VU0155041

Product NameVU0155041
CAS1093757-42-6
MFC14H15Cl2NO3
MW316.18
EINECS
MOL File1093757-42-6.mol

Chemical Properties

Boiling point	540.2±50.0 °C(Predicted)
Density	1.429±0.06 g/cm3(Predicted)
storage temp.	Store at RT
solubility	Soluble to 100 mM in 1eq. NaOH and to 100 mM in DMSO
form	white powder
pka	4.48±0.44(Predicted)
color	Pale purple to purple
InChI	1S/C14H15Cl2NO3/c15-8-5-9(16)7-10(6-8)17-13(18)11-3-1-2-4-12(11)14(19)20/h5-7,11-12H,1-4H2,(H,17,18)(H,19,20)/t11-,12+/m0/s1
InChIKey	VSMUYYFJVFSVCA-NWDGAFQWSA-N
SMILES	OC(=O)[C@@H]1CCCC[C@@H]1C(=O)Nc2cc(Cl)cc(Cl)c2

Safety Information

Hazard Codes	Xn
Risk Statements	22
WGK Germany	3
Storage Class	11 - Combustible Solids
Hazard Classifications	Acute Tox. 4 Oral

Usage And Synthesis

Uses

Acts as an allosteric modulator (PAM) of mGluR4, part of the class of receptors influencing Parkinson’s disease and it’s expression.

Biological Activity

VU0155041 is a mixed allosteric agonist/positive allosteric modulator (PAM) of mGluR4. VU0155041 is approximately 8-fold more potent than PHCCC and does not show any significant potentiator or antagonist activity at other mGluR subtypes. It is soluble in an aqueous vehicle and intracerebroventricular administration of 31-316 nmol of VU0155041 dose-dependently decreased haloperidol-induced catalepsy and reserpine-induced akinesia in rats. VU0155041 exhibits selectivity for mGluR4 relative to 67 different targets and does not affect the function of striatal NMDA receptors.', 'VU0155041 is a positive allosteric modulator of the metabotropic glutamate receptor subtype 4. It also shows some direct agonist activity, but at a site different from the glutamate binding site. /VU0155041 is approximately 8-fold more potent than PHCCC and enhances the activity of glutamate also about 8-fold. It shows promising anti-Parkinsonian effects in animal models of Parkinsonμs 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 nnmol, 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 nmol, 93 nmol (10 μL)
Administration:	Intracerebroventrical injection, after the Haloperidol (1.5 mg/kg) treatment 2 hours
Result:	Decreased the cataleptic effects of Haloperidol, and the effects still presented 30 min after infusion.

IC 50

Human mGlu₄: 798 nM (EC₅₀); Rat mGlu₄: 693 nM (EC₅₀)

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