Pimavanserin

Pimavanserin is an inverse agonist of the serotonin (5-HT) receptor subtype 5-HT2A (IC50 = 1.86 nM, Ki = 0.5 nM). 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 (Cay-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 (Cay-10009019) in mice. Pimavanserin acts synergistically with haloperidol (Cay-12014) or risperidone (Cay-13629) to suppress (+)-MK-801-induced hyperactivity and attenuates haloperidol- and risperidone-induced catalepsy in rats. Formulations containing pimavanserin have been used for the treatment of psychosis in Parkinson's disease.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: (Request formulation change), A crystalline solid. Solubility: DMF: 33 mg/ml, DMSO: 33 mg/ml, Ethanol: 33 mg/ml, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 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.