GABA Receptor

The GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory compound in the mature vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors); whereas GABAB receptors are G protein-coupled receptors, also called metabotropic receptors.

Cat No.	product name
T0024	Primidone	Primidone is an anticonvulsant of the pyrimidinedione class.
T0028	4-Amino-3-hydroxybutyric Acid	Agent for improving learning or memory [US6803366]Gamma Hydroxybutyric Acid, commonly abbreviated GHB, is an illegal therapeutic drug in multiple countries. In ...
T0048	Nikethamide	Nikethamide is a stimulant which mainly influences the respiratory cycle. Widely known by its former sales name of Coramine, it was used in the mid-twentieth ce...
T0051	Urethane	Urethane was an antineoplastic agent .Now is used for other medicinal purposes.
T0128	Vigabatrin	Vigabatrin, an analogue of gamma-aminobutyric acid, is an irreversible inhibitor of 4-aminobutyrate transaminase responsible for the catabolism of γ-aminobuty...
T0169	Nefiracetam	Nefiracetam are underway in Phase 2 trials. Nefiracetam, a GABAergic、 cholinergic、and monoaminergic neuronal system enhancer, is used for Ro 5-4864-induced ...
T0349	Riluzole	Riluzole is a glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC L...
T0508	4-Aminobutyric acid	4-Aminobutyric acid is the most common inhibitory neurotransmitter in the central nervous system.
T0627	beta-Alanine	β-Alanine is a naturally occurring beta amino acid formed in vivo by the degradation of dihydrouracil and carnosine. It acts as a neurotransmitter by activatin...
T0675	Topiramate	Topiramate is a unique antiseizure medication that is used in the treatment of partial and generalized seizures. Topiramate has been rarely associated with hepa...
T0702	Gabapentin	Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain.
T0883	Homotaurine	Piroxicam is a nonsteroidal oxicam derivative with anti-inflammatory, antipyretic and analgesic properties.
T0954	Anestan	Halothane is a nonflammable, halogenated, hydrocarbon anesthetic that provides relatively rapid induction with little or no excitement. Analgesia may not be ade...
T0958	Penicillin G sodium salt	Penicillin G sodium is a penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is eff...
T10456	Bamaluzole	Bamaluzole is an agonist of GABA receptor extracted from patent WO 2012064642 A1.
T1065	Baclofen	Baclofen is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing Baclofen ac...
T10757L	Cenobamate	Cenobamate, a sodium channel blocker, enhances GABAergic transmission. It has the potential to be a versatile CNS drug.
T10869L	CP-409092	CP-409092 is a partial GABAA receptor agonist. It has anti-anxiety activity.
T1089	Etomidate	Etomidate is a GABAA receptor agonist, with a short-acting sedative, hypnotic, and general anesthetic properties.
T11061	DMCM hydrochloride	DMCM hydrochloride is a non-selective fully inverse agonist of benzodiazepine. DMCM showed significant differences in human recombinant GABAA zaerxep3 receptor ...
T11137	(E)-GABAB receptor antagonist 1	(E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.(E)-GABAB receptor antagonist 1 is a trans-...
T11277	FG 7142	FG 7142 also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 can increase tyrosine hydroxylati...
T1128	Oxiracetam	Oxiracetam, a cyclic derivative of gamma-aminobutyric acid (GABA), is utilized for the treatment of cognitive impairments.
T11350	GABAB receptor antagonist 1	(E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.GABAB receptor antagonist 1 is a selectiv...
T11686	Isotanshinone I	Isotanshinone I with IC50s of 1.13 μM and 0.432 μM for α-glucosidase and AGE, respectively. Isotanshinone I has inhibitory activity against α-glucosidase an...
T11822	LAU159	LAU159 is a functionally selective positive α1β3 GABA(A) receptor modulator(EC50 : 2.2 μM).
T12043	(-)-Bicuculline methobromide	(-)-Bicuculline methobromide is a potent antagonist of GABAA receptor .
T12044	(-)-Bicuculline methochloride	(-)-Bicuculline methochloride is a potent antagonist of GABAA receptor.
T1240	Flumazenil	Flumazenil antagonizes the benzodiazepine binding site of the gamma-aminobutyric acid (GABA)/benzodiazepine receptor complex in the central nervous system (CNS)...
T12867	SCH 50911 hydrochloride	SCH 50911 hydrochloride is a selective, orally-active and competitive antagonist of γ-Aminobutyric acid B GABA(B) receptor(IC50 : 1.1 μM).
T12867L	SCH 50911	SCH 50911 is (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid and is a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist,...
T1396	Bemegrid	Bemegride is a central nervous system stimulant and antidote for barbiturate poisoning.
T1413	Pentetrazol	Pentylenetetrazol is a GABA(A) receptor antagonist, that displays activity as a central nervous system and respiratory stimulant.
T14571	Bifenazate	Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm[1] and it also is a positive allosteric modulator of GABA receptor[2...
T14938	CGP 36742	CGP 36742 is a selective antagonist of the GABAB receptor that can penetrate the blood-brain barrier after peripheral administration (IC50: 32 μM). It is use...
T15212	Emamectin Benzoate	Emamectin Benzoate, by binding gamma-aminobutyric acid (GABA) receptor and glutamate-gated chloride channels disrupting nerve signals within arthropods, acts as...
T15380	Gidazepam	Gidazepam is an GABA receptor channels agonist.
T15737	Lesogaberan	Lesogaberan is an effective and selective GABAB receptor agonist (EC50: 8.6 nM for human recombinant GABAB receptors). For rat brain GABAB and GABAA receptors, ...
T1602	Valproic acid sodium salt	Valproate Sodium is the sodium salt form of valproic acid with anti-epileptic activity. Valproate sodium is converted into its active form, valproate ion, in bl...
T16581	Progabide	Progabide is an agonist of the gamma-aminobutyric acid receptor.
T16717	Radequinil	Radequinil is a benzodiazepine receptor partial inverse agonist. Rade quinil binds to GABA(-) and GABA(+) ligand (Kis: 5.15 and 6.11 nM, respectively).
T1673	Acamprosate calcium	Acamprosate calcium is a GABA receptor agonist and modulator of glutamatergic systems, used for treating alcohol dependence.
T16794	RO 4938581	RO 4938581 is an effective and selective agonist of GABAA α5 inverse (Ki: 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α...
T16811	RWJ-51204	RWJ-51204 is a partial agonist of GABA(A) receptor (Ki: 0.2-2 nM).
T17144	TPA 023	TPA 023 is an agonist of the GABAA α2/α3 subtype-selective (Ki: 0.19-0.41 nM).
T17215	Valnoctamide	Valnoctamide inhibits benzodiazepine-refractory status epilepticus. Valnoctamide acts directly on GABAA receptors.
T17306	Arbaclofen hydrochloride	(R)-Baclofen hydrochloride is a selective agonist of the GABAB receptor.
T1860	AWD 131-138	AWD 131-138(Imepitoin) is a new low-affinity partial benzodiazepine receptor agonist. It shows potent anticonvulsant and anxiolytic properties in rodent models.
T19624	Fasoracetam	Fasoracetam is a modulator of GABA receptor potentially for the treatment of attention deficit hyperactivity disorder.
T2067	NS 11394	NS11394 is a effective and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of α(5) > α(3) > α(2) >...
T2196	Fipronil	Fipronil is a broad-use insecticide that belongs to the phenylpyrazole chemical family. Fipronil is a broad-spectrum insecticide that disrupts the insect centra...
T2339	Apalutamide	Apalutamide is a small molecule and androgen receptor (AR) antagonist with potential antineoplastic activity.
T2407	Tiagabine	Tiagabine is an Anti-epileptic Agent. The physiologic effect of tiagabine is by means of Decreased Central Nervous System Disorganized Electrical Activity.
T2749	Ginkgolide A	Ginkgolide A is a highly active PAF antagonist cage molecule that is isolated from the leaves of the Ginkgo biloba tree. Shows potential in a wide variety of in...
T2775	Baicalin	Baicalin is a prolyl endopeptidase inhibitor isolated from scutellaria baicalensis, with antioxidant, anti-tumor, anti-HIV properties.
T2850	(+)-Bicuculline	Bicuculline is a light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolate...
T2990	Phenibut	Phenibut is a central depressant and derivative of the naturally occurring inhibitory neurotransmitter γ-aminobutyric acid (GABA).
T2998	Dihydromyricetin	Dihydromyricetin is a natural antioxidant flavonoid from Ampelopsis grossedentata. Dihydromyricetin is a potent inhibitor of dihydropyrimidinase with an IC50 of...
T3318	Wogonoside	Wogonoside acts as a positive allosteric modulator of the benzodiazepine site of the GABAA receptor.
T3403	Glabridin	Glabridin may serve as an anti-inflammatory agent in diabetes-related vascular dysfunction,through regulating the synthesis and activity of iNOS under high-gluc...
T3644	U93631	GABAA receptor antagonist that binds the picrotoxin site and stabilizes the inactive form of the channel via allosteric interaction. Accelerates the decay of G...
T3927	Phellopterin	Phellopterin is a partial agonist of the central benzodiazepine receptors in vitro. Phellopterin shows a cytotoxic effect on RAW264.7 cell at the concentration ...
T3S2100	Securinine	(-)-Securinine is plant-derived alkaloid and also a GABAA receptor antagonist.
T3S2259	Methyl eugenol	1. Methyleugenol (ME) is a natural constituent of the essential oils of a number of plants widely used in foodstuffs as flavouring agents, in view of the carci...
T4176	rac-BHFF	Rac-BHFF is potent and selective GABA B receptor positive allosteric modulator that increases the potency and efficacy of GABA ( > 15-fold and > 149% respective...
T4363	CGP 52432	CGP52432 is a very potent antagonist of GABAB receptors (IC50 = 85 nM).
T4440	Saclofen	Saclofen is a sulfonic analog of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) that acts as a competitive antagonist of the GABAB receptor (IC50: ...
T4522	SSD114 hydrochloride	SSD114 is a novel GABAB receptor positive allosteric modulator.
T4655	Pipequaline	Pipequaline is an anticonflict & anticonvulsant quinoline derivative. It is an anxiolytic drug that was never marketed. It possesses a novel chemical structure ...
T4682	Allopregnanolone	Allopregnanolone is under investigation for the treatment of Super-Refractory Status Epilepticus.Allopregnanolone has been investigated for the treatment of Sev...
T4688	Pipequaline hydrochloride	Pipequaline is an anticonflict & anticonvulsant quinoline derivative. It is an anxiolytic drug that was never marketed. It possesses a novel chemical structure ...
T4993	Afloqualone	Afloqualone is a agonist of GABA receptor . Target: GABA Receptor in vitro: Afloqualone is a quinazolinone family GABAergic drug. Afloqualone is an analogue of ...
T4S1616	Sanggenone D	Sanggenone D represents a new scaffold of positive GABAA receptor modulators, it also inhibits COX-2 activity (IC 50 = 73-100 μM). Sanggenone D has anti-inflam...
T5330	Fluralaner	Fluralaner is an isoxazoline ectoparasiticide. It potently and selectively inhibits binding of the GABA receptor channel blocker EBOB to housefly head membranes...
T5375	Loreclezole	Loreclezole is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit-containing receptors.
T5734	(+)-BORNEOL	(+)-BORNEOL is a natural bicyclic monoterpene used for analgesia and anesthesia in traditional Chinese medicine; enhances GABA receptor activity with an EC50 of...
T5880	Aminooxyacetic acid hemihydrochloride	Aminooxyacetic acid hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.
T6355	(R)-baclofen	(R)-baclofena， a derivative of gamma-aminobutyric acid，is commonly utilized for the treatment of spasticity.
T6507	Gabapentin HCl	Gabapentin HCl is a GABA analogue, used to treat seizures and neuropathic pain.
T7000	Tiagabine hydrochloride	Tiagabine Hydrochloride is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric ac...
T7064	Valproic Acid	Valproic Acid is a branched chain fatty acid which potentially enhances central GABAergic neurotransmission and inhibits Na+ channels. Currently, the various mo...
T7136	AZD6280	AZD6280 is a novel, subtype-selective GABAAα2/3 receptor positive modulators, used for treatment of generalized anxiety disorder.
T7165	Basmisanil	Basmisanil is a negative allosteric modulator/inverse agonist of GABAAα5 receptors.Formulations containing basmisanil are in clinical trials for the treatment ...
T7557	Guvacine hydrochloride	Guvacine hydrochloride is an inhibits of GABA uptake (IC50 : 10 μM)
T7622	Gabazine	Gabazine is an antagonist of GABAA receptors (Ki : 74-150 nM)
T7699	AZD-7325	AZD-7325 is a GABA-Aα2,3 -selective receptor modulator.
T7721	GANAXOLONE	Ganaxolone is a positive allosteric modulator of the action of the GABAA receptor, acts on well-characterized targets in the brain known to have anxiolytic and ...
T7793	6-(4-Methoxyphenyl)-3-pyridazinamine	6-(4-Methoxyphenyl)-3-pyridazinamine is a GABAA receptor antagonist
T7794	Zuranolone	Zuranolone is an agonist of GABAA receptor.
T7803	Gaboxadol (hydrochloride)	Gaboxadol (hydrochloride) is a GABAA receptor agonist.
T8036	6-Methylflavone	6-Methylflavone is an activator of α1β2γ2L and α1β2 GABAA receptors.
T8040	Cholesterol myristate	Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic ac...
T8162	Cannabidivarin	Cannabidivarin is a potent inhibitor against gamma 2 subunit of GABAA receptors. it may serve as a novel drug with definite control over childhood absence epile...
T8193	Thujone	Thujone is an inhibitor of ACh with an IC50 value of 24.7μM.
T8268	6,2'-Dihydroxyflavone	6,2'-Dihydroxyflavone is a novel antagonist of GABAA receptor.
T8568	Suritozole	Suritozole is a negative modulator at the gamma-aminobutyric acidA (GABAA) receptor
T8572	CL 218872	CL 218872 is a benzodiazepine agonist displaying selectivity for α1 subunit-containing GABAA receptors (Ki values are 130, 1820, 1530, > 10000, 490 and > 10000...
T8630	Baclofen hydrochloride	Baclofen hydrochloride is a GAMMA-AMINOBUTYRIC ACID derivative that is a specific GABA-B RECEPTORS agonist. It is used in the treatment of MUSCLE SPASTICITY, e...
T8639	Phenibut (hydrochloride)	Phenibut (hydrochloride) is a GABA mimetic that acts as an agonist at GABAB receptors, blocks α2δ subunit-containing voltage-gated calcium channels, stimulat...
T8664	SSD114 hydrochloride	SSD114 hydrochloride is a GABAB receptor positive allosteric modulator.
T9113	Myristicin	Myristicin has anti-cholinergic, antibacterial, and hepatoprotective effects, it also has anti-inflammatory properties related with its inhibition of NO, cytoki...
TN1027	beta-Amyrin	beta-Amyrin has antiviral, hepatoprotective, antinociceptive, anti-inflammatory, it retard acute inflammation in rat model of periodontitis.
TN1420	Bacopaside I	Bacopaside I is a modulator of Aquaporin-1 channel, has neuroprotective functions, it has anti-Alzheimer's disease, it ameliorates cognitive impairment in APP/P...
TN1432	Bacopasaponin C	Bacopasaponin C may have antioxidant activity, it also shows anti-leishmanial property.
TN1591	DL-Menthol	DL-Menthol has short term toxicity in rats, it plays a role in the induction of surgical anesthesia in fishes, related at least in part to the activation of GAB...
TN1717	Guvacine	Guvacine can enhance the inhibition of spinal neurones by GABA.
TN1842	Kushenol I	Kushenol I is a GABAA receptor modulator, it exhibits inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2).Kushenol I is shown to be acti...
TN2268	Tetrahydromagnolol	Tetrahydromagnolol can activate cannabinoid (CB) receptors.
TN3351	Aflatrem	Aflatrem is a tremorgenic mycotoxin with acute neurotoxic effects, a single low dose of aflatrem is able to induce degeneration of neuronal processes in hippoca...
TN3702	(-)-Corlumine	Corlumine exhibits spasmolytic and GABA antagonist activity.
TN3868	Dihydroxyaflavinine	Dihydroxyaflavinine is a fungal toxin, it inhibits non-competitively GABAA receptor channel expressed in Xenopus oocytes.Dihydroxyaflavinine shows oral toxicity...
TN4298	Isohyenanchin	Isohyenanchin is the potent antagonist of RDLac homo-oligomers, it is also a weak antagonist of ionotropic GABA receptors.
TN4322	Isopulegol	Isopulegol presents depressant- and anxiolytic-like effects, it also has anticonvulsant and bioprotective effects against PTZ-induced convulsions are possibly r...
TN4440	Limonexic acid	Limonexic acid shows antinociceptive actions , it produces dose-related inhibition of glutamate- and capsaicin-induced pain. Limonexic acid can effectively prot...
TN5089	Tabernanthine	Tabernanthine shows affinity for opiate receptors, it can decrease morphine and cocaine self-administration in rats, it may be effective in treating addiction t...
TN5147	Tilifodiolide	Tilifodiolide exerts in vitro and in vivo anti-inflammatory activity and in vivo antinociceptive effects. Tilifodiolide exerted antidiarrheal activity by decrea...
TQ0023	Lorediplon	Lorediplon is a novel hypnotic drug acting as a GABAA receptor modulator, differentially active at the α1-subunit, associated with promoting sleep.
TQ0040	ONO-8590580	ONO-8590580 is a negative allosteric modulator of GABAA α5.
TQ0119	Cirsimaritin	Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors. It has antibacterial, anti-inflammation, anti-tumor, antioxidant, renal protection.
TQ0151	L-655708	L-655708 is an effective inverse agonist of the α5 subunit-selective GABAA receptor (Ki: 0.45 nM).