Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B.
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.
Bikbulatov
Ruslan V
RV
Department of Pharmacognosy, School of Pharmacy, University of Mississippi, University, MS 38677-1848, USA.
Yan
Feng
F
Roth
Bryan L
BL
Zjawiony
Jordan K
JK
D020013:Calcium Signaling / Q000187:drug effects; D004224:Diterpenes / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D045785:Diterpenes, Clerodane; D006801:Humans; D007700:Kinetics; D011485:Protein Binding; D017473:Receptors, Opioid, kappa / Q000819:agonists*; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics
D004224:Diterpenes; D045785:Diterpenes, Clerodane; D017473:Receptors, Opioid, kappa; D013438:Sulfhydryl Compounds; C508456:salvinorin B; C090499:salvinorin A