VU0155041

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

IC 50

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