AZ 12216052 is a positive allosteric modulator of metabotropic glutamate receptor 8 (mGluR8).1 It potentiates glutamate-induced [35S]GTPγS binding in GHEK cells expressing human mGluR8b (EC50 = 1 μM). In a cell-based model of Parkinson's disease, AZ 12216052 inhibits MPP+-induced decreases in the viability of undifferentiated SH-SY5Y cells when used at concentrations ranging from 0.001 to 1 μM and in retinoic acid-differentiated SH-SY5Y cells at 0.1 and 1 μM.2 AZ 12216052 (10 mg/kg) increases the time spent in the open areas of the elevated zero maze and reduces the acoustic startle response in mice, indicating anxiolytic-like activity in response to avoidable and unavoidable anxiogenic stimuli, respectively.1
|1. Duvoisin, R.M., Pfankuch, T., Wilson, J.M., et al. Acute pharmacological modulation of mGluR8 reduces measures of anxiety. Behav. Brain Res. 212(2), 168-173 (2010).|2. Jantas, D., Greda, A., Golda, S., et al. Neuroprotective effects of metabotropic glutamate receptor group II and III activators against MPP(+)-induced cell death in human neuroblastoma SH-SY5Y cells: The impact of cell differentiation state. Neuropharmacology 83, 36-53 (2014).