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Cat. No. Name Size Price Add Cart
KI0576PF-25459205 mg$526
PF-254592010 mg$722
PF-254592050 mg$1896
PF-2545920200 mg$5220

Chemical Characteristic

Product NamePF-2545920
SynonymsMP-10
CAS No.1292799-56-4
Molecular Weight 392.45
FormulaC25H20N4O
Chemical Name2-((4-(1-methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl)phenoxy)methyl)quinoline
Smilesn1c(ccc2ccccc12)COc1ccc(cc1)c1nn(cc1c1ccncc1)C
Chemical Structure

Biological activities

PF-2545920 is a specific phosphodiesterase-10A (PDE10A) inhibitor.[1] PF-2545920 inhibits PDE10A with an IC50 of 0.18 nM. [2] PF-2545920 inhibits human phosphodiesterases (hPDE10, hPDE2A and hPDE4A) with IC50 of 1.26 nM, 3.6 and 1.7 μM, respectively. [3] Pre-dosing of rats with PF-2545920 (1 mg/kg) reduce tracer uptake in the striatum by 14% relative to the tracer uptake in the cerebellum. [1] PF-2545920 causes some increases in GluR1 phosphorylation levels of 3-, 5.4-, and 4.1-fold with 0.3, 3, and 5 mg/kg doses, respectively. PF-2545920 (3 mg/kg) increases both enkephalin and substance-P mRNA levels. PF-2545920 (0.1-30 mg/kg i.p.) produces a decrease in apomorphine-induced climbing in mice with an ID50 of 0.375 mg/kg and decreases apomorphine-induced stereotypy with an ID50 of 25.069 mg/kg. PF-2545920 also exhibits antipsychotic-like properties by increasing prepulse inhibition (PPI) in C57BL/6J mice. PF-2545920 also dose-dependently decreases locomotor activity with 0.3 mg/kg reducing activity. [3] In vivo, PF-2545920 inhibits conditioned avoidance responding (CAR) and antagonizes phencyclidine- and amphetamine-induced hyperactivity in rats with AED50 of 0.7, 1 and 4.4 mg/kg sc, respectively. [4]

Protocols

PF-2545920 is dissolved and administered in a vehicle containing 10% DMSO and 20% (2-hydroxypropyl)-β-cyclodextrine. [1]

References

[1] Celen S, et al. Preclinical evaluation of 18F-JNJ41510417 as a radioligand for PET imaging of phosphodiesterase-10A in the brain. J Nucl Med. 2010, 51(10): 1584-1591.
[2] Tu Z, et al. Radiosynthesis and in vivo evaluation of [11C]MP-10 as a PET probe for imaging PDE10A in rodent and non-human primate brain. Bioorg Med Chem. 2011, 19(5): 1666-1673.
[3] Grauer SM, et al. Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia. J Pharmacol Exp Ther. 2009, 331(2): 574-590.
[4] Izco-Basurko I, et al. Highlights from the 236th American Chemical Society (ACS) National Meeting & Exposition. Drugs Fut. 2008, 33(11): 991.

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