157891-92-4Relevant articles and documents
Synthesis and evaluation of three structurally related 18F- labeled orvinols of different intrinsic activities: 6-O-[18F] fluoroethyl-diprenorphine ([18F]FDPN), 6-O-[18F] fluoroethyl-buprenorphine ([18F]FBPN), and 6-O-[18F] fluoroethyl-phenethyl-orvinol ([18F]FPEO)
Schoultz, Bent W.,Hj?rnevik, Trine,Reed, Brian J.,Marton, János,Coello, Christopher S.,Willoch, Frode,Henriksen, Gjermund
, p. 5464 - 5469 (2014/07/08)
We report the synthesis and biological evaluation of a triplet of 6-O- 18F-fluoroethylated derivatives of structurally related orvinols that span across the full range of intrinsic activities, the antagonist diprenorphine, the partial agonist buprenorphine, and the full agonist phenethyl-orvinol. [18F]fluoroethyl-diprenorphine, [ 18F]fluoroethyl-buprenorphine, and [18F]fluoroethyl- phenethyl-orvinol were prepared in high yields and quality from their 6-O-desmethyl-precursors. The results indicate suitable properties of the three 6-O-18F-fluoroethylated derivatives as functional analogues to the native carbon-11 labeled versions with similar pharmacological properties.