A potent and selective agonist of M1 receptors (EC50 = 0.2 mM compared to >10 mM for M2-M5); induces concentration-dependent increases in Ca2+ mobilization and ERK1/2 phosphorylation in hM1 CHO cells (EC50s = 0.89 and 10 mM

VU0364572 (trifluoroacetate salt) – 5 mg

Brand:
Cayman
CAS:
1240514-89-9
Storage:
-20
UN-No:
Non-Hazardous - /

VU0364572 is a potent and selective agonist of the muscarinic acetylcholine receptor 1 (M1; EC50 = 0.2 mM compared to >10 mM for M2-M5).{37299} It induces concentration-dependent increases in Ca2+ mobilization and ERK1/2 phosphorylation in CHO cells transfected with the human M1 receptor (EC50s = 0.89 and 10 mM, respectively) with no effect on β-arrestin recruitment. VU0364572 also improves hippocampal-dependent spatial learning and localization abilities and acquistion of contextual fear learning but cannot reverse amphetamine-induced hyperlocomotion in rats. This suggests therapeutic potential of VU0364572 for the treatment of Alzheimer’s disease but not psychosis.{37300}  

 

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Description

A potent and selective agonist of M1 receptors (EC50 = 0.2 mM compared to >10 mM for M2-M5); induces concentration-dependent increases in Ca2+ mobilization and ERK1/2 phosphorylation in hM1 CHO cells (EC50s = 0.89 and 10 mM, respectively); improves hippocampal-dependent spatial learning and localization abilities and acquistion of contextual fear learning but cannot reverse amphetamine-induced hyperlocamotion in rats

Formal name: (3R)-3-[(2-methylbenzoyl)amino]-[1,4′-bipiperidine]-1′-carboxylic acid, ethyl ester, 2,2,2-trifluoroacetate

Synonyms: 

Molecular weight: 487.5

CAS: 1240514-89-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory

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