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A review of salvinorin analogs and their kappa-opioid receptor activity
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-03-12 , DOI: 10.1016/j.bmcl.2018.03.029 Jeremy J Roach 1 , Ryan A Shenvi 1
中文翻译：
萨尔维诺林类似物及其κ阿片受体活性的综述
更新日期：2018-03-12
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-03-12 , DOI: 10.1016/j.bmcl.2018.03.029 Jeremy J Roach 1 , Ryan A Shenvi 1
Affiliation
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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.
中文翻译：
萨尔维诺林类似物及其κ阿片受体活性的综述
植物代谢物 salvinorin A 有效且选择性地激动人类kappa -阿片受体，这是下一代镇痛药的新兴靶标。在这里，我们回顾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。使用分离的 Salvinorin A 进行广泛的外周修饰，提供了大量的 SAR 信息。现在，化学合成的进步使得更深层的改变成为可能。
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