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GABA Receptor
T0024 Primidone Primidone is an anticonvulsant of the pyrimidinedione class.
T0028 4-Amino-3-hydroxybutyric Acid 4-Amino-3-Hydroxybutanoic Acid is used as a chiral reagent in the synthesis of antiepileptic and hypotensive drug GABOB and analogues. Also used in the preparation of HIV-1 inhibit
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 century as a medical c
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-aminobutyric acid. Off-label u
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 transaminase.
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 convulsions.
T0508 4-Aminobutyric acid 4-Aminobutyric acid is the most common inhibitory neurotransmitter in the central nervous system.
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 hepatic injury and large
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. Homotaurine has also
T0954 Anestan Halothane is a nonflammable, halogenated, hydrocarbon anesthetic that provides relatively rapid induction with little or no excitement. Analgesia may not be adequate. NITROUS OXIDE
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 effective against most
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 acts as a gamma-aminob
T1089 Etomidate Etomidate is a GABAA receptor agonist, with a short-acting sedative, hypnotic, and general anesthetic properties.
T1128 Oxiracetam Oxiracetam, a cyclic derivative of gamma-aminobutyric acid (GABA), is utilized for the treatment of cognitive impairments.
T1240 Flumazenil Flumazenil antagonizes the benzodiazepine binding site of the gamma-aminobutyric acid (GABA)/benzodiazepine receptor complex in the central nervous system (CNS), thereby preventing
T1300 Propofol Propofol is an intravenous anesthetic agent used for induction and maintenance of general anesthesia.
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.
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 blood. Although the me
T1673 Acamprosate calcium Acamprosate calcium is a GABA receptor agonist and modulator of glutamatergic systems, used for treating alcohol dependence.
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.
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) > α(1) at GABA(A) al
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 nervous system by
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 inflammatory and immun
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 isolated from Dicentra cucu
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 48 μM. Dihydromyri
T3318 Wogonoside Wogonoside acts as a positive allosteric modulator of the benzodiazepine site of the GABAA receptor.
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 GABA-induced Cl- cur
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% respectively). It exhibits anx
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 acid (GABA) reuptake i
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: 7.8 μM).1 This comp
T4363 CGP 52432 CGP52432 is a very potent antagonist of GABAB receptors (IC50 = 85 nM).
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 carcinogenic potential of
T7064 Valproic Acid Valproic Acid is a branched chain fatty acid which potentially enhances central GABAergic neurotransmission and inhibits Na+ channels. Currently, the various molecular mechanisms o
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 from 40 to 400 μM.
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 that is not closely
T4655 Pipequaline Pipequaline is an anticonflict & anticonvulsant quinoline derivative. It is an anxiolytic drug that was never marketed. It possesses a novel chemical structure that is not closely
T4682 Allopregnanolone Allopregnanolone is under investigation for the treatment of Super-Refractory Status Epilepticus.Allopregnanolone has been investigated for the treatment of Severe Postpartum Depre
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 methaqualone. It has
T5330 Fluralaner Fluralaner is an isoxazoline ectoparasiticide. It potently and selectively inhibits binding of the GABA receptor channel blocker EBOB to housefly head membranes (IC50: 455 pM).
T5375 Loreclezole Loreclezole is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit-containing receptors.
T0702 Gabapentin Gabapentin is an Anti-epileptic Agent. The physiologic effect of gabapentin is by means of Decreased Central Nervous System Disorganized Electrical Activity.
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 glycine and GABA r
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 248 μM.
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 of cognitive impairm
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)
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 anticonvulsant effec
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.
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).
T7794 Zuranolone Zuranolone is an agonist of GABAA receptor.
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.
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-glucose levels; may pos
T0349 Riluzole Riluzole is a glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.
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 acetylcholine receptor
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 epilepsy.
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.
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 GABAA receptors, and of
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 active against the plant
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/PS1 mice via immune-m
TN1432 Bacopasaponin C Bacopasaponin C may have antioxidant activity, it also shows anti-leishmanial property.
TN2268 Tetrahydromagnolol Tetrahydromagnolol can activate cannabinoid (CB) receptors.
T12043 (-)-Bicuculline methobromide (-)-Bicuculline methobromide is a potent antagonist of GABAA receptor .
T12044 (-)-Bicuculline methochloride (-)-Bicuculline methochloride is a potent antagonist of GABAA receptor.
T11061 DMCM hydrochloride DMCM hydrochloride is a non-selective fully inverse agonist of benzodiazepine. DMCM showed significant differences in human recombinant GABAA zaerxep3 receptor subtypes. For sp1, s
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].
T10757L Cenobamate Cenobamate, a sodium channel blocker, enhances GABAergic transmission. It has a potential to be a versatile CNS drug.
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 useful in the treatment
T10869L CP-409092 CP-409092 is a partial GABAA receptor agonist. It has anti-anxiety activity.
T15212 Emamectin Benzoate Emamectin Benzoate, by binding gamma-aminobutyric acid (GABA) receptor and glutamate-gated chloride channels disrupting nerve signals within arthropods, acts as a chloride channel
T15380 Gidazepam Gidazepam is an GABA receptor channels agonist.
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).
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-GABAB receptor antag
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 and cause upregulatio
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 and negative alloste
T10456 Bamaluzole Bamaluzole is an agonist of GABA receptor extracted from patent WO 2012064642 A1.
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, the binding affinity
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 formation of AGE,
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).
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, α3β3γ2a (Ki, 174, 1
T16811 RWJ-51204 RWJ-51204 is a partial agonist of GABA(A) receptor (Ki: 0.2-2 nM).
T11822 LAU159 LAU159 is a functionally selective positive α1β3 GABA(A) receptor modulator(EC50 : 2.2 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, binds to GABA(B) re
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 spinal cord damage
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 nM for α1, α2, α
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, stimulates dopamine receptor
T8568 Suritozole Suritozole is a negative modulator at the gamma-aminobutyric acidA (GABAA) receptor
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, especially that due t
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-inflammatory activity, it
T9113 Myristicin Myristicin is a natural product found in spices and umbelliferous plants. Myristicin has anti-cholinergic, antibacterial, and hepatoprotective effects, it also has anti-inflammato
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 hippocampal neurotransmitte
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 to the fall armywor
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 related to positive m
TN4440 Limonexic acid Limonexic acid shows antinociceptive actions , it produces dose-related inhibition of glutamate- and capsaicin-induced pain. Limonexic acid can effectively protect hepatocyte again
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 opioid and stimula
TN5147 Tilifodiolide Tilifodiolide exerts in vitro and in vivo anti-inflammatory activity and in vivo antinociceptive effects. Tilifodiolide exerted antidiarrheal activity by decreasing the intestinal
T8664 SSD114 hydrochloride SSD114 hydrochloride is a GABAB receptor positive allosteric modulator.
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 subunits of the GABAA rec
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- and glutamate-gated c
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 increased levels of ga
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.
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 prionitis Linn. (a common
T11349 GABAA receptor agent 1 GABAA receptor agent 1 has strong anticonvulsant activity and is a high affinity ligand of GABAA receptor.
TMS0418 Dihydroergotoxine mesylate It is mainly used to improve symptoms and physical symptoms of mental degeneration related to aging.
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 functional recovery and dam
T7595 L-DAB HBR L-DAB HBR is an inhibitor of GABA transaminase  (IC50 > 500 μM).
T3741 (-)-borneol (-)-Borneol has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.
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