| 靶点: |
mGlu8 |
| 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. |
| 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. |
| 参考文献: |
1. Reed BT, et al. Differential modulation of retinal ganglion cell light responses by orthosteric and allosteric metabotropic glutamate receptor 8 compounds. Neuropharmacology. 2013 Apr;67:88-94.
2. Jantas D, et al. Allosteric and Orthosteric Activators of mGluR8 Differentially Affect the Chemotherapeutic-Induced Human Neuroblastoma SH-SY5Y Cell Damage: The Impact of Cell Differentiation State. Basic Clin Pharmacol Toxicol. 2018 Oct;123(4):443-451.
3. Duvoisin RM, et al. Acute pharmacological modulation of mGluR8 reduces measures of anxiety. Behav Brain Res. 2010 Oct 15;212(2):168-73.
4. Duvoisin RM, et al. Opposing roles of mGluR8 in measures of anxiety involving non-social and social challenges. Behav Brain Res. 2011 Aug 1;221(1):50-4. |
| 溶解性: |
soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.549 ml |
12.744 ml |
25.487 ml |
| 5 mM |
0.51 ml |
2.549 ml |
5.097 ml |
| 10 mM |
0.255 ml |
1.274 ml |
2.549 ml |
| 50 mM |
0.051 ml |
0.255 ml |
0.51 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |