86537-86-2Relevant articles and documents
8-Alkyldihydrocodeinones and dihydromorphinones: Analgesic activity and affinity for opiate receptors
Ghozland,Maroni,Viloria,Cros
, p. 22 - 26 (2007/10/02)
A series of 8-alkyldihydrocodeinones and dihydromorphinones were prepared from codeinone 2. Their morphinomimetic activities were determined by measuring their affinity for the opiate receptors and their analgesic activity was assessed after intracerebroventricular injection in mouse. Good analgesia affinity correlations were observed. The substitution at the C-8 carbon atom, with the exception of methylation, does not improve the narcotic activity over that of dihydrocodeinone and dihydromorphinone. The axially-substituted derivatives are characterized by a pharmacological stereoselectivity: as they are less sterically hindered than their equatorial homologues, a different mode of binding might account for their higher affinity for the opiate receptors.
