PF-05180999 is an inhibitor of phosphodiesterase 2A (IC50: 1.6 nM).

PF-05180999 is also a weak inducer of CYP3A4, and with no direct inhibition of human recombinant cytochrome P450 (CYP) enzymes (1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A) and no induction of CYP1A2. PF-05180999 binds to the rat, dog and monkey PDE2A (Kis: 4.2, 8.4, and 5.5 nM and IC50s: 2.6, 5.2, and 3.4 nM, respectively). PF-05180999 displays weak activity against PDE, with IC50s of 2.03 μM (PDE10A1), 26.969 μM (PDE7B), 50.09 μM (PDE11A4), and >56.25 μM (PDE1B1, PDE3A1, PDE4D3, PDE5A1, PDE6 (bovine), PDE8B, PDE9A1), respectively [1].

PF-05180999 induces acute and exposure-dependent elevation in the accumulation of cGMP bulk levels in the cortex, striatum, and hippocampus, but with no changes in cAMP and the associated downstream phospho-cAMP response element-binding protein (p-CREB) in mice. PF-05180999 (0.032-0.32 mg/kg mg/kg, s.c.) dramatically decreases the working memory errors produced by ketamine in a working memory radial arm maze (RAM) model in rats [1].

1394033-54-5

C19H17F3N8

414.39

PF-05180999

DMSO:50 mg/mL (120.66 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years