Functional selectivity induced by mGlu4 receptor positive allosteric modulation and concomitant activation of Gq coupled receptors

Article ID	Journal	Published Year	Pages	File Type
5815003	Neuropharmacology	2013	11 Pages	PDF

Abstract

âº Convergent activation of H1 and mGlu4 receptors induces biased signaling. âº Potentiation by signaling convergence is synergistic with small molecule PAMs. âº PAMs exhibit functional selectivity in the presence of signaling convergence.

Keywords

GPCR 7TMR DMSO G-protein-coupled receptor Functional selectivity Cho Chinese Hamster Ovary CNS dihydrofolate reductase Dimethyl sulfoxide central nervous system Allosteric modulator Histamine glutamate Receptor mGlu receptor Metabotropic glutamate receptor