GABA Receptor Agonist

Emamectin-d₃ is the deuterium labeled Emamectin. Emamectin is a macrocyclic lactone insecticide. Emamectin acts as agonist for GABA-gated chloride channels.

(R)-Baclofen hydrochloride (Arbaclofen hydrochloride) is a selective GABAB receptor agonist.

Phenibut (Standard) is the analytical standard of Phenibut (HY-108403). This product is intended for research and analytical applications. Phenibut (β-Phenyl-GABA) is a GABA-B agonist. Phenibut acts as a GABA-mimetic, primarily at GABAB receptors. Phenibut has anxiolytic and nootropic (cognition enhancing) effects.

AZD7325 (Standard) is the analytical standard of AZD7325. This product is intended for research and analytical applications. AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.

Miltirone is an orally active natural compound found in the root of Salvia miltiorrhiza. Miltirone is a central benzodiazepine receptor partial agonist, with an IC50 of 0.3 μM. Miltirone induces ROS - and-p53 dependent apoptosis. Miltirone inhibits carboxylesterase 2 (CES2; Ki = 0.04 μM) and SARS-CoV main protease (Mpro).

THIP (Gaboxadol) Standard is the analytical standard of THIP (HY-10232). This product is intended for research and analytical applications. THIP (Gaboxadol) is a blood-brain barrier-penetrant, orally active selective GABA_A receptor agonist. THIP exhibits EC₅₀ values of 33 μM and 130 μM for α₄β₂δ and α₄β₁δ receptors, respectively. THIP activates extrasynaptic GABA_A receptors to produce tonic inhibition and inhibits GABAergic interneurons to cause disinhibition. THIP is used in research on insomnia, sleep disorders, and addictive behaviors.

Clomethiazole (Standard) is the analytical standard of Clomethiazole. This product is intended for research and analytical applications. Chlormethiazole is an potent and orally active GABAA agonist. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus.

JY-XHe-053 is a potent and selective agonist of GABAA receptors containing the α5 subunit (K_is of 22.0 nM, 12.3 nM, 34.9 nM, 0.7 nM for α1, α2, α3, α5, respectively). JY-XHe-053 lacks significant anti-anxiety activity, despite its efficacy at α2- and α3-GABAA receptors.

Y-23684 is a partial agonist of benzodiazepine receptor (BZR) with anticonvulsant and anxiolytic activities. Y-23684 can be used in the research of treatment of anxiety disorders.

PF 0713 is a GABAA receptor agonist..

Loreclezole (Standard) is the analytical standard of Loreclezole. This product is intended for research and analytical applications. Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.

Imepitoin (Standard) is the analytical standard of Imepitoin. This product is intended for research and analytical applications. Imepitoin (AWD 131-138) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.

Afloqualone-d₇ (HQ-495-d₇) is deuterium labeled Afloqualone. Afloqualone (HQ-495) is an orally active central muscle relaxant and antivertiginous agent that can increase the sensitivity of GABA receptors in neurons of the lateral vestibular nucleus. Afloqualone (HQ-495) can be used in the research of low back pain and neck-arm-shoulder syndrome.

3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated from the roots of Polygala tenuifolia WILLD, with anti-stress effect, prolonging the sleeping time in animals. 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and γ-subunit of GABAA receptor, but shows no effect on the amounts of α-, β-subunits.

DAA-1106 (Standard) is the analytical standard of DAA-1106. This product is intended for research and analytical applications. 0

Lesogaberan (hydrochloride) (Standard) is the analytical standard of Lesogaberan (hydrochloride) (HY-10061B). This product is intended for research and analytical applications. Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.

Pynazolam is a predicted positive allosteric modulator of GABA_A receptor. 3D-field QSAR and RVM models predict an IC₅₀ of approximately 0.40 nM. Pynazolam can be used in studies related to GABA_A receptor pharmacology.

TACA (Standard) is the analytical standard of TACA (HY-100800). This product is intended for research and analytical applications. TACA (trans-4-Aminocrotonic acid) is a potent agonist of GABAA and GABAC receptors (KD= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons.

Ru-32514 is an agonist of benzodiazepine receptor.

U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects.