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Pimavanserin

CAS No. : 706779-91-1

MCE 站：Pimavanserin

产品活性：Pimavanserin是选择性的 5-HT2A 受体反向激动剂，pIC₅₀ 和 pK_d 分别为8.73 ａnd 9.3。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

In Vitro: Pimavanserin (ACP-103) competitively antagonizes the binding of [³H]ketanserin to heterologously expressed human 5-HT_2A receptors with a mean pK_i of 9.3 in membranes ａnd 9.70 in whole cells. Pimavanserin demonstrates lesser affinity (mean pK_i 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 lacked affinity ａnd functional activity at 5-HT_2B receptors, dopamine D₂ receptors, ａnd other human monoaminergic receptors. Pimavanserin (ACP-103) is highly selective for 5-HT_2A receptors, lacking affinity for other receptors in a broad profile screen including 65 different molecular targets; the only other receptor for which Pimavanserin demonstrates affinity is 5-HT_2C, ａnd Pimavanserin is approximately 30-fold selective for 5-HT_2A receptors over 5-HT_2C receptors depending on the assay.

In Vivo: Pimavanserin (ACP-103) is a potent, efficacious, orally active 5-HT_2A receptor inverse agonist with a behavioral pharmacological profile consistent with utility as an antipsychotic agent. Pimavanserin attenuates 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 reduces the hyperactivity induced in mice by the N-methyl-D-aspartate receptor noncompetitive antagonist 5H-dibenzo[a,d]cyclohepten-5,10-imine (dizocilpine maleate; MK-801) (0.1 ａnd 0.3 mg/kg s.c.; 3 mg/kg p.o.), consistent with a 5-HT_2A receptor mechanism of action in vivo ａnd antipsychotic-like efficacy. Pimavanserin demonstrates >42.6% oral bioavailability in rats.

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