Mardepodect hydrochloride (Synonyms: PF-2545920 hydrochloride) |
| رقم الكتالوجGC36541 |
هيدروكلوريد Mardepodect (PF-2545920 hydrochloride) هو مثبط فعال وفعال عن طريق الفم وانتقائي PDE10A مع IC50 من 0.37 نانومتر ، مع انتقائية أكثر من 1000 ضعف على أجهزة PDE الأخرىيمكن لهيدروكلوريد ماردبودكت عبور الحاجز الدموي الدماغي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2070014-78-5
Sample solution is provided at 25 µL, 10mM.
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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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