Discovery of conolidine derivative DS39201083 as a potent novel analgesic without mu opioid agonist activity.
Bioorg Med Chem Lett
; 29(15): 1938-1942, 2019 08 01.
Article
em En
| MEDLINE
| ID: mdl-31147104
ABSTRACT
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.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Receptores Opioides mu
/
Alcaloides Indólicos
/
Analgésicos Opioides
Limite:
Animals
Idioma:
En
Ano de publicação:
2019
Tipo de documento:
Article