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5940215 
Journal Article 
Discovery of conolidine derivative DS39201083 as a potent novel analgesic without mu opioid agonist activity 
Arita, T; Asano, M; Kubota, K; Domon, Y; Machinaga, N; Shimada, K 
2019 
Yes 
Bioorganic & Medicinal Chemistry Letters
ISSN: 0960-894X
EISSN: 1464-3405 
29 
15 
1938-1942 
English 
31147104 
WOS:000471750200015 
We discovered a novel compound, 5-methyl-1,4,5,7-tetrahydro-2,5-ethanoazocino[4,3-b]indol-6(3H)-one sulfuric acid salt (DS39201083), which was formed by derivatization of a natural product, conolidine. DS39201083 had a unique bicyclic skeleton and was a more potent analgesic than conolidine, as revealed in the acetic acid-induced writhing test and formalin test in ddY mice. The compound showed no agonist activity at the mu opioid receptor.