GABA Receptor Agonist

Thiomuscimol is a GABAA receptor agonist (IC₅₀=19 nM). It has been used as a photoaffinity label for the purification and identification of GABA binding sites within the GABAA receptor complex.

Josamycin propionate (Standard) is the analytical standard of Josamycin propionate. This product is intended for research and analytical applications. Josamycin propionate is classified as a macrolide antibiotic.

Alphadolone is a GABAA receptor positive allosteric modulator. Alphadolone has antinociceptive effects. Alphadolone causes general anaesthesia.

Pagoclone is an active (+)-enantiomer of the racemate RP 59037. Pagoclone is a partial GABA(A) receptor agonist used for the treatment of panic and anxiety disorders.

NS-2710 is a high-efficacy GABAAα3 agonist with a K_i of 9.2 nM. NS-2710 can be used for anxiety research.

diproqualone is methaqualone analogous with sedative, anxiolytic, anti-inflammatory and analgesic properties.

SX-3228 is a selective benzodiazepine1 (BZ1) receptor agonist with an IC₅₀ of 17 nM.

ZAPA sulfate is an agonist at low affinity GABA_A-receptors. ZAPA sulfate induces membrane hyperpolarization of the Ascaris muscle cell with an EC₅₀ of 10.3 μM.

Adinazolam (U 41123) is a triazolobenzodiazepine. Adinazolam binds to peripheral-type benzodiazepine receptors which interact allosterically with GABA receptors. Adinazolam has dual anxiolytic and antidepressant activities.

Lesogaberan (AZD-3355) is a potent and selective GABA_B receptor agonist with an EC₅₀ of 8.6 nM for human recombinant GABA_B receptors. The affinity (K_is) of Lesogaberan for rat GABA_B and GABA_A receptors, as measured by displacement of [³H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.

Zopiclone N-oxide (RP 29753) is a less active metabolite of Zopiclone. Zopiclone N-oxide is also an impurity of Eszopiclone and is formed by the oxidation of Eszopiclone.

Imepitoin (AWD 131-138) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.

MRK-623 (Compound 14k) is an orally active, high-affinity GABA_A receptor agonist, with the K_i values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. MRK-623 shows anxiolytic effect.

Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity.

Isonipecotic acid is a GABAA receptor partial agonist.

CP-409092 is a partial agonist of GABA_A receptor, with anti-anxiety activity.

Arbaclofen placarbil is a novel transported proagent of the active R-isomer of baclofen. Baclofen is a racemic GABA_B receptor agonist

ASP8062 is an orally active, blood-brain barrier-permeable selective GABA_B receptor positive allosteric modulator. ASP8062 enhances GABA-mediated activation of GABA_B receptors and strengthens GABAergic neurotransmission. ASP8062 reverses Reserpine (HY-N0480)-induced myalgia, regulates the sleep-wake cycle, increases delta wave power during non-REM sleep, and impairs motor coordination at high doses. ASP8062 penetrates the central nervous system with a half-life of 40-50 h. ASP8062 can be used in research related to opioid use disorder, fibromyalgia, chronic pain, and alcohol use disorder.

Acamprosate-d₃ (calcium) is the deuterium labeled Acamprosate calcium. Acamprosate calcium is a GABA receptor agonist and modulator of glutamatergic systems.

Baclofen-d₄ is the deuterium labeled Baclofen. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research.