Mardepodect hydrochloride (PF-2545920 hydrochloride) 是一种有效的选择性 PDE10A 抑制剂，IC50 为 0.37 nM，比作用于其他 PDE 选择性高 1000 多倍。
Mardepodect hydrochloride (PF-2545920 hydrochloride) is a potent and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over the PDE. IC50: 0.37 nM (PDE10A)[1].
In the conditioned avoidance response assay (CAR), Mardepodect (PF-2545920) is active with an ED50 of 1 mg/kg. Administration of Mardepodect (PF-2545920) to mice causes a dose dependent increase in striatal cGMP.
[1]. Wilson JM et al. Phosphodiesterase 10A inhibitor, MP-10 (PF-2545920), produces greater induction of c-Fos in D2 neurons than in D1 neurons in the neostriatum. Neuropharmacology. 2015 Dec;99:379-86. [2]. Verhoest PR et al. 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. J Med Chem. 2009 Aug 27;52(16):5188-96.
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