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Pimavanserin

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。

TargetMol的所有产品仅用作科学研究或药证申报,不能被用于人体,我们不向个人提供产品和服务。请您遵守承诺用途,不得违反法律法规规定用于任何其他用途。
Pimavanserin Chemical Structure
Pimavanserin, CAS 706779-91-1
规格 价格/CNY 货期 数量
1 mg ¥ 176 现货
5 mg ¥ 297 现货
10 mg ¥ 479 现货
25 mg ¥ 987 现货
50 mg ¥ 1,490 待询
1 mL * 10 mM (in DMSO) ¥ 327 现货
其他形式的 Pimavanserin:
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
产品目录号及名称: Pimavanserin (T2076)
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纯度: 98%
纯度: 97.84%
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参考文献
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) competitively antagonizes the binding of [3H]ketanserin to heterologously expressed human 5-HT2A receptors with a mean pKi of 9.3 in membranes and 9.70 in whole cells. Pimavanserin demonstrates lesser affinity (mean pKi 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-HT2C receptors, and lacked affinity and functional activity at 5-HT2B receptors, dopamine D2 receptors, and other human monoaminergic receptors[1]. Pimavanserin (ACP-103) is highly selective for 5-HT2A 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-HT2C, and Pimavanserin is approximately 30-fold selective for 5-HT2A receptors over 5-HT2C receptors depending on the assay[2].
体内活性 Pimavanserin (ACP-103) is a potent, efficacious, orally active 5-HT2A 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-HT2A 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-HT2A receptor mechanism of action in vivo and antipsychotic-like efficacy. Pimavanserin demonstrates >42.6% oral bioavailability in rats[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

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TargetMol Library Books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.
lumateperone Tosylate Phenylbiguanide Wf-516 Lurasidone hydrochloride Bromperidol Flumexadol Desvenlafaxine Dolasetron Mesylate

相关化合物库

该产品包含在如下化合物库中:
药物功能重定位化合物库 抗癌上市药物库 神经退行性疾病化合物库 抗癌药物库 GPCR靶点分子库 抗癌临床化合物库 膜蛋白靶向化合物库 ReFRAME 相关化合物库 上市药物库 已知活性化合物库

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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。

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Keywords

Pimavanserin 706779-91-1 GPCR/G Protein Neuroscience 5-HT Receptor inhibit Serotonin Receptor ACP103 ACP-103 匹莫范色林 Inhibitor ACP 103 5-hydroxytryptamine Receptor inhibitor

 

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