Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Effects of Epoxidation on the Actions of Normorphine, Norcodeine, N-Allylnormorphine (Nalorphine) and N-Allylnorcodeine on the Electrically Stimulated Guinea Pig Ileum
NOBUO CHOMASAAKI HIROBEISSEI TAKAYANAGI
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Keywords: guineapig ileum
JOURNAL FREE ACCESS

1985 Volume 33 Issue 4 Pages 1681-1686

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Abstract

The effects of epoxidation of normorphine, norcodeine, N-allylnormorphine (nalorphine) and N-allylnorcodeine on the twitch response of guinea pig ileum to electrical stimulation were studied. Normorphine, norcodeine and their epoxides are narcotic agonists, while nalorphine, N-allylnorcodeine and their epoxides are agonist-antagonists. The agonistic effects (via mu-receptor) of normorphine and norcodeine were not influenced by epoxidation of the 7, 8-double bond. Epoxidation also little influenced the competitive antagonistic action (via mu-receptor) of nalorphine and N-allylnorcodeine against morphine. On the other hand, the agonistic action (via kappa-receptor) of nalorphine and N-allylnorcodeine was considerably decreased by epoxidation.

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© The Pharmaceutical Society of Japan
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