A 5-HT2A inverse agonist
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Pimavanserin

Item No. 23462

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(4-fluorophenyl)methyl]-N-(1-methyl-4-piperidinyl)-N'-[[4-(2-methylpropoxy)phenyl]methyl]-urea
CAS Number
706779-91-1
Molecular Formula
C25H34FN3O2
Formula Weight
427.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 33 mg/mlDMSO: 33 mg/mlEthanol: 33 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
λmax
226 nm
SMILES
FC1=CC=C(CN(C2CCN(C)CC2)C(NCC3=CC=C(OCC(C)C)C=C3)=O)C=C1
InChi Code
InChI=1S/C25H34FN3O2/c1-19(2)18-31-24-10-6-20(7-11-24)16-27-25(30)29(23-12-14-28(3)15-13-23)17-21-4-8-22(26)9-5-21/h4-11,19,23H,12-18H2,1-3H3,(H,27,30)
InChi Key
RKEWSXXUOLRFBX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    10 mg

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    25 mg

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    50 mg

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    Product Description

    Pimavanserin is an inverse agonist of the serotonin (5-HT) receptor subtype 5-HT2A (IC50 = 1.86 nM; Ki = 0.5 nM).1 It is selective for 5-HT2A over a panel of 65 ion channels, enzymes, and receptors (Kis = >100 nM). Pimavanserin reduces head-twitch behavior and prepulse inhibition deficits induced by the 5-HT2A receptor agonist DOI (Item No. 13885) in rats at doses of 3 mg/kg, p.o. and 1-10 mg/kg, s.c., respectively. It also exhibits antipsychotic-like activity, reducing hyperactivity induced by (+)-MK-801 (Item No. 10009019) in mice. Pimavanserin acts synergistically with haloperidol (Item No. 12014) or risperidone (Item No. 13629) to suppress (+)-MK-801-induced hyperactivity and attenuates haloperidol- and risperidone-induced catalepsy in rats.2 Formulations containing pimavanserin have been used for the treatment of psychosis in Parkinson's disease.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Vanover, K.E., Weiner, D.M., Makhay, M., 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-hydroxytryptamine2A receptor inverse agonist. J. Pharmacol. Exp. Ther. 318(2), 910-918 (2006).

    2. Gardell, L.R., Vanover, K.E., Pounds, L., et al. ACP-103, a 5-hydroxytryptamine 2A receptor inverse agonist, improves the antipsychotic efficacy and side-effect profile of haloperidol and risperidone in experimental models. J. Pharmacol. Exp. Ther. 322(2), 862-870 (2007).

    3. Goldman, J.G., and Holden, S. Treatment of psychosis and dementia in Parkinson’s disease. Curr. Treat. Options. Neurol. 16(3), 281 (2014).