Abstract
In vitro characterization and comparison of JDTic, its dehydroxy analogue and nor-BNI, and its dehydroxy analogue demonstrates that the N-substituted 3,4-dimethyl-(3-hydroxyphenyl)piperidine-derived antagonist, JDTic, relies more heavily on its phenol address group for affinity and antagonist activity relative to the corresponding naltrexone derived antagonists, nor-BNI. The structural flexibility of the former class of compound relative to the latter is postulated to underlie the difference.
Publication types
-
Research Support, U.S. Gov't, P.H.S.
MeSH terms
-
Animals
-
Binding, Competitive
-
Brain / metabolism
-
In Vitro Techniques
-
Naltrexone / analogs & derivatives*
-
Naltrexone / chemistry*
-
Naltrexone / pharmacology
-
Phenols / chemistry*
-
Phenols / pharmacology
-
Piperidines / chemistry*
-
Piperidines / pharmacology
-
Radioligand Assay
-
Rats
-
Receptors, Opioid, delta / antagonists & inhibitors
-
Receptors, Opioid, delta / metabolism
-
Receptors, Opioid, kappa / antagonists & inhibitors*
-
Receptors, Opioid, kappa / metabolism
-
Receptors, Opioid, mu / antagonists & inhibitors
-
Receptors, Opioid, mu / metabolism
-
Structure-Activity Relationship
-
Tetrahydroisoquinolines / chemistry*
-
Tetrahydroisoquinolines / pharmacology
Substances
-
7-hydroxy-N-(1-((4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl)methyl)-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide
-
Phenols
-
Piperidines
-
Receptors, Opioid, delta
-
Receptors, Opioid, kappa
-
Receptors, Opioid, mu
-
Tetrahydroisoquinolines
-
norbinaltorphimine
-
Naltrexone