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. |