A selective positive allosteric modulator of mGluR4 (EC50 = 2.5 μM in a thallium flux assay); has no effect on radioligand binding at 67 G protein-coupled receptors

VU0155041 (sodium salt) – 50 mg

Brand:
Cayman
CAS:
1259372-69-4
Storage:
-20
UN-No:
Non-Hazardous - /

VU0155041 is a positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4) with an EC50 value of 2.5 μM for glutamate response in a thallium flux assay.{37088} It is selective for mGluR4, exhibiting no effect on radioligand binding at 67 G protein-coupled receptors, ion channels, and transporters, and lacking antagonist activity at NMDA receptors in striatal medium spiny neurons at a concentration of 10 μM. In vivo, VU0155041 decreases catalepsy induced by haloperidol (Item No. 12014) and reverses askinesias induced by reserpine (Item No. 16474) in rat models of Parkinson’s disease. Chronic treatment with VU0155041 restores social behavior in the Oprm-/- mouse model of autism.{37089} It also increases the percentage of time spent in the open arms of the elevated plus maze, a measure of decreased anxiety, in mice.{37090}  

 

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Description

A selective positive allosteric modulator of mGluR4 (EC50 = 2.5 μM in a thallium flux assay); has no effect on radioligand binding at 67 G protein-coupled receptors, ion channels, and transporters; lacks antagonist activity at NMDA receptors in striatal medium spiny neurons at a concentration of 10 μM; decreases haloperidol-induced catalepsy and reverses reserpine-induced askinesias in rat models of Parkinson’s disease; restores social behavior in the Oprm-/- mouse model of autism; decreases anxiety-like behavior in the elevated plus maze in mice

Formal name: (1R,2S)-rel-2-[[(3,5-dichlorophenyl)amino]carbonyl]-cyclohexanecarboxylic acid, monosodium salt

Synonyms: 

Molecular weight: 338.2

CAS: 1259372-69-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease

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