gabaa receptor

GABAA receptor agent 6 (compound 2027) is a potent γ-GABAAR antagonist with low cellular membrane permeability (Ki = 0.56 μM) [1].

GABAA Receptor Agent 5 (compound 018) serves as a potent γ-GABAAR antagonist, possessing a Ki of 0.020 μM. This compound exhibits γ-GABAAR antagonist properties, yet it demonstrates low cellular membrane permeability [1].

GABAA receptor agent 4 (compound 1e) is a potent antagonist of γ-GABAAR with Ki of 0.18 µM. GABAA receptor agent 4 has immunomodulatory potential which was shown to efficiently rescue the inhibition of T cell proliferation [1].

GABAA receptor agent 1 has strong anticonvulsant activity and is a high affinity ligand of GABAA receptor.

GABAA receptor agent 7 (compoud 5c) has anticonvulsant activity both in vitro and in vivo with low neurotoxicity which can be used in epilepsy research. GABAA receptor agent 7 is a potent positive modulator of GABAA receptor [1].

GABAA receptor agent 2 TFA is a potent, high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptor). GABAA receptor agent 2 TFA has no effect on four human GABA transport proteins (hGAT-1, hBGT-1, hGAT-2 and hGAT-3).

GABAA receptor agent 8 (compoud 5e) has the potential in epilepsy research. GABAA receptor agent 8 is a potent positive modulator of GABAA receptor with anticonvulsant activity both in vitro and in vivo as well as low neurotoxicity [1].

GABAA receptor agonist 1 (compound 3e) is a potent agonist of GABAA receptor that binds at the GABA binding site of GABAA receptor to produce GABAergic effects. GABAA receptor agonist 1 has anti-depression activities in classical mouse models of FST and TST depression that has the potential in the research of depression [1].

GABAA receptor agonist 2 (compound 4c) is a highly potent GABAA receptor agonist which exhibits anti-depressive properties in classical mouse models of depression, such as the FST and TST. By binding to the GABA binding site on the GABAA receptor, GABAA receptor agonist 2 produces GABAergic effects. Notably, Compound 4c holds promise for depression research [1].

GABAA receptor modulator-2 (Compound 20) is a selective, orally active α5-GABAAR negative conformation modulator (Ki: 4.1 nM). gABAA receptor modulator-2 exhibits high metabolic stability and a good central nervous system safety profile.

BL-1020 Mesylate (CYP-1020 Mesylate) is an orally available GABA A receptor agonist and D2 antagonist that decreases dopamine activity and enhances GABAA activity.BL-1020 Mesylate has been used in the study of schizophrenia, Alzheimer's disease, and bi-directional cognitive impairment.

Cholesterol Myristate (Cholesteryl Myristate) is a natural steroid found in traditional Chinese medicine that interacts with various ion channels, including the GABAA receptor, nicotinic acetylcholine receptor, and the inward-rectifier potassium ion channel.

3,4,5-Trimethoxycinnamic acid (O-Methylsinapic acid) (TMCA) is one of the constituents of Polygalae Radix and may exert anti-seizure activity by acting at the GABAA/BZ receptor complex.

Acetoxyvalerensre (acetylvalerenolic acid) (acetylvalerenolic acid) is a derivative of valerenic acid, which is a a GABAA receptor modulator.

Suritozole (MDL-26479) is a negative modulator at the gamma-aminobutyric acidA (GABAA) receptor

ELB-139 is a GABAA receptor agonist that can be used to study depression and epilepsy.

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 dampens the stroke-induced inflammatory response. 2'MeO6MF has anxiolytic and sedative effects.

SCS is a GABAA receptor antagonist.

Muscimol HBr (Agarin HBr) is an agonist of GABAA receptor.

Lirequinil (Ro 41-3696) is a small molecule GABAA receptor agonist used to study neurological disorders.

Dipropofol (4,4-Bis(2,6-di-isopropylphenol)) is a small molecule GABAA receptor agonist that can be used to study epilepsy.

4,4-dimethyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-2-one is a benzodiazepine derivative. It is an orthosteric modulator of the GABAA receptor and selectively binds to the benzodiazepine site of the GABAA receptor. It has anxiolytic, anticonvulsant and sedative activity.

Propanidid (Sombrevin) is a gamma-aminobutyric acid type A receptor (GABAA) agonist and a fast-acting intravenous anesthetic that lowers arterial blood pressure.

DMCM hydrochloride is a non-selective fully inverse agonist of benzodiazepine. DMCM showed significant differences in human recombinant GABAA αxβ3γ2 receptor subtypes. For α1, α2, α3, and α5 receptors, their Kis were 10 nM, 13 nM, 7.5 nM, 2.2 nM, respectively.

Broflanilide is metabolized to desmethyl-broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin GABA receptor and inhibits S. litura RDL GABAR (IC50: 1.3 nM).

Glabridin (KB-289522) 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 possess a therapeutic effect on metabolic disorders( such as diabetes and hyperglycemia), by modulating glucose metabolism through AMPK in skeletal muscle cells. Glabridin may have potential as a chemopreventive agent against liver Y metastasis, by inhibiting the invasion of human HCC cells.

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 cucullaria, Adlumia fungosa, Fumariaceae, and several Corydalis species.

Urethane (Ethylurethane) was an antineoplastic agent .Now is used for other medicinal purposes.

Rosmanol has antioxidant activity, it can activate the antioxidant response element. Rosmanol has biphasic modulation of GABAA receptors, demonstrates CNS activity in mouse models of antinociception, antidepressant and anxiolysis. Rosmanol potently induce

Flumazenil (Ro 15-1788) antagonizes the benzodiazepine binding site of the gamma-aminobutyric acid (GABA)/benzodiazepine receptor complex in the central nervous system (CNS), thereby preventing the chloride channel opening events and inhibiting neuronal hyperpolarization. As a result, flumazenil reverses benzodiazepine-induced effects including sedation, psychomotor deficits, amnesia, and hypoventilation in a dose-dependent manner. Flumazenil is an imidazobenzodiazepine derivative, effective in reversing benzodiazepine-induced activities.

Loreclezole is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit-containing receptors.

Cipepofol (HSK3486) is a GABAA receptor agonist with sedative properties and protective effects in a variety of cardiovascular diseases.Cipepofol activates the Sirtuin1 (Sirt1)/Nrf2 pathway and induces apoptosis in cardiomyocytes, and can be used to study myocardial infarction, myocardial ischemia/reperfusion injury, and octopus pot syndrome.

MIDD0301 is a potent positive allosteric α5β3γ selective GABAA receptor (GABAAR) ligand with EC50 of 17 nM.

Pivagabine (CXB-722), a hydrophobic 4-aminobutyric acid derivative, exhibits neuromodulatory activity and successfully penetrates the blood-brain barrier in rats. It counteracts the impact of foot shock on GABAA receptor function and corticotropin-releasing factor (CRF) levels in the rat brain.

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- currents with little effect on peak amplitude. Also inhibits 5-HT3A receptors via a similar mechanism.

Withasomniferolide A, a withanolide extracted from the roots of Withania somnifera, has been identified as a positive activator of the GABAA receptor, isolated using a methanol extract [1].

Pregnanolone is a cell membrane modulator potentially for the treatment of pain. Pregnanolone is an endogenous neurosteroid that is biosynthesized from progesterone. It is a positive allosteric modulator of the GABAA receptor, as well as a negative allost

FG 7142 (LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex. FG 7142 , a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM).

Songorine (Napellonine) shows favorable anti-tumor activity in preliminary pharmacological verification trials including cell proliferation and molecular docking assays.

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 neurotransmitter systems. Aflatrem potentiates the gamma-aminobutyric acid (GABA)-induced

K1 peptide TFA exhibits high affinity as a ligand for the GABAA receptor-associated protein (GABARAP) [1].

6-(4-Methoxyphenyl)-3-pyridazinamine is a GABAA receptor antagonist

Isonipecotic acid (4-Piperidinecarboxylic acid) is a heterocyclic compound. Isonipecotic acid mainly characterized as a GABAA receptor partial agonist.

Etifoxine hydrochloride (HOE 36-801 hydrochloride) is an anxiolytic and anticonvulsant drug. Unlike benzodiazepines, Etifoxine hydrochloride appears to produce its anxiolytic effects by binding to β2 and β3 subunits of the GABAA receptor complex, and so is acting at a different target site to benzodiazepines, although the physiological effect that is produced is similar to that of benzodiazepines.

ABP-700 is a positive allosteric modulator of the GABAA receptor.

U-101017 is a partial benzodiazepine receptor and GABAA receptor agonist.

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 (Kis) is 5.1 nM and 1.4 μM, respectively.

CP-409092 hydrochloride is a partial agonist of the GABAA receptor with anti-anxiety activity.

GABAA receptor agonist

CP-457920 is a selective α 5 GABAA receptor agonist for the treatment of dementia in Alzheimer's disease.