萨尔维诺林类似物及其κ-阿片受体活性综述。
A review of salvinorin analogs and their kappa-opioid receptor activity.
作者信息
Roach Jeremy J, Shenvi Ryan A
机构信息
Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
出版信息
Bioorg Med Chem Lett. 2018 May 15;28(9):1436-1445. doi: 10.1016/j.bmcl.2018.03.029. Epub 2018 Mar 12.
Abstract
The plant metabolite salvinorin A potently and selectively agonizes the human kappa-opioid receptor, an emerging target for next-generation analgesics. Here we review analogs of the salvinorin chemotype and their effects on selectivity, affinity and potency. Extensive peripheral modifications using isolated salvinorin A have delivered a trove of SAR information. More deep-seated changes are now possible by advances in chemical synthesis.
摘要
植物代谢产物萨尔维诺林A能有效且选择性地作用于人κ-阿片受体，这是新一代镇痛药的一个新兴靶点。在此，我们综述了萨尔维诺林化学型的类似物及其对选择性、亲和力和效力的影响。利用分离出的萨尔维诺林A进行广泛的外围修饰，已获得了大量的构效关系信息。现在，化学合成技术的进步使更深入的结构改变成为可能。
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