Discovery of conolidine derivative DS39201083 as a potent novel analgesic without mu opioid agonist activity

[Display omitted] 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 c...

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Published inBioorganic & medicinal chemistry letters Vol. 29; no. 15; pp. 1938 - 1942
Main Authors Arita, Tsuyoshi, Asano, Masayoshi, Kubota, Kazufumi, Domon, Yuki, Machinaga, Nobuo, Shimada, Kousei
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier Ltd 01.08.2019
Elsevier
Subjects
Acetic acid writhing test
Analgesic
Chemistry
Chemistry, Medicinal
Chemistry, Organic
Conolidine
Indole alkaloid
Life Sciences & Biomedicine
Non-opioid
Pharmacology & Pharmacy
Physical Sciences
Science & Technology
Non-opioid
Analgesic
Conolidine
Indole alkaloid
Acetic acid writhing test
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Summary:[Display omitted] 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.
Bibliography:ObjectType-Article-1
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ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2019.05.045