Title of article :
Design, synthesis, and structure–activity relationship of novel opioid κ-agonists Original Research Article
Author/Authors :
Koji Kawai، نويسنده , , Jun Hayakawa، نويسنده , , Toru Miyamoto، نويسنده , , Yoshifumi Imamura، نويسنده , , Shinichi Yamane، نويسنده , , Hisanori Wakita، نويسنده , , Hideaki Fujii، نويسنده , , Kuniaki Kawamura، نويسنده , , Hirotoshi Matsuura، نويسنده , , Naoki Izumimoto، نويسنده , , Ryosuke Kobayashi، نويسنده , , Takashi Endo، نويسنده , , Hiroshi Nagase، نويسنده ,
Abstract :
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.
Keywords :
Opioid , ?-agonist , Analgesic , Antipruritus , Message-address
