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Pimavanserin hemitartrate

CAS No. : 706782-28-7

MCE 站：Pimavanserin hemitartrate

产品活性：Pimavanserin (ACP-103) hemitartrate 是一种有效的 5-HT 2A 受体反向激动剂，pIC₅₀ 和 pK_i 值分别为8.73和9.3。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

In Vitro: Pimavanserin hemitartrate 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 hemitartrate 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 hemitartrate 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 lacks affinity ａnd functional activity at 5-HT 2B receptors, dopamine D2 receptors, ａnd other human monoaminergic receptors.

In Vivo: Pimavanserin hemitartrate 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 hemitartrate demonstrates 42.6% oral bioavailability in rats.

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