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Natural Products for the Treatment of Pain: Chemistry and Pharmacology of Salvinorin A, Mitragynine, and Collybolide
Biochemistry ( IF 2.9 ) Pub Date : 2020-09-15 , DOI: 10.1021/acs.biochem.0c00629
Soumen Chakraborty 1, 2 , Susruta Majumdar 1, 2
Affiliation  

Pain remains a very pervasive problem throughout medicine. Classical pain management is achieved through the use of opiates belonging to the mu opioid receptor (MOR) class, which have significant side effects that hinder their utility. Pharmacologists have been trying to develop opioids devoid of side effects since the isolation of morphine from papaver somniferum, more commonly known as opium by Sertürner in 1804. The natural products salvinorin A, mitragynine, and collybolide represent three nonmorphinan natural product-based targets, which are potent selective agonists of opioid receptors, and emerging next-generation analgesics. In this work, we review the phytochemistry and medicinal chemistry efforts on these templates and their effects on affinity, selectivity, analgesic actions, and a myriad of other opioid-receptor-related behavioral effects.

中文翻译:

用于治疗疼痛的天然产物:Salvinorin A、帽柱木碱和 Collybolide 的化学和药理学

疼痛在整个医学领域仍然是一个非常普遍的问题。传统的疼痛管理是通过使用属于 μ 阿片受体 (MOR) 类的阿片类药物来实现的,这些药物具有显着的副作用,阻碍了它们的应用。自从从罂粟中分离出吗啡以来,药理学家一直在尝试开发无副作用的阿片类药物,在 1804 年被 Sertürner 更普遍地称为鸦片。天然产物 salvinorin A、帽柱木碱和 collybolide 代表三个非吗啡喃类天然产物靶点,它们是阿片受体的强效选择性激动剂,也是新兴的下一代镇痛药。在这项工作中,我们回顾了这些模板的植物化学和药物化学工作及其对亲和力、选择性、镇痛作用和无数其他阿片受体相关行为影响的影响。
更新日期:2020-09-15
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