AZ12216052 explained

AZ-12216052 is a drug which acts as a potent and selective positive allosteric modulator of the metabotropic glutamate receptor 8, and is used for research into the role of this receptor subtype in various processes including anxiety and neuropathic pain.^{[1] [2] [3] [4] [5]}

Notes and References

1. Duvoisin RM, Pfankuch T, Wilson JM, Grabell J, Chhajlani V, Brown DG, Johnson E, Raber J . 6 . Acute pharmacological modulation of mGluR8 reduces measures of anxiety . Behavioural Brain Research . 212 . 2 . 168–173 . October 2010 . 20385173 . 10.1016/j.bbr.2010.04.006 . 2892883 .
2. Reed BT, Morgans CW, Duvoisin RM . Differential modulation of retinal ganglion cell light responses by orthosteric and allosteric metabotropic glutamate receptor 8 compounds . Neuropharmacology . 67 . 88–94 . April 2013 . 23164615 . 10.1016/j.neuropharm.2012.09.023 . 3562428 .
3. Rossi F, Marabese I, De Chiaro M, Boccella S, Luongo L, Guida F, De Gregorio D, Giordano C, de Novellis V, Palazzo E, Maione S . 6 . Dorsal striatum metabotropic glutamate receptor 8 affects nocifensive responses and rostral ventromedial medulla cell activity in neuropathic pain conditions . Journal of Neurophysiology . 111 . 11 . 2196–2209 . June 2014 . 24304862 . 10.1152/jn.00212.2013 .
4. Jantas D, Greda A, Leskiewicz M, Grygier B, Pilc A, Lason W . Neuroprotective effects of mGluR II and III activators against staurosporine- and doxorubicin-induced cellular injury in SH-SY5Y cells: New evidence for a mechanism involving inhibition of AIF translocation . Neurochemistry International . 88 . 124–137 . September 2015 . 25661514 . 10.1016/j.neuint.2014.12.011 . 8865211 .
5. Jantas D, Grygier B, Zatorska J, Lasoń W . Allosteric and Orthosteric Activators of mGluR8 Differentially Affect the Chemotherapeutic-Induced Human Neuroblastoma SH-SY5Y Cell Damage: The Impact of Cell Differentiation State . Basic & Clinical Pharmacology & Toxicology . 123 . 4 . 443–451 . October 2018 . 29753314 . 10.1111/bcpt.13041 . 21666589 . free .