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.

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mGlu8

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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[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.

In Vitro: DMSO : 100 mg/mL (254.87 mM; Need ultrasonic)配制储备液