Prodrug behaviour of nicotinoylmorphine esters

Author:

Broekkamp C L1,Oosterloo S K1,Rijk H W1

Affiliation:

1. Department of CNS Pharmacology, Organon International B.V., P.O. Box 20, 5340 BH Oss, The Netherlands

Abstract

Abstract Morphine and its nicotinoyl esters, dinicotinoylmorphine (nicomorphine), 6-mononicotinoylmorphine (6-MNM) and 3-mononicotinoylmorphine (3-MNM) were tested in mice for central activity to obtain time-effect profiles of these compounds in rats. Two effects, analgesia with the hot plate test and locomotor stimulation in activity cages were measured and nicomorphine, 6-MNM and 3-MNM were found to have a faster onset of action compared with morphine. The effects of 3-MNM and morphine lasted longer than the effect of nicomorphine and 6-MNM. The prodrug behaviour of 3-MNM and nicomorphine for morphine and 6-MNM, respectively, is discussed.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

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