GABA Receptor

RWJ-51204: potent adenosine A2A blocker, GABA(A) partial agonist (IC50: 0.2-2 nM), neuroprotective, may treat Parkinson's.

Riluzole hydrochloride, an anticonvulsant Na+ channel blocker, inhibits GABA uptake (IC50: 43 µM).

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

BPDBA is an effective, selective, and non-competitive inhibitor of the betaine/GABA transporter (BGT-1), displaying inhibitory activity against human BGT-1 and

ELB-139 is a GABA A receptor agonist. ELB139 increases 5-HT in the striatum and prefrontal cortex of rats.

NNC 05-711 (NO-711 hydrochloride) is a potent and selective inhibitor of GAT-1 (GABA transporter 1), exerting anticonvulsant and analgesic effects.

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

Alpidem (Ananxyl), a non-sedative imidazopyridine anxiolytic, treats anxiety with high benzodiazepine receptor affinity.

DMCM hydrochloride is a non-selective fully inverse agonist of benzodiazepine.

NNC 05-2090 HCl: BGT-1 inhibitor, IC50 = 10.6 μM, potential for epilepsy, neurological research.

CGP 54626 hydrochloride is a GABAB receptor antagonist.

Piperidine-4-sulfonic acid is a potent GABA agonist, demonstrating an IC50 value of 0.034 μM for the inhibition of H-GABA binding [1].

RPC425 is a noncompetitive inhibitors of the Betaine-γ-Aminobutyric Acid Transporter 1 (BGT1).

Org-21465, a gamma-aminobutyric acid (GABA) receptor agonist, is used potentially for the use of anesthesia.

L-822179 (α5IA) is a selective inverse agonist for the Α5 subtype of GABAA receptor with higher intrinsic activity at the A5 subtype than other drugs.

GABAA antagonist

FGIN-1-27 is a high-affinity agonist of the translocator protein and a specific peripheral benzodiazepine receptor (PBR) ligand(Ki = 5.0 nM).

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

GMA-839 is a selective modulator of gamma-aminobutyric acid(A) receptors.

U 89843A is a positive allosteric modulator of gamma-aminobutyric acid (GABA)A receptors.

(+)-Bicuculline methiodide is a GABAA receptor blocker that blocks epileptogens and may be used in the study of neurological disorders.

CP-409092 is a partial GABAA receptor agonist. It has anti-anxiety activity.

mGAT3/4-IN-2 are potent inhibitors of mGAT3/mGAT4 with their pIC50 values of 5.44 and 5.25, respectively.

COR659: suppresses alcohol/chocolate intake in rats; enhances GABAB receptor, blocks CB1 receptor.

Diproqualone, analogous to methaqualone, exhibits sedative, anxiolytic, anti-inflammatory, and analgesic properties [1].

ADX71441, a GABAB PAM, lengthens urinary latencies, lessens events & volume, and may aid in alcoholism and bladder pain.

Adipiplon(NG2-73, NG273) is a novel selective gamma-aminobutyric acid (GABA) partial agonist.

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

CGP 64213 is a GABAb receptor agonist.

CGP55845 hydrochloride is a potent and selective GABAB receptor antagonist with an IC 50 of 6 nM which can be used in neurological research [1] [2].

(-)-Bicuculline methochloride is a potent antagonist of GABAA receptor.

Potent GABAA antagonist; IC50: 24 nM (α1β2γ2), Ki: 28 nM (rat); inactive on human GABA transporters.

JM-1232 is a sedative and hypnotic drug being researched as a potential anesthetic.

CGP-54626 is a selective antagonist of the GABAB receptor (IC50 = 4 nM ).

Afizagabar, a first-in-class α5-GABAAR antagonist, IC50: 585 nM, Ki: 66 nM, may boost memory.

mGAT-IN-1 is a potent, non-selective GAT inhibitor that inhibits mGAT3 activity well (IC50: 2.5 μM, pIC50: 5.61).

L 663581 is the benzodiazepine receptor partial agonist.

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

NCS-382 (sodium) is a potent antagonist of the GABA receptor, exhibiting anti-sedative and anti-hypnotic properties, with applications in neurological disease

SCS is a GABAA receptor antagonist.

CGP 55845: potent, selective GABAB blocker, IC50=5 nM, hinders agonist binding, reduces GABA/glutamate release.

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

GABA-IN-2 (Compound 5), a GABA inhibitor, exhibits both larvicidal and insecticidal properties, achieving an 87% mortality rate at a concentration of 50 mg/L [1

(R)-4-Amino-3-hydroxybutyric acid, also known as (R)-GABOB, acts as a modulator of GABA receptors, specifically binding to both GABAA and GABAB receptors and blocking GABA reuptake in rat brain synaptosomes. Additionally, it serves as a GABAC receptor agonist, triggering currents in patch-clamp assays with Xenopus oocytes that express the human receptor. In vivo studies reveal its capability to suppress electrical discharges in the amygdala in cats undergoing N-amidinobenzamide-triggered seizures, indicating its potential therapeutic application in managing seizure disorders.

Tuclazepam (KC 1956) is a derivative of the benzodiazepine class of drugs, exhibiting anti-anxiety and sedative properties.

5α-Androstan-3α-ol is a γ-aminobutyric acid (GABA) receptor agonist. It inhibits the transcriptional activity of the orphan nuclear receptor CAR (constitutive androstane receptor). By binding to CAR and promoting its dissociation from coactivator proteins, 5α-Androstan-3α-ol negatively regulates CAR's activity. This compound is useful for studying hormone metabolism and drug detoxification mechanisms mediated by nuclear receptors.

Refisolone is an antagonist of the GABAA receptor.

Compound 3e, a potent GABAA agonist, targets GABA sites and has potential anti-depressive effects in mice.

β-CCM is a benzodiazepine receptor inverse agonist with anxiogenic and convulsant effects. It enhances emotional reactivity and reduces interference sensitivity in spatial working memory tasks. β-CCM is applicable in research related to anxiety disorders.

EF1502 is a potent and selective GABA transporter inhibitor.