Analogues of capsaicin with agonist activity as novel analgesic agents: structure-activity studies. 4. Potent, orally active analgesics

…, GA Hughes, I James, KJ Masdin, J Winter

文献索引：Wrigglesworth, Roger; Walpole, Christopher S. J.; Bevan, Stuart; Campbell, Elizabeth A.; Dray, Andy; Hughes, Glyn A.; James, Iain; Masdin, Kay J.; Winter, Janet Journal of Medicinal Chemistry, 1996 , vol. 39, # 25 p. 4942 - 4951

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被引用次数: 61

摘要

Structural features of three regions of the capsaicin molecule necessary for agonist properties were delineated by a previously reported modular approach. These in vitro agonist effects were shown to correlate with analgesic potency in rodent models. Combination of optimal structural features from each of these regions of the capsaicin molecule have led to highly potent agonists (eg, 1b). Evaluation in vivo established that 1b ...