gabaa

GABAA receptor agent 1 has strong anticonvulsant activity and is a high affinity ligand of 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, exhibiting a Ki of 0.18 µM, and demonstrates immunomodulatory potential by effectively rescuing the inhibition of T cell proliferation [1].

GABAA receptor agent 7 (compound 5c) is a potent positive modulator of the GABAA receptor with anticonvulsant activity in vitro and in vivo, and low neurotoxicity, making it suitable for epilepsy research [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 (compound 5e) is a potent positive modulator of the GABAA receptor, exhibiting anticonvulsant activity in both in vitro and in vivo studies, with low neurotoxicity, indicating its potential in epilepsy research [1].

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

GABAA receptor agonist 2 (compound 4c) is a highly potent compound that 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, it 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) that exhibits high metabolic stability and a good central nervous system safety profile.

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.

Clomethiazole (Distraneurin) is an orally active GABAA agonist and it is an anticonvulsant agent. It also has the potential for treating convulsive status epilepticus. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes.

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.

SCS is a GABAA receptor antagonist.

γ-Aminobutyric acid (4-Aminobutyric acid) is the predominant inhibitory neurotransmitter in the central nervous system.

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.

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

1. Pulegone ((+)-Pulegone) has cytotoxicity followed by regenerative cell proliferation is the MOA for Pulegone-induced urothelial tumors in female rats. 2. Pulegone induces a verapamil-sensitive psychostimulant effect that appears to independ on the opening of L-type calcium channels. 3. Pulegone has negative reinforcing properties and seems to possess anxiolytic-like actions unrelated to the benzodiazepine site of the γ-aminobutyric acid type A (GABAA) receptor.

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.

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.

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

DL-Menthol ((±)-Menthol) is a racemic mixture of the monoterpene alcohols (–)-menthol and (+)-menthod, which have been found in Cannabis. (–)-Menthol is more common than (+)-menthol in nature and exhibits analgesic, antibacterial, and anticancer properties, as well as inhibits cholinesterase.2 (+)-Menthol inhibits the growth of F. verticillioides (MIC: 1.5 mM) but, unlike (–)-menthol, does not exhibit analgesic, antibacterial, anticancer, or cholinesterase inhibitory activities.

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

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

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

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.

Pazinaclone is a non-benzodiazepine (GABAA) partial agonist with sedative and anxiolytic activity.

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

2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. It offers neuroprotection, improves functional recovery, and dampens the stroke-induced inflammatory response. 2'MeO6MF also has anxiolytic and sedative effects.

Anxiolytic/nonsedative agent-1 (TCS 1205) is a potent and selective GABAA agonist. Anxiolytic/nonsedative agent-1 shows appreciable affinity for the BzR in bovine brain membranes with Kis of 14, 121, 239 nM for α1β2γ2, α2β2γ2, α5β3γ2, respectively. Anxiolytic/nonsedative agent-1 shows α2 selective efficacy in vitro and anxioselective effects in vivo.

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

Lirequinil (Ro 41-3696) is a small molecule GABAA receptor agonist utilized in the study of neurological disorders.

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.

RWJ-51204 is a selective adenosine A2A receptor antagonist and a partial agonist of GABA(A) receptor (IC50: 0.2-2 nM). It has neuroprotective and movement-improving effects and can be used in research related to Parkinson's disease.

PZ-II-029 is a modulator of α6β3γ2-selective GABAA channel.

Positive allosteric modulator of GABAA receptors

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.

Darigabat (PF-06372865) is an orally active and selective GABAA receptor modulator that crosses the blood-brain barrier and exhibits anxiolytic activity, with Ki values of 2.9 nM, 21 nM, and 134 nM for α2, α1 PAM, and α2 PAM, respectively.Darigabat is used in the study of anxiety disorders and epilepsy.

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).

Alpidem (Ananxyl) is an anxiolytic drug from the imidazopyridine family. Alpidem does not produce sedative effects at normal doses, and is instead used specifically for the treatment of anxiety. Alpidem has nanomolar binding affinity for both the central benzodiaze

Lopirazepam is a potent small molecule GABAA receptor agonist, which can be used to treat anxiety disorders, insomnia, epilepsy and other diseases.

Bicuculline ((+)-Bicuculline) is a light-sensitive competitive antagonist of GABAA receptors, originally identified in 1932 from plant alkaloid extracts, and isolated from Dicentra cucullaria, Adlumia fungosa, Fumariaceae, and various Corydalis species.

Eudesmin shows antiinflammatory, neuritogenic, anticonvulsant and sedative effects, the mechanism of eudesmin may be related to up-regulation of GABAA and GAD65 expressions, and anti-apoptosis of neuron the in brain.50 microM (+)-eudesmin can induce neurite outgrowth and enhance nerve growth factor (NGF)-mediated neurite outgrowth from PC12 cells by stimulating up-stream MAPK, PKC and PKA pathways.

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

Valepotriate (Valtrate) fraction can have sedative effects and affect behavioral parameters related to recognition memory. Valepotriates, a new class of cytotoxic and antitumor agents, they are very potent cytotoxic agents for the HTC hepatoma cells. Valepotriates may have a potential anxiolytic effect on the psychic symptoms of anxiety.

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, α3, α4, α5 and α6-subunit containing receptors respectively). Orally active anxi

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

(-)-Securinine (Securinine) is plant-derived alkaloid and also a GABAA receptor antagonist.

(+)-Kavain ((R)-KAWAIN) is one of the six major kavalactones found in the Piper methysticum (kava) plant; reversible inhibitor of MAO-B.