152658-01-0Relevant academic research and scientific papers
Design, synthesis, and structure-activity relationship of novel opioid κ-agonists
Kawai, Koji,Hayakawa, Jun,Miyamoto, Toru,Imamura, Yoshifumi,Yamane, Shinichi,Wakita, Hisanori,Fujii, Hideaki,Kawamura, Kuniaki,Matsuura, Hirotoshi,Izumimoto, Naoki,Kobayashi, Ryosuke,Endo, Takashi,Nagase, Hiroshi
, p. 9188 - 9201 (2008)
By focusing on 4,5-epoxymorphinan, a traditional opioid skeleton but a new structure in the opioid κ-agonist research field, and by rationally applying the 'message-address concept' and 'accessory site hypothesis,' we discovered a new chemical class opioid κ-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.
