Abstract
The N-(2-cyanoethyl)-9alpha-ethyl-5-methyl-6,7-benzomorphan (1c) is a more potent antinociceptive and has stronger receptor binding affinity than its N-methyl analogue 1b. The N-(2-cyanoethyl)-4-phenylpiperidine compounds 2b and 3b were almost inactive compared to their N-methyl congeners 2a and 3a, respectively. It appears that the pharmacological effect of the N-(2-cyanoethyl) moiety is dependent on the opioid on which it is substituted.
Publication types
-
Research Support, U.S. Gov't, P.H.S.
MeSH terms
-
Analgesics / chemical synthesis*
-
Analgesics / metabolism
-
Animals
-
Benzomorphans / analogs & derivatives
-
Benzomorphans / chemical synthesis*
-
Benzomorphans / metabolism
-
Benzomorphans / pharmacology
-
Binding, Competitive
-
Brain / metabolism
-
Dihydromorphine / metabolism
-
Haplorhini
-
Humans
-
In Vitro Techniques
-
Macaca mulatta
-
Meperidine / analogs & derivatives*
-
Meperidine / chemical synthesis
-
Meperidine / metabolism
-
Meperidine / pharmacology
-
Mice
-
Morphinans / chemical synthesis*
-
Morphine Dependence / physiopathology
-
Nitriles / chemical synthesis*
-
Piperidines / chemical synthesis*
-
Rats
-
Structure-Activity Relationship
Substances
-
Analgesics
-
Benzomorphans
-
Morphinans
-
Nitriles
-
Piperidines
-
Meperidine
-
Dihydromorphine