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Mardepodect (PF-2545920) 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。
中文别名:
2-[(4-(1-甲基-4-(吡啶-4-基)-1H-吡唑-3-基)苯氧基)甲基]喹啉
物化属性:
密度:1.216
沸点:568.569°C at 760 mmHg
折射率:1.661
闪光点:297.66°C
PSA:52.83000
LOGP:5.27630
[1]. 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, 52(16), 5188-5196.
[2]. Grauer SM, et al. Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia. J Pharmacol Exp Ther, 2009, 331(2), 574-590.
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