1290628-31-7

AZ 12216052 is a positive allosteric modulator of metabotropic glutamate receptor 8 (mGluR8). 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. 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.

AZ 12216052 is a positive allosteric modulator of mGluR8, which are attractive therapeutic targets for anxiety disorders.

mGlu8

[1] ROBERT M. DUVOISIN . Acute pharmacological modulation of mGluR8 reduces measures of anxiety[J]. Behavioural Brain Research, 2010, 212 2: Pages 168-173. DOI: 10.1016/j.bbr.2010.04.006
[2] D. JANTAS . 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[J]. Neuropharmacology, 2014, 83: Pages 36-53. DOI: 10.1016/j.neuropharm.2014.03.019