Discovery of a structurally novel opioid kappa-agonist derived from 4,5-epoxymorphinan.

@article{Nagase1998DiscoveryOA,
  title={Discovery of a structurally novel opioid kappa-agonist derived from 4,5-epoxymorphinan.},
  author={Hiroshi Nagase and Junko Hayakawa and Kuniaki Kawamura and Ken-ichi Kawai and Yuko Takezawa and Hirohide Matsuura and Choshin Tajima and Toyoshige Endo},
  journal={Chemical & pharmaceutical bulletin},
  year={1998},
  volume={46 2},
  pages={
          366-9
        }
}
A new type of kappa-agonist, 17-cyclopropylmethyl-3, 14 beta-dihydroxy-4,5 alpha-epoxy-6 beta-[N-methyl-trans-3-(3-furyl) acrylamido]morphinan hydrochloride (1, TRK-820), was discovered by a new working hypothesis. The "message-address concept" for opioid antagonists and the "accessory site" for general antagonists were applied to design TRK-820. A unique structural feature of TRK-820, which is different from other prototypical kappa-opioid receptor agonists, is the existence of the 4,5… CONTINUE READING

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