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编 号:F197802
分子式:C29H29FN7O5P
分子量:605.56
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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生物活性:
ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions.

体内研究:
ITI-214 在测试中显著增强记忆性能,最低有效剂量为 3 mg/kg。Animal Model:Male Sprague-Dawley rats
Dosage:0.1-10 mg/kg
Administration:p.o.
Result:Significantly enhanced memory performance in the test with a minimum effective dose of 3 mg/kg.

体外研究:
与下一个最接近的 PDE 家族酶 PDE4D (Ki= 33 nM) 相比,ITI-214 对 PDE1 亚型的活性高 1000 倍以上,对所有其他 PDE 酶家族的选择性高 10,000-300,000 倍。
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