Bay 36-7620

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抑制剂描述：

产品名称：Bay 36-7620

产品别名：见爱必信官网

英文别名：Bay 36-7620

靶点：GPCRs

CAS：232605-26-4

纯度：98%

外观：见爱必信官网

保存方法：Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

描述：

代谢型谷氨酸(mGlu)受体是G-蛋白偶联受体(GPCR),其作用主要是作为突触传递的调节剂,在许多生理和病理过程中发挥作用.BAY36-7620是强效的非竞争性mGlu1受体拮抗剂.. 

溶解性：Soluble in DMSO > 10 mM

体外研究：

BAY36-7620 is a potent and selective antagonist at mGlu1receptors and inhibits >60% of mGlu1a receptor constitutive activity (IC50 = 0.38 μM). BAY36-7620 is thus the first described mGlu1 receptor inverse agonist. Moreover, BAY36-7620 did not displace the [3H]quisqualate binding from the Glu-binding pocket, indicating that BAY36-7620 is a noncompetitive mGlu1 antagonist.

体内研究：BAY 36-7620 protected against pentylenetetrazole-induced convulsions in the mouse. As assessed in rats, BAY 36-7620 was devoid of the typical side effects of the ionotropic glutamate (iGlu) receptor antagonists phencyclidine and MK-801. Therefore, BAY 36-7620 did not disrupt sensorimotor gating, induce phencyclidine-like discriminative effects or stereotypical behavior, or facilitate intracranial self-stimulated behavior.

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