Pimavanserin

Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.

Product Specifications

CAS Number

[706779-91-1]

Product Name Alternative

ACP-103

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

5-HT Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/pimavanserin.html

Purity

99.86

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

CC(C)COC1=CC=C(CNC(N(CC2=CC=C(F)C=C2)C3CCN(C)CC3)=O)C=C1

Molecular Formula

C25H34FN3O2

Molecular Weight

427.55

Precautions

H302, H315, H319, H335

References & Citations

[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. 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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

5-HT2 Receptor; α-1 microglobulin

Citation 01

ACS Chem Neurosci. 2019 Nov 20;10 (11) :4476-4491. |bioRxiv. 2020 Feb.|Department Neuroscience. Virginia Commonwealth University. 2016 Oct.|Int J Clin Exp Med. 2019;12 (8) :10342-10349|Int J Neuropsychopharmacol. 2021 Sep 21;24 (9) :749-757.|J Med Chem. 2023 Jul 13;66 (13) :9057-9075.|Patent. US20200352950A1.|Proc Natl Acad Sci U S A. 2020 Oct 20;117 (42) :26438-26447.|Sci Rep. 2024 Jan 16;14 (1) :1396.|bioRxiv. 2023 Jul 31:2023.07.29.551106.|Food Chem Toxicol. 2023 Jun:176:113800.|Nat Commun. 2023 Dec 15;14 (1) :8221.