GABA Receptor Agonist

LI-633 is a selective and orally active GABAA receptor positive allosteric modulator (PAM) with a K_i of 21 nM. LI-633 produces robust potentiation of GABA-induced inward current, with EC₅₀ values ranging from 8 nM (α5β2γ2) to 128 nM (α3β2γ2). LI-633 potentiates muscimol-induced GABAergic currents in rat dorsal root ganglion (DRG) neurons with an EC₅₀ of 70.4 nM. LI-633 can be used for the study of visceral pain.

Lesogaberan (AZD-3355) napadisylate 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 napadisylate 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 napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.

Brexanolone caprilcerbate is a potent GABAA receptor positive allosteric modulator.

CP-615003 is a potent and subtype-selective partial agonist of GABA_A receptor (GABA_A receptor) (K_i = 1.1 μM). CP-615003 is mainly converted into the active metabolite CP-900725 through oxidative deamination in monkeys and humans, and the latter also has GABA_A receptor affinity. CP-615003 is a substrate of P-glycoprotein (P-gp/MDR1), resulting in severe limitation of its penetration into the central nervous system (CNS). CP-615003 can be used for the study of CNS-related indications.

DAA-1097 is an orally active and selective agonist for the peripheral benzodiazepine receptor (PBR). DAA-1097 has anxiolytic effects.

Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a 5GABAA partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors.

5α-Androstan-3α-ol is a γ-aminobutyric acid (GABA) receptor agonist. 5α-Androstan-3α-ol can inhibit the transcriptional activity of the orphan nuclear receptor CAR (constitutive androstane receptor). 5α-Androstan-3α-ol negatively regulates the activity of CAR by binding to CAR and promoting its dissociation from coactivator proteins. 5α-Androstan-3α-ol can be used to study nuclear receptor-mediated hormone metabolism and drug detoxification mechanisms.

Divaplon is a GABA receptor agonist with the EC₅₀ values of 31 and 2 nM for α3β2γ2 and α5β2γ2, respectively. Divaplon shows anxiolytic activity.

(S)-Baclofen is a GABAB receptor agonist that crosses the blood-brain barrier and is orally active, with IC₅₀ values ​​of 1.77 μM for GABAB and 1564 μM for GABAA. (S)-Baclofen can be used in research on muscle disorders such as spasticity.

RWJ-51204 is a partial agonist of GABA(A) receptor, with K_i of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.

Picamilon sodium is an orally active derivative of γ-aminobutyric acid that has nootropic effect. Picamilon sodium improves the epilepsy model in rats and promotes correction of functional disorders of the pancreas during Alloxan (HY-W017227)-induced diabetes mellitus in rats.

PWZ-029 is a selective inverse agonist for 5 GABA_A receptors. PWZ-029 is a benzodiazepine site ligand. PWZ-029 shows a weak but significant partial agonistic effect at 1- and 3-containing receptors. PWZ-029 significantly increases retention session latency in mouse fibroblast cells. PWZ-029 can improve object recognition in normal and scopolamine-treated rat model.

γ-Aminobutyric acid-¹⁵N (4-Aminobutyric acid-¹⁵N) is the ¹⁵N-labeled γ-Aminobutyric acid (HY-N0067). γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABA_A receptors) and metabotropic receptors (GABA_B receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system.

GABAA receptor modulator-8 (10c) is a blood-brain barrier penetrated, selective and positive modulator of GABAA receptor, with excellent antiepileptic activity.

Carbromal (Standard) is the analytical standard of Carbromal. This product is intended for research and analytical applications. Carbromal (Adalin; Adisomnol) is a sedative with centrally depressant effects.

Azocarnil is a GABAergic agonist-potentiator. Azocarnil can be used in neurological research.

HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects. HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

(S)-Norzopiclone ((S)-N-Desmethyl zopiclone; SEP-174559) is a metabolite of Zopiclone with anxiolytic and anticonvulsant effects. (S)-Norzopiclone has benzodiazepine-like actions at γ2-bearing subtypes of the GABA_A receptor and inhibits nACh and NMDA receptors.

Adipiplon (NG2-73) is a selective GABA_A receptor positive allosteric modulator. Adipiplon is particularly useful in the research of a variety of central nervous system (CNS) disorders.

Adinazolam-d₅ (U 41123-d₅) is a deuterium labeled Adinazolam (HY-A0198). Adinazolam is a triazolobenzodiazepine. Adinazolam binds to peripheral-type benzodiazepine receptors which interact allosterically with GABA receptors. Adinazolam has dual anxiolytic and antidepressant activities.