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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-Pimavanserin
Pimavanserin

Chemical Structure : Pimavanserin

CAS No.: 706779-91-1

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Pimavanserin (ACP-103, ACP103)

货号: PC-20963Not For Human Use, Lab Use Only.

Pimavanserin (ACP-103) is a potent, selective, orally active 5-HT2A receptor inverse agonist, competitively antagonizes the binding of [(3)H]ketanserin to heterologously expressed human 5-HT(2A) receptors with pKi of 9.3 in membranes and 9.70 in whole cells.

规格 价格 库存 数量
25 mg ￥980 In stock
50 mg ￥1480 In stock
100 mg ￥2280 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Pimavanserin (ACP-103) is a potent, selective, orally active 5-HT2A receptor inverse agonist, competitively antagonizes the binding of [(3)H]ketanserin to heterologously expressed human 5-HT(2A) receptors with pKi of 9.3 in membranes and 9.70 in whole cells.
ACP-103 displayed potent inverse agonist activity in the cell-based functional assay receptor selection and amplification technology (R-SAT) with pIC50 of 8.3.
ACP-103 displayed no affinity and functional activity at 5-HT(2B) receptors, dopamine D(2) receptors, and other human monoaminergic receptors.
ACP-103 attenuated head-twitch behavior (3 mg/kg p.o.), and prepulse inhibition deficits (1-10 mg/kg s.c.) induced by the 5-HT(2A) receptor agonist (+/-)-2,5-dimethoxy-4-iodoamphetamine hydrochloride in rats and reduced the hyperactivity induced in mice by the N-methyl-d-aspartate receptor noncompetitive antagonist MK-801 (dizocilpine maleate).

物理化学性质&存储条件

分子量 427.56
分子式 C25H34FN3O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1-(4-fluorobenzyl)-3-(4-isobutoxybenzyl)-1-(1-methylpiperidin-4-yl)urea

参考文献

1. Vanover KE, et al. Pharmacol Biochem Behav. 2008 Oct;90(4):540-4.

2. Vanover KE, et al. J Pharmacol Exp Ther. 2006 May;317(2):910-8.

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