Article: article d'un périodique ou d'un magazine.
Interaction of 3,8-diazabicyclo (3.2.1) octanes with mu and delta opioid receptors
Pharmacological Research Communications
Date de publication
In Vitro Journal Article --- Old month value: May
A series of 3,8-diazabicyclo (3.2.1) octanes (DBO) (1) substituted at the nitrogen atoms by acyl and aralkenyl groups, were tested in in vitro binding assays towards mu and delta opioid receptors. The most representative terms (1a, 1d, 1g, 1j,) were also evaluated for the analgesic potency in vivo by the hot plate method. Among the compounds tested the most potent was the p.nitrocinnamyl DBO (1d) which displayed a mu/delta selectivity and an analgesic activity respectively 25 and 17 fold those of morphine. On the contrary, the m.hydroxycinnamyl DBO (1g) was markedly less active as agonist than the parent 1a, thus suggesting that structure 1 interacts with opioid receptors in a different fashion than morphine. Compound 1j isomer of 1a which is provided with high mu affinity, but lower analgesic potency, was found to possess a mixed agonist-antagonist activity.
Animals Bicyclo Compounds/metabolism/*pharmacology Brain/drug effects/metabolism Bridged Compounds/*pharmacology Male Mice Molecular Conformation Morphine/pharmacology Narcotics/*pharmacology Octanes/metabolism/*pharmacology Receptors, Opioid/*metabolism Receptors, Opioid, delta Receptors, Opioid, mu Time Factors
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