Pimavanserin tartrate
(Synonyms: 匹莫范色林L-酒石酸盐,ACP-103 hemitartrate) 目录号 : GC36919
A 5-HT2A inverse agonist
Cas No.:706782-28-7
Sample solution is provided at 25 µL, 10mM.
Pimavanserin is an inverse agonist of the serotonin (5-HT) receptor subtype 5-HT2A (IC50 = 1.86 nM; Ki = 0.5 nM).1 It is selective for 5-HT2A over a panel of 65 ion channels, enzymes, and receptors (Kis = >100 nM). Pimavanserin reduces head-twitch behavior and prepulse inhibition deficits induced by the 5-HT2A receptor agonist DOI in rats at doses of 3 mg/kg, p.o. and 1-10 mg/kg, s.c., respectively. It also exhibits antipsychotic-like activity, reducing hyperactivity induced by (+)-MK-801 in mice. Pimavanserin acts synergistically with haloperidol or risperidone to suppress (+)-MK-801-induced hyperactivity and attenuates haloperidol- and risperidone-induced catalepsy in rats.2 Formulations containing pimavanserin have been used for the treatment of psychosis in Parkinson's disease.3
1.Vanover, K.E., Weiner, D.M., Makhay, M., 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-hydroxytryptamine2A receptor inverse agonistJ. Pharmacol. Exp. Ther.318(2)910-918(2006) 2.Gardell, L.R., Vanover, K.E., Pounds, L., et al.ACP-103, a 5-hydroxytryptamine 2A receptor inverse agonist, improves the antipsychotic efficacy and side-effect profile of haloperidol and risperidone in experimental modelsJ. Pharmacol. Exp. Ther.322(2)862-870(2007) 3.Goldman, J.G., and Holden, S.Treatment of psychosis and dementia in Parkinson's diseaseCurr. Treat. Options. Neurol.16(3)281(2014)
Animal experiment: |
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] |
References: [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. |
Cas No. | 706782-28-7 | SDF | |
别名 | 匹莫范色林L-酒石酸盐,ACP-103 hemitartrate | ||
Canonical SMILES | O=C(NCC1=CC=C(OCC(C)C)C=C1)N(CC2=CC=C(F)C=C2)C3CCN(C)CC3.O=C(O)[C@H](O)[C@@H](O)C(O)=O.O=C(NCC4=CC=C(OCC(C)C)C=C4)N(CC5=CC=C(F)C=C5)C6CCN(C)CC6 | ||
分子式 | C54H74F2N6O10 | 分子量 | 502.59 |
溶解度 | DMSO: ≥ 75 mg/mL (74.61 mM) | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
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1 mg | 5 mg | 10 mg |
1 mM | 1.9897 mL | 9.9485 mL | 19.8969 mL |
5 mM | 0.3979 mL | 1.9897 mL | 3.9794 mL |
10 mM | 0.199 mL | 0.9948 mL | 1.9897 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
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