Description
PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT
4A, 5-HT
4B, 5-HT
4D, and 5-HT
4E (K
is = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay). It increases cAMP levels in HEK293 cells expressing 5-HT
4A, 5-HT
4B, 5-HT
4D, and 5-HT
4E receptors (EC
50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg.