substituted 6,8-dioxabicyclo[3.2.1]octan-2-ones have anticonvulsant activity, Bioorg. Med. Chem. Lett. 5(3):265-270 (1995).
Ref 551302A study of 3-amino-N-hydroxypropanesulfonamide derivatives as potential GABAB agonists and their fragmentation to 3-aminopropanesulfinic acid, Bioorg. Med. Chem. Lett. 6(14):1709-1714 (1996).
Ref 551323Synthesis of halogenated/nitrated flavone derivatives and evaluation of their affinity for the central benzodiazepine receptor, Bioorg. Med. Chem. Lett. 7(15):2003-2008 (1997).
Ref 5513366-Bromo-3??nitroflavone, a new high affinity benzodiazepine receptor agonist recognizes two populations of cerebral cortical binding sites, Bioorg. Med. Chem. Lett. 7(3):373-378 (1997).
Ref 551657Capreomycin Binds across the Ribosomal Subunit Interface Using tlyA-Encoded 2??O-Methylations in 16S and 23S rRNAs. Molecular Cell Volume 23, Issue 2, 21 July 2006, Pages 173-182.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 551901US patent application no. US20040102438 A1.

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