A positive allosteric modulator of the M4 muscarinic acetylcholine receptor; potentiates acetylcholine responses in CHO cells expressing M4 receptors (EC50s = 17.7

VU0467154 – 5 mg

Brand:
Cayman
CAS:
1451993-15-9
Storage:
-20
UN-No:
Non-Hazardous - /

VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor that potentiates acetylcholine responses in CHO cells expressing M4 receptors (EC50s = 17.7, 630, and 1,000 nM for rat, human, and cynomolgus monkey receptors, respectively).{41907} It is selective for M4 over M1-3 and M5 receptors and a panel of receptors, transporters, and cation channels when used at a concentration of 10 µM. In vivo, VU0467154 (3-56.6 mg/kg, p.o.) reverses amphetamine-induced hyperlocomotion in rats. It reverses MK-801-induced hyperlocomotion, deficits in a pairwise visual discrimination task, and impairments in the acquisition of contextual fear conditioning in wild-type, but not M4 knockout, mice. VU0467154 (3-30 mg/kg) also increases freezing behavior in contextual and tone fear conditioning tests in wild-type mice when administered prior to the conditioning session. Chronic administration of VU0467154 (10 mg/kg once daily) reduces motor incoordination and prevents decreases in locomotion in the YAC128 transgenic mouse model of Huntington’s disease.{41908}  

 

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Description

A positive allosteric modulator of the M4 muscarinic acetylcholine receptor; potentiates acetylcholine responses in CHO cells expressing M4 receptors (EC50s = 17.7, 630, and 1,000 nM for rat, human, and cynomolgus monkey receptors, respectively); selective for M4 over M1-3 and M5 receptors and a panel of receptors, transporters, and cation channels at 10 µM; reverses amphetamine-induced hyperlocomotion in rats from 3-56.6 mg/kg; reverses MK-801-induced hyperlocomotion, deficits in a pairwise visual discrimination task, and impairments in the acquisition of contextual fear conditioning in wild-type mice; increases freezing behavior in contextual and tone fear conditioning tests in wild-type mice when administered prior to the conditioning session from 3-30 mg/kg; reduces motor incoordination and prevents decreases in locomotion in the YAC128 transgenic mouse model of Huntington’s disease at 10 mg/kg

Formal name: 5-amino-3,4-dimethyl-N-[[4-[(trifluoromethyl)sulfonyl]phenyl]methyl]-thieno[2,3-c]pyridazine-6-carboxamide

Synonyms: 

Molecular weight: 444.5

CAS: 1451993-15-9

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory||Research Area|Neuroscience|Behavioral Neuroscience|Schizophrenia & Psychosis||Research Area|Neuroscience|Neurodegenerative Disorders|Huntington’s Disease

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