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MK-0249 (Compound 1) is a potent, selective and orally active histamine H 3 receptor antagonist, with an IC 50 of 1.7 nM for human H3.
IC50& Target:human H 3 receptor 1.7 nM (IC 50 ) rhesus H 3 receptor 4.3 nM (Ki) human H 3 receptor 6.8 nM (Ki) rat H 3 receptor 33 nM (Ki)
In Vitro:MK-0249 (Compound 1) shows very good hepatic clearance values (CLh e 11 mL/min/kg), and is a substrate for rat P-gp but not for human P-gp. MK-0249 displays potent binding affinity to human, rat, and rhesus H 3 receptors with K i values of 6.8 ± 1.3
Biological Activity:MK-0249 (Compound 1) is a potent, selective and orally active histamine H 3 receptor antagonist, with an IC 50 of 1.7 nM for human H3.