MRK-016

• CAT Number: I003248
• CAS Number: 342652-67-9
• Molecular Formula: C17H20N8O2
• Molecular Weight: 368.39
• Purity: ≥95%
• Target: GABA Receptor
• Solubility: Soluble in DMSO
• Storage: Store at -20°C

MRK-016 (Cat No.:I003248) is a compound that acts as a functionally selective, inverse agonist at the benzodiazepine site of GABAA α5 receptors. By binding to the benzodiazepine site on these receptors, MRK-016 exerts its effects by inhibiting the activity of GABAA α5 receptors. This selective antagonism of GABAA α5 receptors can lead to specific modulation of neurotransmission and neuronal activity, offering potential therapeutic applications in disorders where GABAA α5 receptor function is implicated, such as cognitive impairments and neurological conditions.

Reference

[1]. Eimerbrink MJ et al. Administration of the inverse benzodiazepine agonist MRK-016 rescues acquisition and memory consolidation following peripheral administration of bacterial endotoxin. Behav Brain Res, 2015 Jul 15, 288:50-3.

[2]. Chambers MS et al. An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. J Med Chem, 2004 Nov 18, 47(24):5829-32.

[3]. Atack JR et al. In vitro and in vivo properties of 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)-pyrazolo[1,5-d]-[1,2,4]triazine (MRK-016), a GABAA receptor alpha5 subtype-selective inverse agonist. J Pharmacol Exp Ther, 2009 Nov, 331(2):470-84.