1261171-52-1

1261171-52-1 structure

1261171-52-1 structure

Name: mGluR5 modulator 1
Chemical Name: mGluR5 modulator 1
CAS Number: 1261171-52-1
Molecular Formula: C₁₈H₁₉ClFN₃O₂
Molecular Weight: 363.81
Catalog: Signaling Pathways GPCR/G Protein mGluR
Create Date: 2022-03-12 09:52:52
Modify Date: 2024-01-14 20:47:21
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].

Name	mGluR5 modulator 1

Description	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].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> mGluR Research Areas >> Neurological Disease
Target	mGluR5[1]
In Vitro	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].
References	[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.

Molecular Formula	C₁₈H₁₉ClFN₃O₂
Molecular Weight	363.81