mGluR5 modulator 1

mGluR5 modulator 1 is a mGluR5 positive allosteric modulator. mGluR5 modulator 1 can be used for the research of the schizophrenia and cognitive impairments[1].

Signaling Pathways >> GPCR/G Protein >> mGluR

Research Areas >> Neurological Disease

mGluR5[1]

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 Ca2+ 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 Ca2+ mobilization (pKB=5.4 and 5.3, respecyively), inositol monophosphate accumulation, and ERK1/2 phosphorylation signaling (pKB=5.88 and 5.4, respecyively) assays in HEK293A-mGlu5-low cells[1]. mGluR5 modulator 1 enhances the effect of DHPG in cortical neurons with pEC50 values of 6.32 and 6.33 in Ca2+ mobilization and inositol monophosphate (IP1) accumulation assays[1].

[1]. Arsova A, et al. Positive Allosteric Modulators of Metabotropic Glutamate Receptor 5 as Tool Compounds to Study Signaling Bias. Mol Pharmacol. 2021 May;99(5):328-341.