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

@article{Wrigglesworth1996AnaloguesOC,
  title={Analogues of capsaicin with agonist activity as novel analgesic agents: structure-activity studies. 4. Potent, orally active analgesics.},
  author={Roger Wrigglesworth and Chris Walpole and Stuart Bevan and Elizabeth A. Campbell and Andy Dray and Glyn A Hughes and Iain F James and K J Masdin and Jon Winter},
  journal={Journal of medicinal chemistry},
  year={1996},
  volume={39 25},
  pages={4942-51}
}
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 had analgesic properties but poor oral activity, short duration of… CONTINUE READING

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