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N-DesmethylPimavanserin是Pimavanserin的活性代谢物。Pimavanserin是选择性的5-HT2A受体反向激动剂,pIC50和pKd分别为8.73和9.3。
N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.
The mean plasma half-lives for Pimavanserin and its metabolite N-Desmethyl Pimavanserin (AC-279) are 57 hours and 200 hours, respectively.
[1]. Vanover KE, et al. Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist. J Pharmacol Exp Ther. 2006 May;317(2):910-8.
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