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].

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 (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-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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

363.81

C₁₈H₁₉ClFN₃O₂

1261171-52-1

FC1=CC(Cl)=CC=C1N2CCN(C(COCC3=CC=NC=C3)=O)CC2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]