GABA Receptor

Saripidem (SL-85.0274) is a compound with anxiolytic activity.

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

Golexanolone can be used to study neurological diseases.

NS-2710, a GABA receptor agonist, is used potentially for the treatment of anxiety.

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

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

Progabide (SL 76002) is an agonist of the gamma-aminobutyric acid receptor.

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

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

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

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

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

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

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

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

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

GABAA antagonist

SCS is a GABAA receptor antagonist.

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

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.

CGP 54626 hydrochloride is a GABAB receptor antagonist.

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

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

CGP 64213 is a GABAb receptor agonist.

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

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].

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

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.

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

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

CGP36216 hydrochloride acts as a selective antagonist at the presynaptic GABA receptor, specifically binding to the GABAB receptor with a Ki value of 0.3 μM. This compound is leveraged in research focused on anxiety and trauma-related disorders [1] [2].

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

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

(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.

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

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

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

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

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

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].

Cyproflanilide is a GABAR antagonist that exhibits high activity against a variety of pests, including those from the Lepidoptera, Coleoptera, and Thysanoptera orders.

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.

Moxetomidate is a GABAA receptor (GABAA receptor) agonist with hypnotic properties.

BGT1-IN-1 (compound 9) is an effective inhibitor of BGT1, demonstrating IC50 values of 13.9 µM for hBGT1 and 58.3 µM for GAT3. It exhibits no cytotoxic effects and possesses neuroprotective activity.

CGS-9895 is a GABA antagonist that operates by interacting with the benzodiazepine binding site on GABA receptors containing the γ subunit (ag).