A potent inhibitor of PDE10A (IC50 = 1.26 nM for the human recombinant enzyme); selective for PDE10A over other PDEs with IC50 values ranging from 1.7 to >10 μM; increases cAMP and cGMP production as well as phosphorylation of CREB and GluR1 in mouse striatum in a dose-dependent manner; reduces apomorphine-induced climbing behavior 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

PF-2545920 – 25 mg

Brand:
Cayman
CAS:
898562-94-2
Storage:
-20
UN-No:
Non-Hazardous - /

PF-2545920 is a potent inhibitor of phosphodiesterase 10A (PDE10A; IC50 = 1.26 nM for the human recombinant enzyme).{38516} 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 (Item No. 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 (Item No. 10009019) in rats. Formulations containing PF-2545920 are under clinical investigation for the treatment of schizophrenia and Huntington’s disease.  

 

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Description

A potent inhibitor of PDE10A (IC50 = 1.26 nM for the human recombinant enzyme); selective for PDE10A over other PDEs with IC50 values ranging from 1.7 to >10 μM; increases cAMP and cGMP production as well as phosphorylation of CREB and GluR1 in mouse striatum in a dose-dependent manner; reduces apomorphine-induced climbing behavior 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); reverses (+)-MK-801-induced deficits in prepulse inhibition and social odor recognition in rats,

Formal name: 2-[[4-[1-methyl-4-(4-pyridinyl)-1H-pyrazol-3-yl]phenoxy]methyl]-quinoline

Synonyms: 

Molecular weight: 392.5

CAS: 898562-94-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphodiesterases||Research Area|Neuroscience|Behavioral Neuroscience|Schizophrenia & Psychosis||Research Area|Neuroscience|Neurodegenerative Disorders|Huntington’s Disease

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