Pimavanserin

Name: Pimavanserin
Brand: Tocris Bioscience
SKU: 7667

Tocris Bioscience, part of Bio-Techne | Catalog # 7667

COA / SDS

Selective 5-HT2A inverse agonist

Key Product Details

Description:	Selective 5-HT_2A inverse agonist
Chemical Name:	N-[(4-Fluorophenyl)methyl]-N-(1-methyl-4-piperidinyl)-N'-[[4-(2-methylpropoxy)phenyl]methyl]urea
Purity:	≥98% (HPLC)
Molecular Weight:	427.56

View Full Technical Details for Pimavanserin

Technical Data
Citations

Biological Activity for Pimavanserin

Pimavanserin (also known as ACP-103) is a selective, potent 5-HT_2A receptor inverse agonist (IC₅₀ = 2 nM). Pimavanserin displays ~ 40-fold higher affinity for 5-HT_2A over 5-HT_2C 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 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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Reconstitution Calculator

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References for Pimavanserin

References are publications that support the biological activity of the product.

Vanover 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. 2006 PMID: 16469866
Yuede 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. 2021 PMID: 33278025
Gras Lavigne Pimavanserin promotes trophic factor release and protects cultured primary dopaminergic neurons exposed to MPP⁺ in a GDNF-dependent manner. ACS Chem.Neurosci. 2021 PMID: 34032411
Snigdha 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. 2010 PMID: 19864614