Lever J R, Mazza S M, Dannals R F, Ravert H T, Wilson A A, Wagner H N
Department of Environmental Health Sciences, Johns Hopkins University School of Hygiene and Public Health, Baltimore, MD 21205.
Int J Rad Appl Instrum A. 1990;41(8):745-52. doi: 10.1016/0883-2889(90)90022-9.
We have developed a simple and rapid method for the production of buprenorphine (BPN), a potent opioid partial agonist, labelled with carbon-11 at the 6-methoxy position. The procedure uses a precursor synthesized in high yield (89%) from BPN in two steps and employs [11C]iodomethane as the radiolabelling reagent. [11C]BPN of 97% radiochemical purity can be prepared in high specific activity (41 GBq/mumol; 1120 mCi/mumol) in a radiochemical yield of 10% at end-of-synthesis (not decay corrected). The [11C]BPN is available for use in studies of cerebral opioid receptors by positron emission tomography within 24 min from end-of-bombardment, including radiosynthesis, purification, formulation for i.v. injection and determination of specific activity.
