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Submit ReviewPimavanserin
Description: Selective 5-HT2A inverse agonist
Chemical Name: N-[(4-Fluorophenyl)methyl]-N-(1-methyl-4-piperidinyl)-N'-[[4-(2-methylpropoxy)phenyl]methyl]urea
Purity: ≥98% (HPLC)
Biological Activity 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.
Compound Libraries for Pimavanserin
Pimavanserin is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Pimavanserin
| M. Wt | 427.56 |
| Formula | C25H34FN3O2 |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Pimavanserin
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 21.38 | 50 | |
| ethanol | 42.76 | 100 |
Preparing Stock Solutions for Pimavanserin
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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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Product Datasheets for Pimavanserin
References for Pimavanserin
References are publications that support the biological activity of the product.
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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Keywords: Pimavanserin, Pimavanserin supplier, Potent, selective, high, affinity, 5-HT2A, agonists, receptors, serotonin, ACP-103, agonism, Receptors, 7667, Tocris Bioscience
Citations for Pimavanserin
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.