MP-III-024

MP-III-024 is a novel selective positive allosteric modulator (PAM) of the GABA-A receptor, specifically displaying functional selectivity for the α2 and α3 subtypes of the GABA-A receptor over the α1 and α5 subtypes. This imidazodiazepine derivative acts at the benzodiazepine site but exhibits antinociceptive (pain-reducing) and antihyperalgesic (reducing increased pain sensitivity) effects with little to no sedative or off-target actions at standard doses in animal models. Developed primarily for research into pain modulation, it has been studied in combination with opioids (notably morphine) as a means to achieve effective pain control with lower opioid dosages, thereby potentially reducing opioid-related adverse effects. Initial development and synthesis involved the University of Wisconsin-Milwaukee and associated research centers[1][2][3].

Other names

methyl 8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepine-3-carboxylate