Abstract
To study drug-receptor interactions, new thio-derivatives of salvinorin A, an extremely potent natural kappa-opioid receptor (KOR) agonist, were synthesized. Obtained compounds were examined for receptor binding affinity. Analogs with the same configuration at carbon atom C-2 as in natural salvinorin A showed higher affinity to KOR than their corresponding epimers.
Publication types
-
Research Support, N.I.H., Extramural
MeSH terms
-
Calcium Signaling / drug effects
-
Diterpenes / chemical synthesis*
-
Diterpenes / pharmacokinetics
-
Diterpenes, Clerodane
-
Humans
-
Kinetics
-
Protein Binding
-
Receptors, Opioid, kappa / agonists*
-
Structure-Activity Relationship
-
Sulfhydryl Compounds / chemical synthesis*
-
Sulfhydryl Compounds / pharmacokinetics
Substances
-
Diterpenes
-
Diterpenes, Clerodane
-
Receptors, Opioid, kappa
-
Sulfhydryl Compounds
-
salvinorin B
-
salvinorin A