Target Information

Target General Infomation
Target ID
T51487
Former ID
TTDS00403
Target Name
Gamma-aminobutyric acid receptor subunit alpha-1
Gene Name
GABRA1
Synonyms
GABA(A) receptor subunit alpha-1; GABRA1
Target Type
Successful
Disease Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Anesthesia [ICD9: 338; ICD10: R20.0]
Depression [ICD9: 311; ICD10: F30-F39]
Epileptic seizures [ICD9: 345.9, 780.3; ICD10: G40, P90, R56]
Epilepsy; Anxiety disorder [ICD9: 300, 345; ICD10: F40-F42, G40]
Epilepsy [ICD10: G40]
Headache; Anxiety disorder [ICD9:339, 784.0, 300, 311; ICD10: G43-G44, R51, F32, F40-F42]
Intractable chronic pain; Cystitis [ICD9:338, 780; ICD10: R52, G89, N30]
Insomnia; Epilepsy [ICD9:307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F51.0, G47.0, G40]
Inflammation [ICD10: E08-E13, E10.2, E11, E11.2, E13.2, I73.9, I80-I82, N00-N29, G89]
Insomnia [ICD9: 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F51.0, G47.0]
Insomnia; Anxiety disorder [ICD9:307.41, 307.42, 327.0, 780.51, 780.52, 300, 311; ICD10: F51.0, G47.0, F32, F40-F42]
Intractable insomnia [ICD10: G47]
Muscle spasm [ICD10: M62.838]
Premenstrual syndrome [ICD10: N94.3]
Respiratory distress syndrome [ICD9: 518.5, 518.82; ICD10: J80]
Sleep maintenance insomnia [ICD9: 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F51.0, G47.0]
Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand- gated chloride channel (By similarity).
BioChemical Class
Ligand-gated ion channel
Target Validation
T51487
UniProt ID
P14867
Sequence
MRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPG
LGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHAC
PLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVM
TTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDP
LIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKID
RLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
Drugs and Mode of Action
Drug(s) Amobarbital Drug Info Approved Insomnia; Anxiety disorder [550722], [551871]
Barbital Drug Info Approved Insomnia [536555]
Barbituric acid Drug Info Approved Depression [536555]
Butabarbital Drug Info Approved Insomnia [538357], [542144]
Butalbital Drug Info Approved Headache; Anxiety disorder [538316], [542145], [551871]
Butethal Drug Info Approved Insomnia [550763]
Clobazam Drug Info Approved Epilepsy; Anxiety disorder [542156], [550702]
Ethanol Drug Info Approved Intractable chronic pain; Cystitis [537292], [539450], [551871]
Ethchlorvynol Drug Info Approved Insomnia [538355], [542191]
Hexobarbital Drug Info Approved Anesthesia [550698]
Meprobamate Drug Info Approved Anxiety disorder [538193], [542240]
Methohexital Drug Info Approved Anesthesia [538449], [542249]
Methoxyflurane Drug Info Approved Anesthesia [542250], [550732]
Methylphenobarbital Drug Info Approved Anxiety disorder [550692]
Methyprylon Drug Info Approved Insomnia [536255], [542254]
Nitrazepam Drug Info Approved Insomnia; Epilepsy [550758], [551871]
Pentobarbital Drug Info Approved Insomnia; Anxiety disorder [538348], [540880], [551871]
Picrotoxin Drug Info Approved Respiratory distress syndrome [540650], [550699]
Primidone Drug Info Approved Epilepsy [538190], [540777]
Secobarbital Drug Info Approved Intractable insomnia [551871]
THIOCOLCHICOSIDE Drug Info Approved Muscle spasm [551871]
Zaleplon Drug Info Approved Insomnia [467682], [538325]
Zolpidem Drug Info Approved Insomnia [467685], [551871]
ZK-93423 Drug Info Phase 3 Epileptic seizures [467683], [533661]
ALLOPREGNANOLONE Drug Info Phase 2 Discovery agent [467451], [524035]
Zolpidem Drug Info Phase 1 Sleep maintenance insomnia [531325]
ELTANOLONE Drug Info Discontinued in Phase 3 Premenstrual syndrome [546011]
U-78875 Drug Info Discontinued in Phase 1 Anxiety disorder [544810]
CGS-9896 Drug Info Terminated Discovery agent [544687]
Divaplon Drug Info Terminated Discovery agent [544692]
Inhibitor (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]
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-(1H-Indol-3-yl)-2-oxo-N-phenethyl-acetamide Drug Info [526738]
2-(3-Bromo-phenyl)-6-nitro-chromen-4-one Drug Info [551323]
2-(3-Bromo-phenyl)-chromen-4-one Drug Info [551323]
2-(3-Chloro-phenyl)-chromen-4-one Drug Info [551323]
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-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-(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-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 [533363]
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-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-(biphenyl-3-yl)-5-(piperidin-4-yl)isoxazol-3-ol Drug Info [530818]
4-benzyl-5-(4-piperidyl)isothiazol-3-ol Drug Info [528034]
4-Benzyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info [527382]
4-Methoxymethyl-3,6-dipropoxy-9H-beta-carboline Drug Info [534660]
4-Methyl-5-(4-piperidyl)isothiazol-3-ol Drug Info [528034]
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 [527382]
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 [527382]
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-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-Methyl-2-oxa-spiro[4.4]nonan-1-one Drug Info [533975]
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]
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]
ALLOPREGNANOLONE Drug Info [527511]
AMENTOFLAVONE Drug Info [526653]
Barbituric acid derivative Drug Info [551407]
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]
CGP-27492 Drug Info [533678]
CGS-13767 Drug Info [529466]
CGS-8216 Drug Info [529466]
CGS-9895 Drug Info [533348]
CGS-9896 Drug Info [528080]
CI-218872 Drug Info [533745]
Divaplon Drug Info [533379]
ELTANOLONE Drug Info [527511]
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]
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-(p-methylbenzyl)-5-nitroindol-3-ylglyoxylamide Drug Info [528709]
N-Benzyl-2-(1H-indol-3-yl)-2-oxo-acetamide Drug Info [528709]
N-benzyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide Drug Info [528709]
N-butyl-2-(1H-indol-3-yl)-2-oxoacetamide Drug Info [528709]
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]
NORHARMANE Drug Info [533363]
NSC-19028 Drug Info [551323]
NSC-73613 Drug Info [551323]
NSC-93394 Drug Info [551323]
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 [534008]
Ro-154513 Drug Info [534008]
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]
U-78875 Drug Info [525465]
U-89267 Drug Info [533912]
ZK-93423 Drug Info [530319]
Antagonist Amobarbital Drug Info [536555], [537688]
Barbital Drug Info [536555], [537688]
Barbituric acid Drug Info [536555], [537688]
Butabarbital Drug Info [535022], [536555], [537688]
Butalbital Drug Info [536555]
Butethal Drug Info [536555]
Clobazam Drug Info [536555]
Ethanol Drug Info [536555]
Ethchlorvynol Drug Info [536555]
Hexobarbital Drug Info [536555], [537688]
Meprobamate Drug Info [536555]
Methohexital Drug Info [536555]
Methoxyflurane Drug Info [536555]
Methylphenobarbital Drug Info [536555], [537688]
Methyprylon Drug Info [536555]
Nitrazepam Drug Info [536555]
Pentobarbital Drug Info [536555], [537688]
Picrotoxin Drug Info [536555]
Primidone Drug Info [536555]
Secobarbital Drug Info [536555], [537688]
Modulator Zaleplon Drug Info [556264]
Zolpidem Drug Info
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Retrograde endocannabinoid signaling
GABAergic synapse
Morphine addiction
Nicotine addiction
Reactome Ligand-gated ion channel transport
GABA A receptor activation
WikiPathways SIDS Susceptibility Pathways
Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell
Iron uptake and transport
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 467682(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: 4345).
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 467685(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: 4348).
Ref 524035ClinicalTrials.gov (NCT01673828) Allopregnanolone for the Treatment of Traumatic Brain Injury. U.S. National Institutes of Health.
Ref 531325Improved insomnia symptoms and sleep-related next-day functioning in patients with comorbid major depressive disorder and insomnia following concomitant zolpidem extended-release 12.5 mg and escitalopram treatment: a randomized controlled trial. J Clin Psychiatry. 2011 Jul;72(7):914-28.
Ref 533661Abecarnil enhances GABA-induced currents in acutely isolated cerebellar Purkinje cells. Neuropharmacology. 1995 Feb;34(2):157-63.
Ref 536255Nonlinear elimination of methyprylon (noludar) in an overdosed patient: correlation of clinical effects with plasma concentration. J Pharm Sci. 1991 Aug;80(8):768-71.
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 537292Preclinical evaluation of riluzole: assessments of ethanol self-administration and ethanol withdrawal symptoms. Alcohol Clin Exp Res. 2009 Aug;33(8):1460-8.
Ref 538190FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040586.
Ref 538193FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040797.
Ref 538316FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 076528.
Ref 538325FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 077237.
Ref 538348FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 083270.
Ref 538355FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 084463.
Ref 538357FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 085550.
Ref 538449FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 011559.
Ref 539450(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: 2299).
Ref 540650(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: 4051).
Ref 540777(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: 5338).
Ref 540880(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: 5480).
Ref 542144(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: 7137).
Ref 542145(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: 7138).
Ref 542156(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: 7149).
Ref 542191(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: 7180).
Ref 542240(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: 7225).
Ref 542249(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: 7233).
Ref 542250(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: 7234).
Ref 542254(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: 7238).
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 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 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 550692Drug information of Methylphenobarbital, 2008. eduDrugs.
Ref 550698Drug information of Hexobarbital, 2008. eduDrugs.
Ref 550699Drug information of Fish berry, 2008. eduDrugs.
Ref 550702Drug information of Clobazam, 2008. eduDrugs.
Ref 550722Drug information of Amobarbital, 2008. eduDrugs.
Ref 550732Drug information of Methoxyflurane, 2008. eduDrugs.
Ref 550758Drug information of Nitrazepam, 2008. eduDrugs.
Ref 550763Drug information of Soneryl, 2008. eduDrugs.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
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 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 526653Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors.
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 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 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 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 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 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 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 530818J Med Chem. 2010 Apr 22;53(8):3417-21.Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acid(A) receptor ligands: synthesis, pharmacology, and structure-activity relationships.
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 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 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 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 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 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 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 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 535022Hypnotic drugs. Med Lett Drugs Ther. 2000 Aug 7;42(1084):71-2.
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 537688Effect of barbiturates on polyphosphoinositide biosynthesis and protein kinase C activity in synaptosomes. Neuropharmacology. 1989 Dec;28(12):1317-23.
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 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 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 551407Whiting PJ: The <span class="caps">GABAA</span> receptor gene family: new opportunities for drug development. Curr Opin Drug Discov Devel. 2003 Sep;6(5):648-57.
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.