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ID: ALA1142487

Journal: Bioorg Med Chem

Title: Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.

Authors: Kawai K, Hayakawa J, Miyamoto T, Imamura Y, Yamane S, Wakita H, Fujii H, Kawamura K, Matsuura H, Izumimoto N, Kobayashi R, Endo T, Nagase H.

Abstract: By focusing on 4,5-epoxymorphinan, a traditional opioid skeleton but a new structure in the opioid kappa-agonist research field, and by rationally applying the 'message-address concept' and 'accessory site hypothesis,' we discovered a new chemical class opioid kappa-agonist, TRK-820 (1). Its development as an antipruritus is now in the final stage. Here, the full scope of its design, synthesis, and structure-activity relationship are described.

CiteXplore: 18829333

DOI: 10.1016/j.bmc.2008.09.011