Bay 36-7620CAS号： 232605-26-4分子式： C19H18O2分子量： 278.35描述纯度储存/保存方法外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 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.. |
| 纯度 |
98%
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| 储存/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.
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| 基本信息 | |
| 外观 |
White solid
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| 可溶性/溶解性 |
Soluble in DMSO > 10 mM
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| 生物活性 | |
| 靶点 |
GPCRs
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| In vitro(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.
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| In vivo(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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分子结构图
