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Pimavanserin tartrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pimavanserin tartrate图片
CAS NO:706782-28-7
规格:98%
分子量:1005.2
包装与价格:
包装价格(元)
1g电议
500mg电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议

产品介绍
Pimavanserin tartrate (ACP-103) 是一种有效的 5-HT 2A 受体反向激动剂,pIC50 和 pKi 值分别为8.73和9.3。
CAS:706782-28-7
分子式:C54H74F2N6O10
分子量:1005.2
纯度:98%
存储:Store at -20°C

Background:

Pimavanserin tartrate (ACP-103) is a potent 5-HT 2A receptor inverse agonist with pIC50 and pKi of 8.73 and 9.3, respectively. pIC50: 8.73 (5-HT 2A)[1]pKi: 9.3 (5-HT 2A)[1]


Pimavanserin tartrate competitively antagonizes the binding of [3H]ketanserin to heterologously expressed human 5-HT 2A receptors with a mean pKi of 9.3 in membranes and 9.70 in whole cells. ACP- 103 displays potent inverse agonist activity in the cell-based functional assay receptor selection and amplification technology (R-SAT), with a mean pIC50 of 8.7. Pimavanserin tartrate demonstrates lesser affinity (mean pKi of 8.80 in membranes and 8.00 in whole cells, as determined by radioligand binding) and potency as an inverse agonist (mean pIC50 7.1 in R-SAT) at human 5-HT 2C receptors, and lacks affinity and functional activity at 5-HT 2B receptors, dopamine D2 receptors, and other human monoaminergic receptors[1].


Pimavanserin tartrate attenuates head-twitch behavior (3 mg/kg p.o.), and prepulse inhibition deficits (1-10 mg/kg s.c.) induced by the 5-HT2A receptor agonist in rats and reduces the hyperactivity induced in mice by the N-methyl-D-aspartate receptor noncompetitive antagonist, consistent with a 5-HT 2A receptor mechanism of action in vivo and antipsychotic-like efficacy. Pimavanserin tartrate demonstrates 42.6% oral bioavailability in rats[1].


[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.