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
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