Chemical Name: 5-[2-(2-(3-Fluorophenyl)ethynyl]-N-[(1R)-2-hydroxy-1,2-dimethylpropyl]-2-pyridinecarboxamide
Biological ActivityPotent mGlu5 positive allosteric modulator (EC50 = 1.5 nM) and agonist (EC50 = 171 nM; maximum effect is 65% that of glutamate). Binds allosteric site with high affinity (Ki = 11.8 nM). Increases maximum response to glutamate by 30%. Exhibits bias towards signaling via IP1 and ERK1/2 over iCa2+ in HEK293 and neuronal cells, and activates Gs in HEK 293 cells. Induces epileptiform activity in CA3 hippocampal neurons in vitro and convulsions in vivo.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity.
Rook et al.
Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery.
Sengmany et al.
Direct coupling of detergent purified human mGlu5 receptor to the heterotrimeric G proteins Gq and Gs.
Nasrallah et al.
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