PF-03654764

PF-03654764 is an orally active, selective histamine H 3 receptor antagonist with K i values of 1.2 nM and 7.9 nM for human H 3 and rat H 3 in whole cell assay, respectively. The combination of PF-03654764 and Fexofenadine ( HY-B0801A ) has the potential for allergic rhinitis researchIn VitroPF-03654764 has pK i values of 8.98 and 8.10 for human H 3 and rat H 3 in whole cell assay, respectively. PF-03654764 has pK i values of 8.84, 7.73 and K i values of 1.4 nM and 19 nM for human H 3 and rat H 3 in HEK-293 cells, respectively. PF-03654764 has >1000-fold selectivity for the H3 receptor over the other histamine receptor subtypes. PF-03654764 has a human liver microsomes (HLM) T 1/2 of 120 min and a HLM CL h <5 mL/min•kg. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoPF-03654764 (10 mL/kg; oral; 14 days) has a C max of 8057 ng/mL and an AUC 0-24 of 67400 ng•h/mL in Sprague-Dawley rats . PF-03654764 (1 mL/kg; oral; 7 days) has a C max of 6302 ng/mL and an AUC 0-24 of 18175 ng•h/mL in beagle dogs . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:human H 3 receptor 1.2 nM (Ki) rat H 3 receptor 7.9 nM (Ki) human H 3 receptor 8.98 (pKi) rat H 3 receptor 8.10 (pKi). Specifications and Purity: ≥99.0%. Molecular Formula: C20H28F2N2O. Molecular Weight: 350.45. PubChem CID: 16119082. Isomeric SMILES: CC(C)CNC(=O)C1CC(C1)(C2=CC(=C(C=C2)CN3CCCC3)F)F.