| CAS |
No.706782-28-7 |
| 中文名称 |
匹莫范色林 |
| 英文名称 |
Pimavanserin tartrate |
| 分子式 |
C25H34FN3O2·1/2C4H6O6 |
| 分子量 |
502.59 |
| 溶解性 |
Soluble in DMSO ≥8mg/mL;Soluble in Water ≥5mg/mL |
| 纯度 |
≥98% |
| 外观(性状) |
White to off-white Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 |
冷藏运输 |
| 靶点 |
5-HT Receptor |
| 通路 |
Neuronal Signaling;GPCR & G Protein |
| 背景说明 |
是一种有效的 5-HT 2A 受体反向激动剂，可用于治疗帕金森病相关的精神错乱的研究。 |
| 生物活性 |
Pimavanserin (ACP-103) hemitartrate is a potent 5-HT 2A receptor inverse agonist with pIC50 and pKi of 8.73 and 9.3， respectively.[1] |
| IC50 |
5-HT2A Receptor 8.73 (pIC50) 5-HT2A Receptor 9.3 (pKi)[1] |
| In Vitro |
Pimavanserin hemitartrate 竞争性拮抗 [3H]ketanserin 与异源表达的人 5-HT 2A 受体的结合，膜中的平均 pKi 为 9.3，全细胞中的平均 pKi 为 9.70。Pimavanserin hemitartrate 在基于细胞的功能测定受体选择和扩增技术 (R-SAT) 中显示出有效的反向激动剂活性，平均 pIC50 为 8.7。Pimavanserin hemitartrate 表现出较低的亲和力 (膜中平均 pKi 为 8.80，全细胞中为 8.00，由放射性配体结合确定) 和作为反向激动剂的效力 (平均 pIC50 7.1 在 R-SAT 中) 对人 5-HT 2C 受体的作用，对 5-HT 2B 受体、多巴胺 D2 受体和其他人单胺能受体缺乏亲和力和功能活性[1]。 |
| In Vivo |
Pimavanserin hemitartrate 减弱大鼠中由 5-HT2A 受体激动剂诱导的头部抽搐行为 (3 mg/kg po) 和前脉冲抑制缺陷 (1-10 mg/kg sc) 并减少小鼠中由 N-甲基诱导的多动症-D-天冬氨酸受体非竞争性拮抗剂，符合 5-HT 2A 受体体内作用机制和抗精神病药样功效。Pimavanserin hemitartrate 在大鼠中表现出 42.6% 的口服生物利用度[1]。 |
| 动物实验 |
Rats: Thirty minutes before being placed in the startle apparatus， rats are treated with saline (s.c.)， MDL-100，151 (1.0 mg/kg s.c.)， or one of three doses of ACP-103 (1.0， 3.0， or 10.0 mg/kg s.c.). Five minutes after the pretreatment， rats are administered either DOI HCl (0.5 mg/kg s.c.) or 0.9% saline (s.c.). The acoustic startle session lasted approximately 37 min. After 1 week， rats are tested again in the same acoustic/tactile startle session in the exact order and at the same time as the previous week. The same pretreatment drug or vehicle is administered， and rats are crossed over to receive the treatment opposite to that they received the previous week (e.g.， DOI HCl for week 1， 0.9% saline for week 2)[1]. Mice: Non-Swiss albino mice are used for locomotor activity experiments. For determination of spontaneous activity， ACP-103 is administered alone (s.c. 60 min before session start or p.o. 60 min before session start). For hyperactivity experiments， mice are treated with 0.3 mg/kg MK-801 (i.p.) 15 min presession (the peak dose for producing hyperactivity in an inverted-U dose-effect curve as determined in pilot experiments) in combination with vehicle or ACP-103. Motor activity data are collected during a 15-min session in a lit room[1] |
| 数据来源文献 |
[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. |
| 规格 |
1mg 5mg 10mg 25mg 50mg 100mg 200mg |
| 单位 |
瓶 |
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