Pimavanserin

• CAT Number: I004649
• CAS Number: 706779-91-1
• Molecular Formula: C25H34FN3O2
• Molecular Weight: 427.55
• Purity: 98%
• Synonyms: 1-(4-fluorobenzyl)-3-(4-isobutoxybenzyl)-1-(1-methylpiperidin-4-yl)urea
• Target: HTR2A
• Target Protein: P28223
• Solubility: 10 mM in DMSO
• Appearance: Solid
• Storage: Dry, dark and at 2 - 8 °C for six months or -20°C for two years.
• IC50: 5-HT2A Receptor:8.7 (pIC50)
• IUPAC Name: 1-[(4-fluorophenyl)methyl]-1-(1-methylpiperidin-4-yl)-3-[[4-(2-methylpropoxy)phenyl]methyl]urea
• InChI: 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)
• InChIKey: RKEWSXXUOLRFBX-UHFFFAOYSA-N
• SMILES: CC(C)COC1=CC=C(C=C1)CNC(=O)N(CC2=CC=C(C=C2)F)C3CCN(CC3)C

Pimavanserin（Cat No.:I004649）is an atypical antipsychotic primarily used to treat hallucinations and delusions associated with Parkinson’s disease psychosis. It works by selectively targeting serotonin 5-HT2A receptors without significantly affecting dopamine receptors, which makes it unique compared to traditional antipsychotics. This selective mechanism allows pimavanserin to reduce psychotic symptoms without worsening motor symptoms, a common issue in Parkinson’s patients. Its favorable side effect profile and effectiveness in managing psychosis make it a valuable treatment option, particularly for individuals who cannot tolerate the motor side effects of other antipsychotic medications.

Reference

[1]. Vanover KE, 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-hydroxytryptamine(2A) receptor inverse agonist. J Pharmacol Exp Ther. 2006 May;317(2):910-8.

[2]. Vanover KE, et al. Pharmacokinetics, tolerability, and safety of ACP-103 following single or multiple oral dose administration in healthy volunteers. J Clin Pharmacol. 2007 Jun;47(6):704-14.

[3]. Vanover KE, et al. A 5-HT2A receptor inverse agonist, ACP-103, reduces tremor in a rat model and levodopa-induced dyskinesias in a monkey model. Pharmacol Biochem Behav. 2008 Oct;90(4):540-4.