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Submit ReviewPimavanserin
说明： Selective 5-HT2A inverse agonist
化学名： N-[(4-Fluorophenyl)methyl]-N-(1-methyl-4-piperidinyl)-N'-[[4-(2-methylpropoxy)phenyl]methyl]urea
纯度： ≥98% (HPLC)
生物活性 for Pimavanserin
Pimavanserin (also known as ACP-103) is a selective, potent 5-HT2A receptor inverse agonist (IC50 = 2 nM). Pimavanserin displays ~ 40-fold higher affinity for 5-HT2A over 5-HT2C receptor. Chronic administration of Pimavanserin, suppresses amyloid-β production and improves anxiety-related behavior and memory in Alzheimer's disease mouse models. Pimavanserin shows protective effects on midbrain dopaminergic neurons in a rat model of Parkinson's Disease.
化合物库 for Pimavanserin
Pimavanserin is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for Pimavanserin
| 分子量 | 427.56 |
| 公式 | C25H34FN3O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 706779-91-1 |
| PubChem ID | 10071196 |
| InChI Key | RKEWSXXUOLRFBX-UHFFFAOYSA-N |
| Smiles | O=C(NCC1=CC=C(OCC(C)C)C=C1)N(CC2=CC=C(F)C=C2)C3CCN(C)CC3 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Pimavanserin
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 21.38 | 50 | |
| ethanol | 42.76 | 100 |
制备储备液 for Pimavanserin
以下数据基于产品分子量 427.56。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.34 mL | 11.69 mL | 23.39 mL |
| 5 mM | 0.47 mL | 2.34 mL | 4.68 mL |
| 10 mM | 0.23 mL | 1.17 mL | 2.34 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.47 mL |
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产品说明书 for Pimavanserin
参考文献 for Pimavanserin
参考文献是支持产品生物活性的出版物。
Snigdha et al (2010) Attenuation of phencyclidine-induced object recognition deficits by the combination of atypical antipsychotic drugs and pimavanserin (ACP 103), a 5-hydroxytryptamine(2A) receptor inverse agonist. J.Pharmacol.Exp.Ther. 332 622 PMID: 19864614
Yuede et al (2021) Pimavanserin, a 5HT 2A receptor inverse agonist, rapidly suppresses A beta production and related pathology in a mouse model of Alzheimer's disease. J.Neurochem. 156 658 PMID: 33278025
Gras Lavigne et al (2021) Pimavanserin promotes trophic factor release and protects cultured primary dopaminergic neurons exposed to MPP+ in a GDNF-dependent manner. ACS Chem.Neurosci. 12 2088 PMID: 34032411
Vanover et al (2006) 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-hydroxytryptam J.Pharmacol.Exp.Ther. 317 910 PMID: 16469866
If you know of a relevant reference for Pimavanserin, please let us know.
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关键词: Pimavanserin, Pimavanserin supplier, Potent, selective, high, affinity, 5-HT2A, agonists, receptors, serotonin, ACP-103, agonism, Receptors, 7667, Tocris Bioscience
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.