GABA Receptor

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

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

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

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

<p>CP-409092 is a partial GABAA receptor agonist. It has anti-anxiety activity.</p>

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.

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

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

CGP 64213 is a GABAb receptor agonist.

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

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

GABAA antagonist

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].

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.

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

(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.

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

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

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

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

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).

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].

SCS is a GABAA receptor antagonist.

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].

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

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

<p>PZ-II-029 is a modulator of α6β3γ2-selective GABAA channel.</p>

<p>(-)-Bicuculline methochloride is a potent antagonist of GABAA receptor.</p>

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

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

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

<p>SGE516: neuroactive steroid, enhances GABAA, lowers neuronal activity, protects from seizures.</p>

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

<p>TP003 is a novel non-selective GABAA receptor benzodiazepine site agonist with affinity for α1β2gam2, α2β3gam2, α3β3gam2, α5β2gam2, EC50 of 20.3, 10.6, 3.24, 5.</p>

EF1502 is a potent and selective GABA transporter inhibitor.

<p>Moxetomidate is a GABAA receptor (GABAA receptor) agonist with hypnotic properties.</p>

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.

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

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.

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

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

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.

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

benzodiazepine receptor antagonist,competitive

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

Refisolone is an antagonist of the GABAA receptor.

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.

(-)-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].

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.

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

CGP 44532 a GABAB receptor agonist.

<p>Xilmenolone acts as a positive allosteric modulator of the GABA_A receptor [1].</p>

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