产品
编 号:F111444
分子式:C19H22BrNOS
分子量:392.35
产品类型
结构图
CAS No: 1290628-31-7
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生物活性:
AZ 12216052 is a mGluR8 positive allosteric modulator, and helps mGluR8 modulate signaling inputing to retinal ganglion cells. AZ 12216052 exhibits antianxiety effect.
体内研究:
AZ 12216052 (10 mg/kg; i.p.; 2 h prior to testing) reduces measures of anxiety, without affecting the velocity of the mice.AZ12216052 (10 mg/kg; i.p.; single dose) exhibits remaining anxiolytic effects, might involve mGluR4 in mGluR8?/? mice, as the mGluR4 PAM (Positive Allosteric Modulator) VU 0155041 also reduces measures of anxiety in wild-type mice.Animal Model:WT and Apolipoprotein E-deficient (Apoe?/?) mice (C57BL/6J, 2-month-old) in the elevated zero maze
Dosage:10 mg/kg
Administration:Intraperitoneal injection; singel dose, 2 h prior to testing
Result:Reduced measures of anxiety in the elevated zero maze without affecting the velocity of the mice.Reduced the acoustic startle response.
体外研究:
mGluR8 may modulates the synaptic inputs to retinal ganglion cells.AZ 12216052 (10 μM) enhances the peak excitatory currents of ON-, OFF- currents in ON-OFF-ganglion cells, with a dependent way on the intensity of the light stimuli.AZ 12216052 shows impact of cell differentiation and (0.01-1 μM; 24-48 h) reduces Dox-induced human neuroblastoma SH-SY5Y cell damage partially.AZ 12216052 stimulates proliferation and attenuates staurosporine (St)- and doxorubicin (Dox)-induced toxicity in UN-SH-SY5Y cells.AZ12216052 (10 μM) enhances glutamate activity of human mGluR8b receptor expressed in GHEK cells.