MK-0249 (Compound 1) is a potent, selective and orally active histamine H3 receptor antagonist, with an IC50 of 1.7 nM for human H3[1].
IC 50
human H3 receptor: 1.7 nM (IC50); rhesus H3 receptor: 4.3 nM (Ki); human H3 receptor: 6.8 nM (Ki); rat H3 receptor: 33 nM (Ki)
References
[1] Nagase T, et al. Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists. J Med Chem. 2008 Aug 14;51(15):4780-9. DOI:10.1021/jm8003834
