GABA Receptor

Suriclone (RP 31264), a cyclic pyrrolidone for anxiety, modulates GABA-A receptors without major sedation.

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

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

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

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

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

Panadiplon (FG 10571) is a selective gamma-aminobutyric acid receptor agonist and partial agonist of 5GABAA, a benzodiazepine receptor, used in the treatment of

(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.

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

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

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

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

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

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.

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].

CGP 64213 is a GABAb receptor agonist.

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

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.

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].

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

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

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].

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

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

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

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

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

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

L 663581 is the benzodiazepine receptor partial agonist.

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

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.

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

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.

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

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.

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

benzodiazepine receptor antagonist,competitive

Fletazepam, a benzodiazepine derivative, exhibits sedative, anti-anxiety, and muscle-relaxant properties. It is utilized in neurological research.

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

Compound 4c, a potent GABAA agonist with anti-depressive effects in mouse FST/TST, shows promise in depression research.

SGE516: neuroactive steroid, enhances GABAA, lowers neuronal activity, protects from seizures.

GABA-IN-4 (Compound 17) is a derivative of N-(indol-3-ylglyoxylyl)benzylamine. It exhibits high affinity for the benzodiazepine receptor (BzR), the binding site within the GABAA receptor complex, with a Ki value of 67 nM. Benzodiazepines are widely used as anxiolytic, sedative-hypnotic, and anticonvulsant agents.

EF1502 is a potent and selective GABA transporter inhibitor.

Thiomuscimol hydrobromide is an agonist of GABAA receptor.

Gabaculine, an irreversible GABA-T inhibitor (Ki: 2.9 μM), impacts plastid development and affects DPOR/GluTR levels.

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

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

Refisolone is an antagonist of the GABAA receptor.

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.

S-8510 phosphate is an agonist of inverse Benzodiazepine (BDZ) receptor(Kis of 34.6 nM, 36.2 nM for –GABA and +GABA respectively).

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

2-AEMP TFA is a potent and rapidly acting antagonist of GABA(A)-ρ1 receptors. 2-AEMP is an analog of GABA.

Alfadolone acetate is a gamma-aminobutyric acid (GABA) receptor agonist.

3-Methylglutaconic acid, a primary metabolite accumulating in 3-Methylglutaconic aciduria (MGTA), induces lipid and protein oxidation, while diminishing non-enzymatic antioxidant defenses in cerebral cortex supernatants, thereby promoting oxidative stress in the cerebral cortex. This compound is utilized in research concerning brain damage diseases [1].

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

CGP 44532 a GABAB receptor agonist.

Pipequaline (PK-8165) is an anticonflict & anticonvulsant quinoline derivative. It is an anxiolytic drug that was never marketed. It possesses a novel chemical structure that is not closely related to other drugs of this type. The drug has a similar pharmacological profile to the benzodiazepine family of drugs, but with mainly anxiolytic properties and very little sedative, amnestic or anticonvulsant effects, and so is classified as a nonbenzodiazepine anxiolytic.

CGP 56999A is a GABA(B) receptor antagonist; it boosts BDNF and reduces dopamine loss in rat striatum.