VU 0424465 |
| Catalog No.GC50598 |
Potent mGlu5 positive allosteric modulator and agonist; binds allosteric site with high affinity
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1428630-85-6
Sample solution is provided at 25 µL, 10mM.
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Potent 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.
Rook et al (2013) Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity. Biol.Psychiatry. 73 501 PMID:23140665 |Sengmany et al (2017) Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery. Neuropharmacology 115 60 PMID:27392634 |Nasrallah et al (2018) Direct coupling of detergent purified human mGlu5 receptor to the heterotrimeric G proteins Gq and Gs. Sci.Rep. 8 4407 PMID:29535347
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
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