Rats: Following single intravenous administration (1 mg/kg) of PF-3246799 to rat, plasma clearance was moderate relative to liver blood flow and volume of distribution was moderate resulting in an elimination half-life of 2.8 h. Following single oral administration to rat (2 mg/kg), PF-3246799 was rapidly absorbed and showed moderate oral bioavailability (40%) suggesting complete absorption from the gut, based on blood clearance of 51 ml/min/kg and an assumed liver blood flow of 70 ml/min/kg. Dogs: Following single intravenous administration to dog (0.030 mg/kg), plasma clearance of PF-3246799 was low relative to liver blood flow resulting in an elimination half-life of 3.4 h.

Screening of PF-3246799 in the 5-HT2A recombinant assay gave a significant response with an EC50 68 nM and Emax 82%. PF-3246799 showed weak but measurable agonism of 5-HT2B at 10 uM in both recombinant cell systems and native human tissue.