VU0155041 sodium salt

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VU0155041 sodium salt manufacturers

VU0155041 sodium salt Basic information
Product Name:VU0155041 sodium salt
Synonyms:VU0155041 sodium salt;cis-2-[[(3,5-Dichlorophenyl)amino]carbonyl]cyclohexanecarboxylicacidsodiumsalt;VU0155041 sodium;VU-0155041 sodium,VU0155041 sodium;VU0155041 sodium salt, PAM for mGluR4
CAS:1259372-69-4
MF:C14H15Cl2NO3.Na
MW:339.17
EINECS:
Product Categories:Glutamate
Mol File:1259372-69-4.mol
VU0155041 sodium salt Structure
VU0155041 sodium salt Chemical Properties
storage temp. Desiccate at RT
solubility DMSO: 1 mg/ml; PBS (pH 7.2): 2 mg/ml
form Powder
Water Solubility Soluble to 25 mM in water
Safety Information
MSDS Information
VU0155041 sodium salt Usage And Synthesis
DescriptionVU0155041 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. 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 and reverses askinesias induced by reserpine in rat models of Parkinson’s disease. Chronic treatment with VU0155041 restores social behavior in the Oprm-/- mouse model of autism. It also increases the percentage of time spent in the open arms of the elevated plus maze, a measure of decreased anxiety, in mice.
UsesVU 0155041 Sodium Salt is a positive allosteric modulator of group III mGlu4 receptor that provides functional neuprotection in 6-hydroxydopamine rat models with parkinson’s disease.
in vivo

VU0155041 (31 nmol, 93 nmol; i.c.v.) reverses catalepsy induced by the dopamine D2 receptor antagonist Haloperidol (1.5 mg/kg, i.p.) in rats[1].
VU0155041 (93 nmol, 316 nmol; i.c.v.) reverses Reserpine (HY-N0480) -induced akinesia in rats[1].

Animal Model:Third ventricle cannulated (TVC) Male Sprague-Dawley rats (225-255 g)[1]
Dosage:31, 93 nmol
Administration:I.c.v. injection after the the 1.5 mg/kg of haloperidol treatment 2 h
Result:Decreased the cataleptic effects of haloperidol, and the effects still presented 30 min after infusion.
IC 50mGluR4: 693 nM (EC50)
References[1] COLLEEN M NISWENDER. Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4.[J]. Molecular Pharmacology, 2008, 74 5: 1345-1358. DOI: 10.1124/mol.108.049551
[2] JéRME AJ BECKER. Autistic-Like Syndrome in Mu Opioid Receptor Null Mice is Relieved by Facilitated mGluR4 Activity[J]. Neuropsychopharmacology, 2014, 39 9: 2049-2060. DOI: 10.1038/npp.2014.59
[3] ROBERT M. DUVOISIN . Opposing roles of mGluR8 in measures of anxiety involving non-social and social challenges[J]. Behavioural Brain Research, 2011, 221 1: Pages 50-54. DOI: 10.1016/j.bbr.2011.02.049
VU0155041 sodium salt Preparation Products And Raw materials
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