Pimavanserin

Product Name:Pimavanserin

Synonyms:Pimavanserin;1-(4-Fluorobenzyl)-3-(4-isobutoxybenzyl)-1-(1-methylpiperidin-4-yl)urea;PIMAVANSERIN/1-(4-FLUOROBENZYL)-3-(4-ISOBUTOXYBENZYL)-1-(1-METHYLPIPERIDIN-4-YL)UREA;Unii-jz963p0dik;Pimavamserin;1-[(4-fluorophenyl)Methyl]-1-(1-Methylpiperidin-4-yl)-3-{[4-(2-Methylpropoxy)phenyl]Methyl}urea;N-(4-Fluorobenzyl)-N-(1-Methylpiperidin-4-yl)-N'-[[4-(2-Methylpropyloxy)phenyl]Methyl]carbaMide;N-[(4-Fluorophenyl)Methyl]-N-(1-Methyl-4-piperidinyl)-N'-[[4-(2-Methylpropoxy)phenyl]Methyl]urea; Unii-jz963p0dik;Nuplazid;N-[(4-Fluorophenyl)Methyl]-N-(1-Methyl-4-piperidinyl)-N'-[[4-(2-Methylpropoxy)phenyl]Methyl]urea;1-[(4-fluorophenyl)Methyl]-1-(1-Methylpiperidin-4-yl)-3-{[4-(2-Methylpropoxy)phenyl]Methyl}urea;N-(1-methylpiperidin-4-yl)-N-(4-fluorophenylmethyl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide;1-(4-fluorobenzyl)-3-(4-isobutoxybenzyl)-1-(1-methylpiperidin-4-yl)urea;N-(4-Fluorobenzyl)-N-(1-Methylpiperidin-4-yl)-N'-[[4-(2-Methylpropyloxy)phenyl]Methyl]carbaMide;1-(4-fluoro-benzyl)-3-(4-isobutoxy-benzyl)-1-(1-methyl-piperidin-4-yl)-urea;N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamide;N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-isobutoxybenzyl)carbamide;Pimavamserin;

CAS:706779-91-1

MF:C25H34FN3O2

MW:427.55

EINECS:1806241-263-5

Product Categories:Intermediates & Fine Chemicals;Pharmaceuticals;Inhibitors

Mol File:706779-91-1.mol

HS Code:29339900

PSA:44.81000

LogP:4.99530

Appearance & Physical State:Pale Yellow to Pale Orange Solid

Density:1.15±0.1 g/cm3 (calc.)

Boiling Point:604.2±55.0 °C (760 mmHg, calc.)

Melting Point:100-103 ºC

Flash Point:319.222ºC

Place of Origin:China

Type:API

Grade Standard:Food Grade, Tech Grade, Pharma Grade

Purity:99% min

Appearance:White to off-white solid powder

COA:Availale

Packaging Details:

1) 1kg with plastic container inside/Aluminum foil bag outside. 

2) 25kg with double plastic container inside/Fiber drum outside. 

3) As your request

Storage condition: Store in cool & dry place. Keep away from strong light and heat.

Usage: Mainly used in Pharmaceutical Intermediates/medical intermediate/research purpose

Uses:Drug used in the treatment of Parkinson disease psychosis. Drug used in the treatment of Parkinson’s disease psychosis.

Pimavanserin (INN), or pimavanserin tartate (USAN), marketed under the trade name Nuplazid, is a non-dopaminergic atypical antipsychotic developed by Acadia Pharmaceuticals for the treatment of Parkinson's disease psychosis and schizophrenia. Pimavanserin has a unique mechanism of action relative to other antipsychotics, behaving as a selective inverse agonist of the serotonin 5-HT2A receptor, with 40-fold selectivity for this site over the 5-HT2C receptor and no significant affinity or activity at the 5-HT2B receptor or dopamine receptors. The drug has met expectations for a Phase III clinical trial for the treatment of Parkinson's disease psychosis, and has completed Phase II trials for adjunctive treatment of schizophrenia alongside an antipsychotic medication.

Pimavanserin is expected to improve the effectiveness and side effect profile of antipsychotics. The results of a clinical trial examining the efficacy, tolerability and safety of adjunctive pimavanserin to risperidone and haloperidol were published in November 2012, and the results showed that pimavanserin potentiated the antipsychotic effects of subtherapeutic doses of risperidone and improved the tolerability of haloperidol treatment by reducing the incidence of extrapyramidal symptoms.

On September 2, 2014, the United States Food and Drug Administration granted Breakthrough Therapy status to Acadia's New Drug Application for pimavanserin. It was approved by the FDA to treat hallucinations and delusions associated with psychosis experienced by some people with Parkinson's disease on April 29, 2016.

Chemical Properties:Yellow Solid

Definition ChEBI: A member of the class of ureas in which three of the four hydrogens are replaced by 4-fluorobenzyl, 1-methylpiperidin-4-yl, and 4-(isopropyloxy)benzyl groups. An atypical antipsychotic that is used (in the form of its tartrate salt) for treatment of halluc nations and delusions associated with Parkinson's disease.

Enzyme inhibitor This orally active atypical non-dopaminergic antipsychotic[ (FWfree-base = 427.56 g/mol; CAS 706779-91-1 (free base) and 706782-28-7 (tartrate salt)), also known as ACP-103, Nuplazid? and N-(4-fluorophenylmethyl)- N-(1-methyl-piperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenyl-methyl)carbamide, is a potent inverse agonist and antagonist at serotonin 5-HT2A receptors (Ki = 0.087 nM) and less so at serotonin 5-HT2C receptors (Ki = 0.44 nM). Pimavanserin shows low binding to σ1 receptors (Ki = 120 nM), with no appreciable affinity (Ki > 300 nM) to serotonin 5-HT2B, dopaminergic (including D2), muscarinic, histaminergic, or adrenergic receptors, or to calcium channels. 5-HT2A receptor dysregulation is implicated in both the etiology and treatment of schizophrenia, and the same receptor plays an active role in the regulation of sleep architecture. Nuplazid is specifically indicated in its FDA approval (April, 2016) for the treatment of hallucinations and delusions associated with Parkinson disease. Significantly, 5-HT2A serotonin receptor antagonists differentially regulate 5-HT2A receptor protein level in vivo. See also Ketanserin; RH-34; Risperidone; Ritanserin; Setoperone; Volinanserin.