H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM.
H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM[1].
H4 Receptor antagonist 1 indicates that metabolic stability in rat microsomes is very low with only 1% parent compound remaining after 10 min incubation[1].
[1]. Cramp S, et al. Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2516-9.