mGluR5 modulator 1 is a compound that acts as a positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5). Its primary application lies in the field of schizophrenia and cognitive impairment research.

mGluR5 modulator 1 (compound 2c; 0.1-0.00001 nM) potentiates the L-glutamate and DHPG responses to the same maximum response as the orthosteric agonists alone in the Ca 2+ mobilization and IP1 accumulation assays[1]. mGluR5 modulator 1 (0.1-0.00001 nM) potentiates the L-glutamate and DHPG responses above the orthosteric agonist maximal response in the ERK1/2 phosphorylation assay[1]. mGluR5 modulator 1 induces mGlu5 internalization in the absence of add orthosteric agonist or antagonist[1]. mGluR5 modulator 1 potentiates the responses induced by both orthosteric agonists (L-glutamate or DHPG) in Ca 2+ mobilization (pK B =5.4 and 5.3, respecyively), inositol monophosphate accumulation, and ERK1/2 phosphorylation signaling (pK B =5.88 and 5.4, respecyively) assays in HEK293A-mGlu 5 -low cells[1]. mGluR5 modulator 1 enhances the effect of DHPG in cortical neurons with pEC 50 values of 6.32 and 6.33 in Ca 2+ mobilization and inositol monophosphate (IP1) accumulation assays[1].