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Pimavanserin

产品编号 T2076 CAS 706779-91-1

别名: ACP-103, 匹莫范色林

Pimavanserin (ACP-103) 是特异性的 5-HT2A 受体反向激动剂，在基于细胞的功能测定中，平均 pIC50值为8.7。它是非典型抗精神病药，用于治疗帕金森病患者的幻觉和精神病。

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Pimavanserin, CAS 706779-91-1

规格	价格/CNY	货期
1 mg	￥ 176	现货
5 mg	￥ 297	现货
10 mg	￥ 479	现货
25 mg	￥ 892	现货
50 mg	￥ 1,360	待询
100 mg	￥ 1,980	待询
1 mL * 10 mM (in DMSO)	￥ 327	现货

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其他形式的 Pimavanserin:

Pimavanserin tartrate
现货
Pimavanserin-d3
询价

选择批次

纯度: 98%

纯度: 97.84%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Pimavanserin (ACP-103)(ACP-103) is an effective and specific 5-HT2A receptor inverse agonist (mean pIC50: 8.7, in the cell-based functional assay). Pimavanserin is an atypical antipsychotic used in the treatment of hallucinations and psychosis in patients with Parkinson disease.
靶点活性	5-HT2A:8.7(pIC50)
体外活性	Pimavanserin (ACP-103) 在异源表达的人类5-HT2A受体上与[3H]ketanserin的结合发生竞争性拮抗作用，其平均pKi值在膜中为9.3，在整个细胞中为9.70。 Pimavanserin 对人类5-HT2C受体显示出较低的亲和力（膜中平均pKi为8.80，整个细胞中为8.00，通过放射配体结合测定）和作为反向激动剂的效力较低（R-SAT中平均pIC50为7.1），并且在5-HT2B受体、多巴胺D2受体和其他人类单胺受体上缺乏亲和力和功能活性[1]。 Pimavanserin (ACP-103) 对5-HT2A受体具有高度选择性，对其他受体缺乏亲和力，这些受体在包括65种不同分子靶标的广泛筛选中；Pimavanserin 唯一显示出亲和力的其他受体是5-HT2C，根据测验，Pimavanserin 对5-HT2A受体的选择性大约是对5-HT2C受体的30倍[2]。
体内活性	Pimavanserin（ACP-103）是一种强效、有效、口服活性的5-HT2A受体逆向激动剂，具有与抗精神病化合物效用一致的行为药理学特征。Pimavanserin 减轻由5-HT2A受体激动剂（±）-2,5-二甲氧基-4-碘苯丙胺 hydrochloride 在大鼠中诱发的头摆行为（3 mg/kg p.o.）和预脉冲抑制缺损（1-10 mg/kg s.c.），并减轻由N-甲基-D-天冬氨酸受体非竞争性拮抗剂5H-二苯并[a,d]环庚烯-5,10-亚胺（dizocilpine maleate; MK-801）在小鼠中诱发的过动行为（0.1 和 0.3 mg/kg s.c.; 3 mg/kg p.o.），这与5-HT2A受体作用机制在体内和类似抗精神病化合物的效用一致。Pimavanserin 在大鼠中展示出>42.6%的口服生物利用度[1]。
激酶实验	For the membrane binding, NIH-3T3 cells are grown to 70% confluence in 15 cm2 dishes and transfected with 10 μg of receptor plasmid DNA using Polyfect transfection reagent. Two days after transfection, cells expressing the desired serotonin receptor are homogenized in 20 mM HEPES/10 mM EDTA and spun down at 11,000 g at 4°C for 30 min. The supernatant is discarded, and the pellet is resuspended in 20 mM HEPES/1 mM EDTA and spun down at the same setting. The pellet is then resuspended in 20 mM HEPES/0.5 mM EDTA, and membranes are used for binding assays. Bradford analysis is used to determine total membrane protein. Kd and Bmax values are derived from 12-point concentration experiments using 1 nM [3H]ketanserin for the 5-HT2A receptor and 3 nM [3H]mesulergine for the 5-HT2B and 5-HT2C receptors. Membranes are incubated at room temperature for 3 h with various concentrations of test ligand in the presence of a fixed concentration of radioligand. The suspension is filtered as explained below for whole-cell binding, washed with ice-cold buffer, and dried, and radioactivity is determined using TopCount[1].
细胞实验	Pimavanserin (ACP-103) is dissolved in DMSO and stored, and then diluted with appropriate media before use[1]. For the whole-cell binding, 6 million human embryonic kidney 293T cells are plated in 10-cm dishes and transfected with 5 μg of plasmid DNA using Polyfect. Two days after transfection, cells are harvested with 10 mM EDTA, washed, and resuspended in binding buffer (1× DMEM with 0.1% bovine serum albumin). Then, 60,000 cells transfected with the 5-HT2A receptor or 20,000 cells transfected with the 5-HT2C-INI receptor are incubated at 37°C for 3 h in the presence of 5 nM radioligand ([3H]ketanserin for 5-HT2A receptors and [3H]mesulergine for 5-HT2C-INI receptors) and varying concentrations of ligands (total volume 100 μL in a 96-well plate). Cells are filtered onto a 96-well GF/B filter plate and washed with 300 mL of wash buffer (25 mM HEPES, 1 mM CaCl2, 5 mM MgCl2, and 0.25 M NaCl) using a Filtermate 196 harvester. The filter plates are dried under a heat lamp before addition of 50 μL of scintillation fluid to each well. Plates are counted on a TopCount. Separately, the hydrochloride salt form of Pimavanserin (10 μM) is evaluated at MDS Pharma Services for activity in a broad screen of radioligand binding assays at 65 different receptors[1].

别名	ACP-103, 匹莫范色林
分子量	427.55
分子式	C25H34FN3O2
CAS No.	706779-91-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 60 mg/mL (140.33 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3389 mL	11.6945 mL	23.3891 mL	58.4727 mL
	5 mM	0.4678 mL	2.3389 mL	4.6778 mL	11.6945 mL
	10 mM	0.2339 mL	1.1695 mL	2.3389 mL	5.8473 mL
	20 mM	0.1169 mL	0.5847 mL	1.1695 mL	2.9236 mL
	50 mM	0.0468 mL	0.2339 mL	0.4678 mL	1.1695 mL
	100 mM	0.0234 mL	0.1169 mL	0.2339 mL	0.5847 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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参考文献

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 inver 2. Vanover KE, et al. A 5-HT2A receptor inverse agonist, ACP-103, reduces tremor in a rat model and levodopa-induced dyskinesias in a monkey model. Pharmacol Biochem Behav. 2008 Oct;90(4):540-4.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

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每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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