VU 0155041

VU0155041 is a potent, selective and mixed allosteric agonist/positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 is a partial agonist of mGluR4 that activates the receptor by interacting with a site that is distinct from the glutamate binding site[1].

Signaling Pathways >> GPCR/G Protein >> mGluR

Research Areas >> Neurological Disease

Human mGlu4:798 nM (EC50)

Rat mGlu4:693 nM (EC50)

VU0155041 (30 μM) causes 6.4-fold and 4.7-fold leftward shifts in the glutamate CRC at human and rat mGluR4, respectively[1]. VU0155041 (10 μM) does not affect NMDA receptor currents in striatal medium spiny neurons[1].

VU0155041 (31 nM, 93 nM; i.c.v.) reverses catalepsy induced by the dopamine D2 receptor antagonist haloperidol in rats[1]. VU0155041 (93 nM , 316 nM; i.c.v.) reverses reserpine-induced akinesia in rats[1]. Animal Model: Third ventricle cannulated (TVC) Male Sprague-Dawley rats (225-255 g)[1] Dosage: 31 nM, 93 nM 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.

[1]. Niswender CM, et, al. Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. Mol Pharmacol. 2008 Nov; 74(5): 1345-58.