A 5-HT2A inverse agonist (IC50 = 1.86 nM; Ki = 0.5 nM); selective for 5-HT2A over a panel of 65 ion channels

Pimavanserin – 5 mg

Brand:
Cayman
CAS:
706779-91-1
Storage:
-20
UN-No:
Non-Hazardous - /

Pimavanserin is an inverse agonist of the serotonin (5-HT) receptor subtype 5-HT2A (IC50 = 1.86 nM; Ki = 0.5 nM).{36250} 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.{36251} Formulations containing pimavanserin have been used for the treatment of psychosis in Parkinson’s disease.{36252}  

 

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Description

A 5-HT2A inverse agonist (IC50 = 1.86 nM; Ki = 0.5 nM); selective for 5-HT2A over a panel of 65 ion channels, enzymes, and receptors (Kis = >100 nM); reduces DOI-induced head-twitch behavior and prepulse inhibition deficits in rats at doses of 3 mg/kg, p.o. and 1-10 mg/kg, s.c., respectively; exhibits antipsychotic-like activity, reducing (+)-MK-801-induced hyperactivity in mice; acts synergistically with haloperidol or risperidone to suppress (+)-MK-801-induced hyperactivity and attenuates haloperidol- and risperidone-induced catalepsy in rats

Formal name: N-[(4-fluorophenyl)methyl]-N-(1-methyl-4-piperidinyl)-N’-[[4-(2-methylpropoxy)phenyl]methyl]-urea

Synonyms: 

Molecular weight: 427.6

CAS: 706779-91-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Inverse Agonists||Research Area|Neuroscience|Behavioral Neuroscience|Schizophrenia & Psychosis||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease

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