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Chemical Structure : Pimavanserin
CAS No.: 706779-91-1
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $148 | In stock | |
| 100 mg | $298 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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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).
| M.Wt | 427.56 | |
| Formula | C25H34FN3O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1-(4-fluorobenzyl)-3-(4-isobutoxybenzyl)-1-(1-methylpiperidin-4-yl)urea |
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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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