AZ12216052

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AZ 12216052 是一种 mGluR8 正变结构调节剂，帮助 mGluR8 调节视网膜神经节细胞的信号输入。AZ 12216052 具有抗焦虑作用。

AZ 12216052 is a mGluR8 positive allosteric modulator, and helps mGluR8 modulate signaling inputing to retinal ganglion cells. AZ 12216052 exhibits antianxiety effect.

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.Cell Viability Assay Cell Line:UN- and RA-SH-SY5Y cells Concentration:0.01-1 μM Incubation Time:48 hours Result:Increased cell viability at 0.1 μM, and protected undifferentiated neuroblastoma cells against damaging effects of Iri or Cis.

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.

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Cell Cycle/DNA Damage

GPR

GPR

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1290628-31-7

392.35

C19H22BrNOS

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (254.87 mM; 超声助溶 )

CCC(C)c1ccc(NC(=O)CSCc2ccc(Br)cc2)cc1

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(-20℃)

With Ice Pack

≥ 2 years