PF-2545920 a highly selective and potent PDE10A inhibitor with an IC50 of 0.37 nM. The PDE10A enzyme is expressed primarily in the brain, mostly in the striatum, nucleus accumbens and olfactory tubercle, and is thought to be particularly important in regulating the activity of dopamine-sensitive medium spiny neurons in the striatum which are known to be targets of conventional antipsychotic agents. n the conditioned avoidance response assay (CAR), PF-2545920 was active with an ED50 of 1 mg/kg. Administration of PF-2545920 to mice caused a dose dependent increase in striatal cGMP.
|Animal models||Jugular vein-cannulated male Sprague-Dawley rats|
|Formulation||5:5:90 DMSO:1N HCl:saline|
|Administration||Inject intravenous through jugular vein catheter in a single dose 4 hours before feed|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 70 mg/mL|
|Related PDE Products|
RVT-501 (E6005) is a selective phosphodiesterase 4 (PDE4PDE4) inhibitor with an IC50 of 2.8 nM.
Vardenafil Hcl is a PDE5 inhibitor used for treating erectile dysfunction.
Udenafil(DA8159) is a PDE5 inhibitor used in urology to treat erectile dysfunction.
Theophylline is a methylated xanthine derivative; competitive nonselective phosphodiesterase inhibitor and nonselective adenosine receptor antagonist.
Sildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.