PF-03654764

PF-03654764 is an orally active, selective small molecule antagonist of the histamine H3 receptor, developed by Pfizer. It binds with high affinity to the human H3 receptor and displays over 1000-fold selectivity versus other human histamine receptor subtypes (H1, H2, and H4). In functional assays, it demonstrated potent antagonist properties. The drug was investigated for allergic rhinitis (Phase II) and Alzheimer's disease (Phase I), but development was discontinued after clinical trials showed no significant benefit over existing therapies and a higher incidence of adverse events[2][4][7].

Other names

H3 receptor antagonist 1H-3 receptor antagonist 1H 3 receptor antagonist 13-fluoro-3-(3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl)-N-(2-methylpropyl)cyclobutanecarboxamide