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Membrane transporter/Ion channel GABA Receptor

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
TN6773 Acetoxyvalerensre Acetoxyvalerensre (acetylvalerenolic acid) is a derivative of valerenic acid, which is a a GABAA receptor modulator.
TMS0418 Dihydroergotoxine mesylate It is mainly used to improve symptoms and physical symptoms of mental degeneration related to aging.
T1673 Acamprosate calcium Acamprosate calcium is a GABA receptor agonist and modulator of glutamatergic systems, used for treating alcohol dependence.
T1240 Flumazenil Flumazenil antagonizes the benzodiazepine binding site of the gamma-aminobutyric acid (GABA)/benzodiazepine receptor complex in the central nervous system (CNS),...
T2983 3,4,5-Trimethoxycinnamic acid 3,4,5-Trimethoxycinnamic acid (TMCA) is one of the constituents of Polygalae Radix and may exert anti-seizure activity by acting at the GABAA/BZ receptor complex...
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) > ...
T2339 Apalutamide Apalutamide is a small molecule and androgen receptor (AR) antagonist with potential antineoplastic activity.
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 hepat...
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% respectivel...
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: 7...
T4363 CGP 52432 CGP52432 is a very potent antagonist of GABAB receptors (IC50 = 85 nM).
T4331 Zolpidem Tartrate Zolpidem is a prescription medication used for the treatment of insomnia and some brain disorders. This drug is a controlled substance and has been discontinued....
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 f...
T7064 Valproic Acid Valproic Acid is a branched chain fatty acid which potentially enhances central GABAergic neurotransmission and inhibits Na+ channels. Currently, the various mol...
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 carcino...
T4522 SSD114 hydrochloride SSD114 is a novel GABAB receptor positive allosteric modulator.
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 t...
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 effe...
T4655 Pipequaline Pipequaline is an anticonflict & anticonvulsant quinoline derivative. It is an anxiolytic drug that was never marketed. It possesses a novel chemical structure t...
T4682 Allopregnanolone Allopregnanolone is under investigation for the treatment of Super-Refractory Status Epilepticus.Allopregnanolone has been investigated for the treatment of Seve...
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 m...
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.
T7165 Basmisanil Basmisanil is a negative allosteric modulator/inverse agonist of GABAAα5 receptors.Formulations containing basmisanil are in clinical trials for the treatment o...
T7136 AZD6280 AZD6280 is a novel, subtype-selective GABAAα2/3 receptor positive modulators, used for treatment of generalized anxiety disorder.
T7622 Gabazine Gabazine is an antagonist of GABAA receptors (Ki : 74-150 nM)
T7595 L-DAB HBR L-DAB HBR is an inhibitor of GABA transaminase  (IC50 > 500 μM).
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 a...
T7557 Guvacine hydrochloride Guvacine hydrochloride is an inhibits of GABA uptake (IC50 : 10 μM)
TQ0023 Lorediplon Lorediplon is a novel hypnotic drug acting as a GABAA receptor modulator, differentially active at the α1-subunit, associated with promoting sleep.
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 c...
T6355 (R)-baclofen (R)-baclofena, a derivative of gamma-aminobutyric acid, is commonly utilized for the treatment of spasticity.
TQ0119 Cirsimaritin Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors. It has antibacterial, anti-inflammation, anti-tumor, antioxidant, renal protection.
T2998 Dihydromyricetin Dihydromyricetin is a natural antioxidant flavonoid from Ampelopsis grossedentata. Dihydromyricetin is a potent inhibitor of dihydropyrimidinase with an IC50 of ...
T2990 Phenibut Phenibut is a central depressant and derivative of the naturally occurring inhibitory neurotransmitter γ-aminobutyric acid (GABA).
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 activating...
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 act...
T2407 Tiagabine Tiagabine is an Anti-epileptic Agent. The physiologic effect of tiagabine is by means of Decreased Central Nervous System Disorganized Electrical Activity.
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 central...
T0024 Primidone Primidone is an anticonvulsant of the pyrimidinedione class.
T0128L Vigabatrin Hydrochloride Vigabatrin HCl is a structural analog of the inhibitory neurotransmitter γ-aminobutyric acid (GABA), which irreversibly inhibits the catabolism of GABA by GABA ...
T7000 Tiagabine hydrochloride Tiagabine Hydrochloride is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric aci...
T0954 Anestan Halothane is a nonflammable, halogenated, hydrocarbon anesthetic that provides relatively rapid induction with little or no excitement. Analgesia may not be adeq...
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 GA...
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 inf...
T0349 Riluzole Riluzole is a glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LA...
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.
T2775 Baicalin Baicalin is a prolyl endopeptidase inhibitor isolated from scutellaria baicalensis, with antioxidant, anti-tumor, anti-HIV properties.
T1089 Etomidate Etomidate is a GABAA receptor agonist, with a short-acting sedative, hypnotic, and general anesthetic properties.
T2940 6-Hydroxyflavone 6-Hydroxyflavone is a noncompetitive inhibitors of cytochrome P450 2C9. It is a flavone, a type of chemical compound. It is reported in leaves of Barleria prioni...
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 cen...
T1396 Bemegrid Bemegride is a central nervous system stimulant and antidote for barbiturate poisoning.
T1128 Oxiracetam Oxiracetam, a cyclic derivative of gamma-aminobutyric acid (GABA), is utilized for the treatment of cognitive impairments.
T0128 Vigabatrin Vigabatrin, an analogue of gamma-aminobutyric acid, is an irreversible inhibitor of 4-aminobutyrate transaminase responsible for the catabolism of γ-aminobutyri...
T0702 Gabapentin Gabapentin is an Anti-epileptic Agent. The physiologic effect of gabapentin is by means of Decreased Central Nervous System Disorganized Electrical Activity.
T6507 Gabapentin HCl Gabapentin HCl is a GABA analogue, used to treat seizures and neuropathic pain.
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...
T0508 4-Aminobutyric acid 4-Aminobutyric acid is the most common inhibitory neurotransmitter in the central nervous system.
T0710 L-Cycloserine L-cycloserine irreversibly inhibits GABA pyridoxal 5′-phosphate-dependent aminotransferase in E. coli, as well in the brains of various animals, results in inc...
T1413 Pentetrazol Pentylenetetrazol is a GABA(A) receptor antagonist, that displays activity as a central nervous system and respiratory stimulant.
T0051 Urethane Urethane was an antineoplastic agent .Now is used for other medicinal purposes.
T3318 Wogonoside Wogonoside acts as a positive allosteric modulator of the benzodiazepine site of the GABAA receptor.
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 isolated...
T3741 (-)-borneol (-)-Borneol has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.
T0883 Homotaurine Because of its similarity in structure to the neurotransmitter gamma-aminobutyric acid (GABA), it has GABAergic effects and may be useful as an anticonvulsant. H...
TQ0040 ONO-8590580 ONO-8590580 is a negative allosteric modulator of GABAA α5.
TQ0151 L-655708 L-655708 is an effective inverse agonist of the α5 subunit-selective GABAA receptor (Ki: 0.45 nM).
TN6773 Acetoxyvalerensre Acetoxyvalerensre (acetylvalerenolic acid) is a derivative of valerenic acid, which is a a GABAA receptor modulator.
T8568 Suritozole Suritozole is a negative modulator at the gamma-aminobutyric acidA (GABAA) receptor
T19624 Fasoracetam Fasoracetam is a modulator of GABA receptor potentially for the treatment of attention deficit hyperactivity disorder.
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 and...
T15775 Lotilaner Lotilaner is a parasiticide. It is used as a potent non-competitive antagonist of insects GABACl receptors (IC50 of 23.84 nM for Drosophila melanogaster GABA rec...
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).
T11822 LAU159 LAU159 is a functionally selective positive α1β3 GABA(A) receptor modulator(EC50 : 2.2 μM).
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, α3...
T16811 RWJ-51204 RWJ-51204 is a partial agonist of GABA(A) receptor (Ki: 0.2-2 nM).
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, ...
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 Arbaclofen hydrochloride, a Gamma-Aminobutyric Acid derivative, is a specific agonist of GABA-B receptors, it is used to treat spasticity, especially that due to...
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 ...
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, stimulate...
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, es...
T10456 Bamaluzole Bamaluzole is an agonist of GABA receptor extracted from patent WO 2012064642 A1.
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 to...
TN6765 Etiocholanone Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent neurosteroid p...
T21802 Etomidate hydrochloride Etomidate hydrochloride is a potent agonist of GABAA receptor. It is a neurological drug and effective parenteral medication and has the potential for management...
T8971 Imidazenil Imidazenil is an modulator of GABA-A that blocks the sedative effects without lowering the convulsion threshold.
T8887 2'MeO6MF 2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors.It offers neuroprotection and improved function...
T8664 SSD114 hydrochloride SSD114 hydrochloride is a GABAB receptor positive allosteric modulator.
TN5147 Tilifodiolide Tilifodiolide exerts in vitro and in vivo anti-inflammatory activity and in vivo antinociceptive effects. Tilifodiolide exerted antidiarrheal activity by decreas...
TN4440 Limonexic acid Limonexic acid shows antinociceptive actions , it produces dose-related inhibition of glutamate- and capsaicin-induced pain. Limonexic acid can effectively prote...
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-inflamm...
TN4322 Isopulegol Isopulegol presents depressant- and anxiolytic-like effects, it also has anticonvulsant and bioprotective effects against PTZ-induced convulsions are possibly re...
TN4298 Isohyenanchin Isohyenanchin is the potent antagonist of RDLac homo-oligomers, it is also a weak antagonist of ionotropic GABA receptors.
TN3868 Dihydroxyaflavinine Dihydroxyaflavinine is a fungal toxin, it inhibits non-competitively GABAA receptor channel expressed in Xenopus oocytes.Dihydroxyaflavinine shows oral toxicity ...
TN3702 (-)-Corlumine Corlumine exhibits spasmolytic and GABA antagonist activity.
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 hippocam...
T9113 Myristicin Myristicin is a natural product found in spices and umbelliferous plants. Myristicin has anti-cholinergic, antibacterial, and hepatoprotective effects, it also ...
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, t...
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 selective a...
T7794 Zuranolone Zuranolone is an agonist of GABAA receptor.
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 activ...
T7793 6-(4-Methoxyphenyl)-3-pyridazinamine 6-(4-Methoxyphenyl)-3-pyridazinamine is a GABAA receptor antagonist
T7803 Gaboxadol (hydrochloride) Gaboxadol (hydrochloride) is a GABAA receptor agonist.
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.
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 ace...
T3S2100 Securinine (-)-Securinine is plant-derived alkaloid and also a GABAA receptor antagonist.
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 epilep...
T7699 AZD-7325 AZD-7325 is a GABA-Aα2,3 -selective receptor modulator.
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/PS...
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 GABA...
TN1717 Guvacine Guvacine can enhance the inhibition of spinal neurones by GABA.
TN2268 Tetrahydromagnolol Tetrahydromagnolol can activate cannabinoid (CB) receptors.
T11349 GABAA receptor agent 1 GABAA receptor agent 1 has strong anticonvulsant activity and is a high affinity ligand of GABAA receptor.
T15212 Emamectin Benzoate Emamectin Benzoate, by binding gamma-aminobutyric acid (GABA) receptor and glutamate-gated chloride channels disrupting nerve signals within arthropods, acts as ...
T11307 Fluxametamide Fluxametamide is a novel isoxazoline insecticide that acts via distinctive antagonism of insect ligand-gated chloride channels, acts as an antagonist of GABA- an...
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 hydroxylation an...
T13690 Etifoxine hydrochloride Etifoxine is an anxiolytic and anticonvulsant drug. Unlike benzodiazepines, etifoxine appears to produce its anxiolytic effects by binding to β2 and β3 subuni...
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-G...
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).
T15380 Gidazepam Gidazepam is an GABA receptor channels agonist.
T10869L CP-409092 CP-409092 is a partial GABAA receptor agonist. It has anti-anxiety activity.
T12043 (-)-Bicuculline methobromide (-)-Bicuculline methobromide is a potent antagonist of GABAA receptor .
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 usef...
T10757L Cenobamate Cenobamate, a sodium channel blocker, enhances GABAergic transmission. It has a potential to be a versatile CNS drug.
T13536 Afoxolaner Afoxolaner is an isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect GABA and glutamate receptors, inhibiting GABA...
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]...
T11061 DMCM hydrochloride DMCM hydrochloride is a non-selective fully inverse agonist of benzodiazepine. DMCM showed significant differences in human recombinant GABAA zaerxep3 receptor s...
T12044 (-)-Bicuculline methochloride (-)-Bicuculline methochloride is a potent antagonist of GABAA receptor.
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 blo...
Acetoxyvalerensre
TN6773CAS 81397-67-3
Acetoxyvalerensre (acetylvalerenolic acid) is a derivative of valerenic acid, which is a a GABAA receptor modulator.
Dihydroergotoxine mesylate
TMS0418CAS 8067-24-1
It is mainly used to improve symptoms and physical symptoms of mental degeneration related to aging.
Acamprosate calcium
T1673CAS 77337-73-6
Acamprosate calcium is a GABA receptor agonist and modulator of glutamatergic systems, used for treating alcohol dependence.
Flumazenil
T1240CAS 78755-81-4
Flumazenil antagonizes the benzodiazepine binding site of the gamma-aminobutyric acid (GABA)/benzodiazepine receptor complex in the central nervous system (CNS),...
3,4,5-Trimethoxycinnamic acid
T2983CAS 90-50-6
3,4,5-Trimethoxycinnamic acid (TMCA) is one of the constituents of Polygalae Radix and may exert anti-seizure activity by acting at the GABAA/BZ receptor complex...
NS 11394
T2067CAS 951650-22-9
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) > ...
Apalutamide
T2339CAS 956104-40-8
Apalutamide is a small molecule and androgen receptor (AR) antagonist with potential antineoplastic activity.
Topiramate
T0675CAS 97240-79-4
Topiramate is a unique antiseizure medication that is used in the treatment of partial and generalized seizures. Topiramate has been rarely associated with hepat...
rac-BHFF
T4176CAS 123557-91-5
Rac-BHFF is potent and selective GABA B receptor positive allosteric modulator that increases the potency and efficacy of GABA ( > 15-fold and > 149% respectivel...
Saclofen
T4440CAS 125464-42-8
Saclofen is a sulfonic analog of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) that acts as a competitive antagonist of the GABAB receptor (IC50: 7...
CGP 52432
T4363CAS 139667-74-6
CGP52432 is a very potent antagonist of GABAB receptors (IC50 = 85 nM).
Zolpidem Tartrate
T4331CAS 99294-93-6
Zolpidem is a prescription medication used for the treatment of insomnia and some brain disorders. This drug is a controlled substance and has been discontinued....
Phellopterin
T3927CAS 2543-94-4
Phellopterin is a partial agonist of the central benzodiazepine receptors in vitro. Phellopterin shows a cytotoxic effect on RAW264.7 cell at the concentration f...
Valproic Acid
T7064CAS 99-66-1
Valproic Acid is a branched chain fatty acid which potentially enhances central GABAergic neurotransmission and inhibits Na+ channels. Currently, the various mol...
Methyl eugenol
T3S2259CAS 93-15-2
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 carcino...
SSD114 hydrochloride
T4522CAS T4522
SSD114 is a novel GABAB receptor positive allosteric modulator.
Pipequaline hydrochloride
T4688CAS 80221-58-5
Pipequaline is an anticonflict & anticonvulsant quinoline derivative. It is an anxiolytic drug that was never marketed. It possesses a novel chemical structure t...
Penicillin G sodium salt
T0958CAS 69-57-8
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 effe...
Pipequaline
T4655CAS 77472-98-1
Pipequaline is an anticonflict & anticonvulsant quinoline derivative. It is an anxiolytic drug that was never marketed. It possesses a novel chemical structure t...
Allopregnanolone
T4682CAS 516-54-1
Allopregnanolone is under investigation for the treatment of Super-Refractory Status Epilepticus.Allopregnanolone has been investigated for the treatment of Seve...
Afloqualone
T4993CAS 56287-74-2
Afloqualone is a agonist of GABA receptor . Target: GABA Receptor in vitro: Afloqualone is a quinazolinone family GABAergic drug. Afloqualone is an analogue of m...
Fluralaner
T5330CAS 864731-61-3
Fluralaner is an isoxazoline ectoparasiticide. It potently and selectively inhibits binding of the GABA receptor channel blocker EBOB to housefly head membranes ...
Loreclezole
T5375CAS 117857-45-1
Loreclezole is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit-containing receptors.
(+)-BORNEOL
T5734CAS 464-43-7
(+)-BORNEOL is a natural bicyclic monoterpene used for analgesia and anesthesia in traditional Chinese medicine; enhances GABA receptor activity with an EC50 of ...
Aminooxyacetic acid hemihydrochloride
T5880CAS 2921-14-4
Aminooxyacetic acid hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.
Basmisanil
T7165CAS 1159600-41-5
Basmisanil is a negative allosteric modulator/inverse agonist of GABAAα5 receptors.Formulations containing basmisanil are in clinical trials for the treatment o...
AZD6280
T7136CAS 942436-93-3
AZD6280 is a novel, subtype-selective GABAAα2/3 receptor positive modulators, used for treatment of generalized anxiety disorder.
Gabazine
T7622CAS 104104-50-9
Gabazine is an antagonist of GABAA receptors (Ki : 74-150 nM)
L-DAB HBR
T7595CAS 1758-80-1
L-DAB HBR is an inhibitor of GABA transaminase  (IC50 > 500 μM).
GANAXOLONE
T7721CAS 38398-32-2
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 a...
Guvacine hydrochloride
T7557CAS 6027-91-4
Guvacine hydrochloride is an inhibits of GABA uptake (IC50 : 10 μM)
Lorediplon
TQ0023CAS 917393-39-6
Lorediplon is a novel hypnotic drug acting as a GABAA receptor modulator, differentially active at the α1-subunit, associated with promoting sleep.
Nefiracetam
T0169CAS 77191-36-7
Nefiracetam are underway in Phase 2 trials. Nefiracetam, a GABAergic、 cholinergic、and monoaminergic neuronal system enhancer, is used for Ro 5-4864-induced c...
(R)-baclofen
T6355CAS 69308-37-8
(R)-baclofena, a derivative of gamma-aminobutyric acid, is commonly utilized for the treatment of spasticity.
Cirsimaritin
TQ0119CAS 6601-62-3
Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors. It has antibacterial, anti-inflammation, anti-tumor, antioxidant, renal protection.
Dihydromyricetin
T2998CAS 27200-12-0
Dihydromyricetin is a natural antioxidant flavonoid from Ampelopsis grossedentata. Dihydromyricetin is a potent inhibitor of dihydropyrimidinase with an IC50 of ...
Phenibut
T2990CAS 1078-21-3
Phenibut is a central depressant and derivative of the naturally occurring inhibitory neurotransmitter γ-aminobutyric acid (GABA).
beta-Alanine
T0627CAS 107-95-9
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 activating...
Baclofen
T1065CAS 1134-47-0
Baclofen is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing Baclofen act...
Tiagabine
T2407CAS 115103-54-3
Tiagabine is an Anti-epileptic Agent. The physiologic effect of tiagabine is by means of Decreased Central Nervous System Disorganized Electrical Activity.
Fipronil
T2196CAS 120068-37-3
Fipronil is a broad-use insecticide that belongs to the phenylpyrazole chemical family. Fipronil is a broad-spectrum insecticide that disrupts the insect central...
Primidone
T0024CAS 125-33-7
Primidone is an anticonvulsant of the pyrimidinedione class.
Vigabatrin Hydrochloride
T0128LCAS 1391054-02-6
Vigabatrin HCl is a structural analog of the inhibitory neurotransmitter γ-aminobutyric acid (GABA), which irreversibly inhibits the catabolism of GABA by GABA ...
Tiagabine hydrochloride
T7000CAS 145821-59-6
Tiagabine Hydrochloride is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric aci...
Anestan
T0954CAS 151-67-7
Halothane is a nonflammable, halogenated, hydrocarbon anesthetic that provides relatively rapid induction with little or no excitement. Analgesia may not be adeq...
U93631
T3644CAS 152273-12-6
GABAA receptor antagonist that binds the picrotoxin site and stabilizes the inactive form of the channel via allosteric interaction. Accelerates the decay of GA...
Ginkgolide A
T2749CAS 15291-75-5
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 inf...
Riluzole
T0349CAS 1744-22-5
Riluzole is a glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LA...
AWD 131-138
T1860CAS 188116-07-6
AWD 131-138(Imepitoin) is a new low-affinity partial benzodiazepine receptor agonist. It shows potent anticonvulsant and anxiolytic properties in rodent models.
Baicalin
T2775CAS 21967-41-9
Baicalin is a prolyl endopeptidase inhibitor isolated from scutellaria baicalensis, with antioxidant, anti-tumor, anti-HIV properties.
Etomidate
T1089CAS 33125-97-2
Etomidate is a GABAA receptor agonist, with a short-acting sedative, hypnotic, and general anesthetic properties.
6-Hydroxyflavone
T2940CAS 6665-83-4
6-Hydroxyflavone is a noncompetitive inhibitors of cytochrome P450 2C9. It is a flavone, a type of chemical compound. It is reported in leaves of Barleria prioni...
Nikethamide
T0048CAS 59-26-7
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 cen...
Bemegrid
T1396CAS 64-65-3
Bemegride is a central nervous system stimulant and antidote for barbiturate poisoning.
Oxiracetam
T1128CAS 62613-82-5
Oxiracetam, a cyclic derivative of gamma-aminobutyric acid (GABA), is utilized for the treatment of cognitive impairments.
Vigabatrin
T0128CAS 60643-86-9
Vigabatrin, an analogue of gamma-aminobutyric acid, is an irreversible inhibitor of 4-aminobutyrate transaminase responsible for the catabolism of γ-aminobutyri...
Gabapentin
T0702CAS 60142-96-3
Gabapentin is an Anti-epileptic Agent. The physiologic effect of gabapentin is by means of Decreased Central Nervous System Disorganized Electrical Activity.
Gabapentin HCl
T6507CAS 60142-95-2
Gabapentin HCl is a GABA analogue, used to treat seizures and neuropathic pain.
Glabridin
T3403CAS 59870-68-7
Glabridin may serve as an anti-inflammatory agent in diabetes-related vascular dysfunction, through regulating the synthesis and activity of iNOS under high-gluc...
4-Aminobutyric acid
T0508CAS 56-12-2
4-Aminobutyric acid is the most common inhibitory neurotransmitter in the central nervous system.
L-Cycloserine
T0710CAS 339-72-0
L-cycloserine irreversibly inhibits GABA pyridoxal 5′-phosphate-dependent aminotransferase in E. coli, as well in the brains of various animals, results in inc...
Pentetrazol
T1413CAS 54-95-5
Pentylenetetrazol is a GABA(A) receptor antagonist, that displays activity as a central nervous system and respiratory stimulant.
Urethane
T0051CAS 51-79-6
Urethane was an antineoplastic agent .Now is used for other medicinal purposes.
Wogonoside
T3318CAS 51059-44-0
Wogonoside acts as a positive allosteric modulator of the benzodiazepine site of the GABAA receptor.
(+)-Bicuculline
T2850CAS 485-49-4
Bicuculline is a light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolated...
(-)-borneol
T3741CAS 464-45-9
(-)-Borneol has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.
Homotaurine
T0883CAS 3687-18-1
Because of its similarity in structure to the neurotransmitter gamma-aminobutyric acid (GABA), it has GABAergic effects and may be useful as an anticonvulsant. H...
ONO-8590580
TQ0040CAS 1802661-73-9
ONO-8590580 is a negative allosteric modulator of GABAA α5.
L-655708
TQ0151CAS 130477-52-0
L-655708 is an effective inverse agonist of the α5 subunit-selective GABAA receptor (Ki: 0.45 nM).
Acetoxyvalerensre
TN6773CAS 81397-67-3
Acetoxyvalerensre (acetylvalerenolic acid) is a derivative of valerenic acid, which is a a GABAA receptor modulator.
Suritozole
T8568CAS 110623-33-1
Suritozole is a negative modulator at the gamma-aminobutyric acidA (GABAA) receptor
Fasoracetam
T19624CAS 110958-19-5
Fasoracetam is a modulator of GABA receptor potentially for the treatment of attention deficit hyperactivity disorder.
Isotanshinone I
T11686CAS 20958-17-2
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 and...
Lotilaner
T15775CAS 1369852-71-0
Lotilaner is a parasiticide. It is used as a potent non-competitive antagonist of insects GABACl receptors (IC50 of 23.84 nM for Drosophila melanogaster GABA rec...
Progabide
T16581CAS 62666-20-0
Progabide is an agonist of the gamma-aminobutyric acid receptor.
Radequinil
T16717CAS 219846-31-8
Radequinil is a benzodiazepine receptor partial inverse agonist. Rade quinil binds to GABA(-) and GABA(+) ligand (Kis: 5.15 and 6.11 nM, respectively).
LAU159
T11822CAS 2055050-87-6
LAU159 is a functionally selective positive α1β3 GABA(A) receptor modulator(EC50 : 2.2 μM).
RO 4938581
T16794CAS 883093-10-5
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, α3...
RWJ-51204
T16811CAS 205701-85-5
RWJ-51204 is a partial agonist of GABA(A) receptor (Ki: 0.2-2 nM).
SCH 50911
T12867LCAS 733717-87-8
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, ...
TPA 023
T17144CAS 252977-51-8
TPA 023 is an agonist of the GABAA α2/α3 subtype-selective (Ki: 0.19-0.41 nM).
Valnoctamide
T17215CAS 4171-13-5
Valnoctamide inhibits benzodiazepine-refractory status epilepticus. Valnoctamide acts directly on GABAA receptors.
Arbaclofen hydrochloride
T17306CAS 63701-55-3
Arbaclofen hydrochloride, a Gamma-Aminobutyric Acid derivative, is a specific agonist of GABA-B receptors, it is used to treat spasticity, especially that due to...
CL 218872
T8572CAS 66548-69-4
CL 218872 is a benzodiazepine agonist displaying selectivity for α1 subunit-containing GABAA receptors (Ki values are 130, 1820, 1530, > 10000, 490 and > 10000 ...
Phenibut (hydrochloride)
T8639CAS 3060-41-1
Phenibut (hydrochloride) is a GABA mimetic that acts as an agonist at GABAB receptors, blocks α2δ subunit-containing voltage-gated calcium channels, stimulate...
Baclofen hydrochloride
T8630CAS 28311-31-1
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, es...
Bamaluzole
T10456CAS 87034-87-5
Bamaluzole is an agonist of GABA receptor extracted from patent WO 2012064642 A1.
Tabernanthine
TN5089CAS 83-94-3
Tabernanthine shows affinity for opiate receptors, it can decrease morphine and cocaine self-administration in rats, it may be effective in treating addiction to...
Etiocholanone
TN6765CAS 53-42-9
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent neurosteroid p...
Etomidate hydrochloride
T21802CAS 53188-20-8
Etomidate hydrochloride is a potent agonist of GABAA receptor. It is a neurological drug and effective parenteral medication and has the potential for management...
Imidazenil
T8971CAS 151271-08-8
Imidazenil is an modulator of GABA-A that blocks the sedative effects without lowering the convulsion threshold.
2'MeO6MF
T8887CAS 89112-85-6
2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors.It offers neuroprotection and improved function...
SSD114 hydrochloride
T8664CAS 2319790-02-6
SSD114 hydrochloride is a GABAB receptor positive allosteric modulator.
Tilifodiolide
TN5147CAS 126724-95-6
Tilifodiolide exerts in vitro and in vivo anti-inflammatory activity and in vivo antinociceptive effects. Tilifodiolide exerted antidiarrheal activity by decreas...
Limonexic acid
TN4440CAS 99026-99-0
Limonexic acid shows antinociceptive actions , it produces dose-related inhibition of glutamate- and capsaicin-induced pain. Limonexic acid can effectively prote...
Sanggenone D
T4S1616CAS 81422-93-7
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-inflamm...
Isopulegol
TN4322CAS 7786-67-6
Isopulegol presents depressant- and anxiolytic-like effects, it also has anticonvulsant and bioprotective effects against PTZ-induced convulsions are possibly re...
Isohyenanchin
TN4298CAS 19417-00-6
Isohyenanchin is the potent antagonist of RDLac homo-oligomers, it is also a weak antagonist of ionotropic GABA receptors.
Dihydroxyaflavinine
TN3868CAS 76410-56-5
Dihydroxyaflavinine is a fungal toxin, it inhibits non-competitively GABAA receptor channel expressed in Xenopus oocytes.Dihydroxyaflavinine shows oral toxicity ...
(-)-Corlumine
TN3702CAS 79082-64-7
Corlumine exhibits spasmolytic and GABA antagonist activity.
Aflatrem
TN3351CAS 70553-75-2
Aflatrem is a tremorgenic mycotoxin with acute neurotoxic effects, a single low dose of aflatrem is able to induce degeneration of neuronal processes in hippocam...
Myristicin
T9113CAS 607-91-0
Myristicin is a natural product found in spices and umbelliferous plants. Myristicin has anti-cholinergic, antibacterial, and hepatoprotective effects, it also ...
Lesogaberan
T15737CAS 344413-67-8
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, t...
GABAB receptor antagonist 1
T11350CAS 797-17-1
(E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.GABAB receptor antagonist 1 is a selective a...
Zuranolone
T7794CAS 1632051-40-1
Zuranolone is an agonist of GABAA receptor.
Kushenol I
TN1842CAS 99119-69-4
Kushenol I is a GABAA receptor modulator, it exhibits inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2).Kushenol I is shown to be activ...
6-(4-Methoxyphenyl)-3-pyridazinamine
T7793CAS 4776-87-8
6-(4-Methoxyphenyl)-3-pyridazinamine is a GABAA receptor antagonist
Gaboxadol (hydrochloride)
T7803CAS 85118-33-8
Gaboxadol (hydrochloride) is a GABAA receptor agonist.
Thujone
T8193CAS 546-80-5
Thujone is an inhibitor of  ACh with an IC50 value of 24.7μM.
6,2'-Dihydroxyflavone
T8268CAS 92439-20-8
6,2'-Dihydroxyflavone is a novel antagonist of GABAA receptor.
6-Methylflavone
T8036CAS 29976-75-8
6-Methylflavone is an activator of α1β2γ2L and α1β2 GABAA receptors.
Cholesterol myristate
T8040CAS 1989-52-2
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic ace...
Securinine
T3S2100CAS 5610-40-2
(-)-Securinine is plant-derived alkaloid and also a GABAA receptor antagonist.
Cannabidivarin
T8162CAS 24274-48-4
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 epilep...
AZD-7325
T7699CAS 942437-37-8
AZD-7325 is a GABA-Aα2,3 -selective receptor modulator.
beta-Amyrin
TN1027CAS 559-70-6
beta-Amyrin has antiviral, hepatoprotective, antinociceptive, anti-inflammatory, it retard acute inflammation in rat model of periodontitis.
Bacopaside I
TN1420CAS 382148-47-2
Bacopaside I is a modulator of Aquaporin-1 channel, has neuroprotective functions, it has anti-Alzheimer's disease, it ameliorates cognitive impairment in APP/PS...
Bacopasaponin C
TN1432CAS 178064-13-6
Bacopasaponin C may have antioxidant activity, it also shows anti-leishmanial property.
DL-Menthol
TN1591CAS 15356-70-4
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 GABA...
Guvacine
TN1717CAS 498-96-4
Guvacine can enhance the inhibition of spinal neurones by GABA.
Tetrahydromagnolol
TN2268CAS 20601-85-8
Tetrahydromagnolol can activate cannabinoid (CB) receptors.
GABAA receptor agent 1
T11349CAS 1571-87-5
GABAA receptor agent 1 has strong anticonvulsant activity and is a high affinity ligand of GABAA receptor.
Emamectin Benzoate
T15212CAS 155569-91-8
Emamectin Benzoate, by binding gamma-aminobutyric acid (GABA) receptor and glutamate-gated chloride channels disrupting nerve signals within arthropods, acts as ...
Fluxametamide
T11307CAS 928783-29-3
Fluxametamide is a novel isoxazoline insecticide that acts via distinctive antagonism of insect ligand-gated chloride channels, acts as an antagonist of GABA- an...
FG 7142
T11277CAS 78538-74-6
FG 7142 also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 can increase tyrosine hydroxylation an...
Etifoxine hydrochloride
T13690CAS 56776-32-0
Etifoxine is an anxiolytic and anticonvulsant drug. Unlike benzodiazepines, etifoxine appears to produce its anxiolytic effects by binding to β2 and β3 subuni...
(E)-GABAB receptor antagonist 1
T11137CAS 1611483-29-4
(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-G...
SCH 50911 hydrochloride
T12867CAS 160415-07-6
SCH 50911 hydrochloride is a selective, orally-active and competitive antagonist of γ-Aminobutyric acid B GABA(B) receptor(IC50 : 1.1 μM).
Gidazepam
T15380CAS 129186-29-4
Gidazepam is an GABA receptor channels agonist.
CP-409092
T10869LCAS 194098-25-4
CP-409092 is a partial GABAA receptor agonist. It has anti-anxiety activity.
(-)-Bicuculline methobromide
T12043CAS 73604-30-5
(-)-Bicuculline methobromide is a potent antagonist of GABAA receptor .
CGP 36742
T14938CAS 123690-78-8
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 usef...
Cenobamate
T10757LCAS 913088-80-9
Cenobamate, a sodium channel blocker, enhances GABAergic transmission. It has a potential to be a versatile CNS drug.
Afoxolaner
T13536CAS 1093861-60-9
Afoxolaner is an isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect GABA and glutamate receptors, inhibiting GABA...
Bifenazate
T14571CAS 149877-41-8
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]...
DMCM hydrochloride
T11061CAS 1215833-62-7
DMCM hydrochloride is a non-selective fully inverse agonist of benzodiazepine. DMCM showed significant differences in human recombinant GABAA zaerxep3 receptor s...
(-)-Bicuculline methochloride
T12044CAS 53552-05-9
(-)-Bicuculline methochloride is a potent antagonist of GABAA receptor.
Valproic acid sodium salt
T1602CAS 1069-66-5
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 blo...