GABA Receptor

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 countermeasure against tranquilizer overtreatments, before the advent of end

Valproic acid sodium salt (Sodium Valproate) is the sodium salt form of valproic acid with anti-epileptic activity. Valproic acid sodium salt is converted into its active form, valproate ion, in blood. Although the mechanism of action remains to be elucidated, Valproic acid sodium salt increases concentrations of gamma-aminobutyric acid (GABA) in the brain, probably due to inhibition of the enzymes responsible for the catabolism of GABA. This potentiates the synaptic actions of GABA. Valproic acid sodium salt may also affect potassium channels, thereby creating a direct membrane-stabilizing effect.

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.

(+)-BORNEOL (d-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.

Halothane (Anestan) is a nonflammable, halogenated, hydrocarbon anesthetic that provides relatively rapid induction with little or no excitement. Analgesia may not be adequate. NITROUS OXIDE is often given concomitantly. Because halothane may not produce sufficient muscle relaxation, supplemental neuromuscular blocking agents may be required.

6-Methoxyflavanone (6-MeOF) is A positive allosteric modulator of the GABA response of human recombinant GABA A receptor, with antianxiety and anti-inflammatory activity, and can be used to reduce cisplatin induced neuropathic pain.

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.

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.

γ-Acetylenic GABA hydrochloride is a GABA transaminase inhibitor.

Penicillin G sodium(Benzylpenicillin sodium) salt 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 gram-positive bacteria and against gram-negative cocci. It has also been used as an experimental convulsant because of its actions on GAMMA-AMINOBUTYRIC ACID mediated synaptic transmission.

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.

Sarmazenil (Ro 15-3505) is a partial inverse agonist at the benzodiazepine receptor with pro-convulsant properties and is used in the study of chronic hepatic encephalopathy (HE).

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

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.

Nerisopam is an agonist of gamma-aminobutyric acid (GABA) receptor.

NS-2710 is a non-selective GABA(A) receptor partial agonist for the study of anxiety disorders.

Ru-32514 is a benzodiazepine receptor agonist that partially reverses stress-induced arousal in mice and is used in the study of neurological disorders.

SCS is a GABAA receptor antagonist.

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

6,7-Dimethylisatin (6,7-dimethyl-1H-indole-2,3-dione) inhibits hGAT3 with IC50 of 108 μM. 6,7-Dimethylisatin also inhibits hBGT1, hGAT2.

Fengabine (SL-79229) is a GABA receptor agonist with antidepressant activity and is used to treat depression.

Suriclone (RP 31264) is a selective cyclic pyrrolidone analog with sedative and anxiolytic activity, but not significant sedative effects.Suriclone shows its effects by modulating GABA-A receptors.

Panadiplon (FG 10571) is a selective gamma-aminobutyric acid receptor agonist and partial agonist of 5GABAA, a benzodiazepine receptor, used in the treatment of anxiety disorders.Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors.

Golexanolone (Golexanolona) is a novel GABA-A receptor-modulating steroid antagonist that reduces peripheral inflammation and neuroinflammation and improves cognitive and motor function in rats with chronic hyperammonemia, and may be used to study hepatic encephalopathy.

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

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.

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.

Imidazenil is an modulator of GABA-A that blocks the sedative effects without lowering the convulsion threshold.

Homocarnosine acetate is a dipeptide unique to brain consisting of γ-aminobutyric acid (GABA) and histidine. Homocarnosine acetate has antioxidant and anti-inflammatory actions, prevention of DNA damage, and inhibition of advanced glycation end-product formation

AZD 3043 (THRX 918661) is a variant modulator of the γ-aminobutyric acid type A receptor, a novel sedative-hypnotic and a potential short-acting anesthetic that produces hypnosis and EEG suppression in rats.AZD 3043 potentiates the γ-aminobutyric acid type A receptor and inhibits neuronal nicotinic acetylcholine receptors.

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.

Chlorothymol (AI3-00120) is a disinfectant used in oral.

T-2000 (DMMDPB) is a GABA receptor agonist that can be used to study myoclonus and essential tremor.

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

Baclofen hydrochloride (4-amino-3-(4-chlorophenyl)butanoic acid hydron chloride) 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 to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.

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

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.

6-Hydroxyflavanone, extracted from the leaves of Acorus calamus, exhibits anti-inflammatory and anti-neuropathic pain activity by targeting cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), as well as opioid and GABA-A receptors. 6-Hydroxyflavanone has anti-injury sensory properties in a streptozotocin-induced diabetic neuropathy model. in a streptozotocin-induced diabetic neuropathy model with anti-injury sensory properties.

Divaplon is a GABA receptor agonist (IC50: 0.056 µM) that displays non-sedating anxiolytic behavioral characteristics in a rat model of anxiety.

Losigamone (AO-33) is an agonist of GABA receptor and can be used in studies about the treatment of partial seizures.

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

NO-711ME (N-O711 Methyl ester) is a prodrug of NO-711. It also is a potent and selective GABA uptake inhibitor.

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.

BPDBA is an effective, selective, and non-competitive inhibitor of the betaine/GABA transporter (BGT-1), displaying inhibitory activity against human BGT-1 and mouse GAT2, with IC50 values of 20 μM and 35 μM, 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).

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

(E)-GABAB receptor antagonist 1 is a trans-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 allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.

Baicalin (Baicalein 7-O-β-D-glucuronide) is a prolyl endopeptidase inhibitor isolated from scutellaria baicalensis, with antioxidant, anti-tumor, anti-HIV properties.