GABA Receptor

Lotilaner is a parasiticide. It is used as a potent non-competitive antagonist of insects GABACl receptors (IC50 of 23.84 nM for Drosophila melanogaster GABA receptor). It also has no effect on a dog GABAA receptor.

E2730 is a selective and noncompetitive inhibitor of the gamma-aminobutyric acid (GABA) transporter 1 (GAT1) that exhibits oral availability as well as antiepileptic properties. Its inhibition of GAT1 is dependent on the prevailing GABA concentrations and specifically targets GAT1-mediated GABA uptake. Demonstrating in vivo effectiveness, E2730 has been tested at doses ranging from 5-50 mg kg orally in various models, including the rat amygdala kindling and the mouse corneal kindling models, as well as in drug-resistant psychomotor epilepsy, fragile X syndrome at 2.5-300 mg kg, and Dravet syndrome at dosages of 10 mg kg and 20 mg kg [1].

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).

Losigamone (AO-33), an agonist of the GABA receptor, can be utilized in studies on the treatment of partial seizures.

CGP 35348 is a selective antagonist of GABAB receptor (EC50 = 34 μM). CGP 35348 can be used in studies of neuromuscular coordination and spatial learning after neonatal brain damage in albino mice.

Apalutamide (ARN-509) is a small molecule androgen receptor (AR) antagonist with potential antineoplastic activity.

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that inhibits HDAC1 activity, induces HDAC2 degradation, and is orally active. Valproic Acid can be used in epilepsy and bipolar disorder research.

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.

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

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

Dihydromyricetin (Ampelopsin) is a natural antioxidant flavonoid from Ampelopsis grossedentata. Dihydromyricetin is a potent inhibitor of dihydropyrimidinase with an IC50 of 48 μM. Dihydromyricetin can activate autophagy by inhibiting mTOR signaling.

Pentylenetetrazol is a GABA(A) receptor antagonist, that displays activity as a central nervous system and respiratory stimulant.

Miltirone is a CYPs inhibitor, it has been characterized as a low-affinity ligand for central benzodiazepine receptors.

TPA 023 is a selective agonist of GABAA α2 α3 subtype (Kis = 0.19 - 0.41 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.

(R)-baclofen (STX209), a derivative of gamma-aminobutyric acid, is commonly utilized for the treatment of spasticity.

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

6,2'-Dihydroxyflavone is a novel antagonist of the GABAA receptor.

Afoxolaner is an isoxazoline insecticide acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect GABA and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.

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.

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.

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.

Fluralaner (A1443) is an isoxazoline ectoparasiticide. It potently and selectively inhibits binding of the GABA receptor channel blocker EBOB to housefly head membranes (IC50: 455 pM).

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.

α-Thujone is an inhibitor of ACh with an IC50 value of 24.7μM.

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.

Lorediplon is a novel hypnotic drug acting as a GABAA receptor modulator, differentially active at the α1-subunit, associated with promoting sleep.

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

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

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.

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).

Zuranolone is an agonist of GABAA receptor.

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

Jujuboside A, a glycoside extracted from Semen Ziziphi Spinosae, exhibits neurophysiological inhibitory effects and is considered a potential therapeutic agent for the treatment of Alzheimer’s disease.

Furosemide sodium (Frusemide Sodium) is a potent and orally active inhibitor of Na+ K+ 2Cl- (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide sodium is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.

Methionine (D-Methionine) (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.

NNC 05-2090 hydrochloride is a betaine GABA transporter (BGT-1) inhibitor with an IC50 value of 10.6 μM.NNC 05-2090 hydrochloride can be used for the study of epilepsy and neurological disorders.

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

Picrotoxinin is a blocker of chloride channel and a noncompetitive antagonist of GABAA with an IC50 of 1.15 μM for α1β2γ2L GABAA. Picrotoxinin shows convulsant properties.

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

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

Riluzole (RP-54274) is a glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.

Basmisanil (RG1662) is a negative allosteric modulator inverse agonist of GABAAα5 receptors.Formulations containing basmisanil are in clinical trials for the treatment of cognitive impairments associated with Down syndrome.

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.

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.

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.

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