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匹莫范色林 /Pimavanserin 99%+

货号:A754938 同义名: ACP-103 Ambeed 开学季,买赠积分,赢豪礼

Pimavanserin is a potent and selective 5-HT2A receptor inverse agonist with mean pIC50 of with 8.7 in the cell-based functional assay.

Pimavanserin 化学结构 CAS号:706779-91-1
Pimavanserin 化学结构
CAS号:706779-91-1
Pimavanserin 3D分子结构
CAS号:706779-91-1
Pimavanserin 化学结构 CAS号:706779-91-1
Pimavanserin 3D分子结构 CAS号:706779-91-1
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Pimavanserin 纯度/质量文件 产品仅供科研

货号:A754938 标准纯度: 99%+
批次查询: 批次纯度:

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产品名称 5-HT 5-HT1 5-HT2 5-HT3 5-HT5 5-HT6 5-HT7 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

98%
Lamotrigine +

5-HT (human platelets), IC50: 240 μM

5-HT (rat brain synaptosomes), IC50: 474 μM

99%+
Venlafaxine 99%+
Fluvoxamine maleate 99%
Iloperidone 99%+
Ziprasidone HCl 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

98%
Dapoxetine HCl 99%+
Trazodone 98+%
Clomipramine HCl 99%+
Mirtazapine 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

99%+
Duloxetine 98+%
Sertraline HCl ++

5-HT, Ki: 13 nM

99%+
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

99%+
Latrepirdine 2HCl GluR 99%+
Fluoxetine hydrochloride 98%
Paroxetine hydrochloride AChR 99%+
BMY 7378 ++

5-HT1A, pIC50: 6.4

5-HT1D, pIC50: 5.9

+

5-HT2, pIC50: 5.5

97%
Flibanserin +++

5-HT1A, Ki: 1 nM

+

5-HT2A, Ki: 49 nM

98%
LY310762 +

5-HT1D, Ki: 249 nM

99%+
Cyclobenzaprine HCI 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

99%+
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

99+%
Olanzapine 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

99%
Ketanserin +++

5-HT2C (Rat), Ki: 50 nM

5-HT2C (Human), Ki: 2.5 nM

99%+
Loxapine succinate ++

5-HT2 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 nM

99%
Agomelatine 99%+
Clozapine 99%+
Amitriptyline +

5-HT2, Ki: 235 nM

SERT 98%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

98+%
RS-127445 ++++

5-HT2B, pIC50: 10.4

5-HT2B, pKi: 9.5

99%+
Sarpogrelate HCl ++++

5-HT2A, Kd: 2.1 nM

5-HT2C, Kd: 1.1 nM

98%
Tropisetron 99%
Palonosetron 98+%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

99%+
Ondansetron 99%
Granisetron 98%
Alosetron HCl 98%
Ondansetron hydrochloride dihydrate 99%+
VUF10166 ++++

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

99%+
Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

98%
Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

++++

5-HT2A, pKi: 9.75

5-HT2C, pKi: 10.46

+++

5-HT5A, pKi: 8.84

++++

5-HT6, pKi: 9.6

++++

5-HT7, pKi: 9.94

99%+
Risperidone ++

5-HT1D, Ki: 84.6 nM

5-HT1B, Ki: 14.9 nM

++++

5-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 nM

+

5-HT5A, Ki: 206 nM

++

5-HT7, Ki: 6.6 nM

99%+
SB 271046 HCl +++

5-HT6, pKi: 8.92

99%+
Intepirdine ++++

5-HT6, pKi: 9.63

99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

98+%
BRL 15572 ++

5-HT1B, pKi: 6.1

5-HT1D, pKi: 6

++

5-HT2A, pKi: 6.6

5-HT2B, pKi: 6.2

+

5-HT6, pKi: 5.9

+

5-HT7, pKi: 6.3

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Pimavanserin 生物活性

描述 Pimavanserin is a potent and selective 5-HT2A receptor inverse agonist with mean pIC50 of with 8.7 in the cell-based functional assay.

Pimavanserin 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00086294 Parkinson's Disease ... 展开 >> Dyskinesias 收起 << Phase 2 Completed - United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 收起 <<
NCT03152292 - Recruiting September 2021 -
NCT00087542 Hallucinations ... 展开 >> Psychoses Parkinson's Disease 收起 << Phase 2 Completed - United States, California ... 展开 >> Fountain Valley, California, United States, 92708 Sunnyvale, California, United States, 94089 United States, Connecticut Danbury, Connecticut, United States, 06810 United States, Florida Pompano Beach, Florida, United States, 33060 Tampa, Florida, United States, 33606 United States, Georgia Atlanta, Georgia, United States, 30329 United States, Kansas Kansas City, Kansas, United States, 66160 United States, Maryland Elkridge, Maryland, United States, 21075 United States, New York Albany, New York, United States, 12205 United States, North Carolina Asheville, North Carolina, United States, 28806 United States, Pennsylvania Philadelphia, Pennsylvania, United States, 19107 United States, Rhode Island Pawtucket, Rhode Island, United States, 02860 United States, Tennessee Brentwood, Tennessee, United States, 37027 收起 <<

Pimavanserin 参考文献

[1]Vanover KE, Betz AJ, 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.

[2]Vanover KE, Weiner DM, et al. Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phen ylmethyl) 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.

Pimavanserin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.69mL

2.34mL

1.17mL

23.39mL

4.68mL

2.34mL

Pimavanserin 技术信息

CAS号706779-91-1
分子式C25H34FN3O2
分子量 427.555
别名 ACP-103
运输蓝冰
存储条件

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(116.94 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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