PF-2545920

PF-2545920 is a potent inhibitor of phosphodiesterase 10A (PDE10A, IC50 = 1.26 nM for the human recombinant enzyme). It is selective for PDE10A over other PDEs with IC50 values ranging from 1.7 to >10 µM. In vivo, PF-2545920 (0.1-3 mg/kg, i.p.) increases cAMP and cGMP production as well as phosphorylation of CREB and GluR1 in mouse striatum in a dose-dependent manner. It reduces climbing behavior induced by apomorphine (Cay-16094) in mice (ID50 = 0.375 mg/kg) and disrupts the conditioned avoidance response in mice and rats (ID50s = 0.441 and 1.079 mg/kg, respectively). PF-2545920 reverses deficits in prepulse inhibition and social odor recognition induced by (+)-MK-801 (Cay-10009019) in rats. Formulations containing PF-2545920 are under clinical investigation for the treatment of schizophrenia and Huntington's disease.Formal Name: 2-[[4-[1-methyl-4-(4-pyridinyl)-1H-pyrazol-3-yl]phenoxy]methyl]-quinoline. CAS Number: 898562-94-2. Molecular Formula: C25H20N4O. Formula Weight: 392.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:20): 0.05 mg/ml, DMSO: 15 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 233, 317 nm. SMILES: CN1C=C(C2=CC=NC=C2)C(C(C=C3)=CC=C3OCC4=NC5=CC=CC=C5C=C4)=N1. InChi Code: InChI=1S/C25H20N4O/c1-29-16-23(18-12-14-26-15-13-18)25(28-29)20-7-10-22(11-8-20)30-17-21-9-6-19-4-2-3-5-24(19)27-21/h2-16H,17H2,1H3. InChi Key: AZEXWHKOMMASPA-UHFFFAOYSA-N.