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内源性大麻素

内源性大麻素

作者: Annie大讲堂 | 来源:发表于2020-02-23 20:36 被阅读0次

有证据表明,内源性大麻素的代谢作用是由外周组织的CB1受体介导的。虽然之前产生CB1受体阻滞剂的尝试已经产生了严重的神经精神副作用,但美国国立卫生研究院的发明家已经发现了一种化合物,它可以阻断脑外显率降低的CB1受体。此外,其中一些化合物对诱导型一氧化氮合酶(iNOS)也有直接抑制作用,而另一组化合物直接激活AMP激酶。这些双靶点化合物可能用于治疗代谢疾病和相关疾病,如肥胖和糖尿病及其并发症,包括肝或肾纤维化,而没有危险的副作用。
There is evidence that the metabolic effects of endocannabinoids are mediated by CB1 receptors in peripheral tissues. While prior attempts at generating CB1 receptor blockers have had serious neuropsychiatric side effects, inventors at NIH have discovered compounds that block CB1 receptors with reduced brain penetrance. In addition, some of these compounds also have a direct inhibitory effect on inducible nitric oxide synthase (iNOS), whereas another group of the compounds directly activates AMP kinas. These dual-target compounds may be useful for treating metabolic disease and related conditions such as obesity and diabetes and their complications, including liver or kidney fibrosis, without the dangerous the side effects.

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