product name PF-2545920 HCl
Description: PF-2545920 HCl is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, and with >1000-fold selectivity over the PDE. It is potentially useful for the treatment of schizophrenia. PF-2545920 is active in a range of antipsychotic models, antagonizing apomorphine-induced climbing in mice, inhibiting conditioned avoidance responding in both rats and mice, and blocking N-methyl-D-aspartate antagonist-induced deficits in prepulse inhibition of acoustic startle response in rats, while improving baseline sensory gating in mice.
References: J Pharmacol Exp Ther. 2009 Nov;331(2):574-90; J Med Chem. 2009 Aug 27;52(16):5188-96.
428.91
Formula
C25H20N4O. HCl
CAS No.
1292799-56-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO:
Water:
Ethanol:
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: PF-2545920 intraperitoneally administrated at dose of 0.3, 3, and 5 mg/kg in male CF-1 mice causes striking increases in GluR1 phosphorylation levels of 3-, 5.4-, and 4.1-fold , respectively. MP-10 at concentration of 1 μM treats Rat striatal slices for 30 min, the level of GluR1S845 phosphorylation at the cell surface is significantly increased 2-fold, without change the level of total GluR1 on the cell surface. MP-10 intraperitoneally administrated at dose of 0.3, 3, and 5 mg/kg in male CF-1 mice results in robust, statistically significant increases in CREBS133 phosphorylation of 3-, 4-, and 2.6-fold, respectively. MP-10 intraperitoneally administrated at dose of 3 mg/kg increases both enkephalin and substance-P mRNA levels in striatum of CF-1 mice. MP-10 intraperitoneally administrated at dose of 0.3-1 mg/kg decreases avoidance responding with a significant treatment effect in the mouse CAR model. Mice treated with MP-10 at dose of 0.03 mg/kg spents more time in the empty than social side in the mice, MP-10 also dose-dependently decreased locomotor activity. Kinase Assay: Cell Assay: |
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| In Vivo | PF-2545920 is shown to be efficacious both in vitro and in vivo with improved penetration in CNS. It has excellent in vivo efficacy in neurochemical elevation of cyclic nucleotides and in models predictive of antipsychotic activity. Administration of PF-2545920 to mice can cause increase in striatal cGMP with the minimal effective dose at about 1mg/kg. |
| Animal model | Jugular vein-cannulated male Sprague-Dawley rats |
| Formulation & Dosage | Dissolved in 5:5:90 DMSO:1N HCl:saline; 0.1 mg/kg; i.v. injection |
| References | J Pharmacol Exp Ther. 2009 Nov;331(2):574-90; J Med Chem. 2009 Aug 27;52(16):5188-96. |
