Synthesis and pharmacology of 1-methoxy analogs of CP-47,497.
Three 1-methoxy analogs of CP-47,497 (7, 8, and 19) have been synthesized and their affinities for the cannabinoid CB(1) and CB(2) receptors have been determined. Although these compounds exhibit selectivity for the CB(2) receptor none have significant affinity for either receptor. Modeling and receptor docking studies were carried out, which provide a rationalization for the weak affinities of these compounds for either receptor.
Huffman
John W
JW
Howard L Hunter Laboratory, Clemson University, Clemson, SC 29634-0973, United States. huffman@clemson.edu
Hepburn
Seon A
SA
Reggio
Patricia H
PH
Hurst
Dow P
DP
Wiley
Jenny L
JL
Martin
Billy R
BR
D000818:Animals; D001665:Binding Sites; D016466:CHO Cells; D003198:Computer Simulation; D006224:Cricetinae; D003412:Cricetulus; D003511:Cyclohexanols / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors / Q000378:metabolism; D043885:Receptor, Cannabinoid, CB2 / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship
D003511:Cyclohexanols; D043884:Receptor, Cannabinoid, CB1; D043885:Receptor, Cannabinoid, CB2; C036088:CP 47497