Discovery of a Structurally Novel Opioid. KAPPA.-Agonist Derived from 4, 5-Epoxymorphinan.

…, Y TAKEZAWA, H MATSUURA, C TAJIMA…

Index: Nagase, Hiroshi; Hayakawa, Jun; Kawamura, Kuniaki; Kawai, Kouji; Takezawa, Yuko; Matsuura, Hirotoshi; Tajima, Chiko; Endo, Takashi Chemical and Pharmaceutical Bulletin, 1998 , vol. 46, # 2 p. 366 - 369

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Citation Number: 124

Abstract

A new type of K-agonist, 17-cyclopropylmethyl-3, 14β-dihydroxy-4, 5α-epoxy-6β-[N-methyl- trans-3-(3-furyl) acrylamido] morphinan hydrochloride (1, TRK-820), was discoverd 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 K-opioid receptor agonists, is ...