• Catalog Number:

  E1KS2687

• Amount:

  5mg1​ PHYSICAL AND CHEMICAL PROPERTIES

2​ Biological Activity 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. [1][2] 3​ References: Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. Verhoest PR et al. J Med Chem. 2009 Aug 27;52(16):5188-96. The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.