title: Facile synthesis of [11C]buprenorphine for positron emission tomographic studies of opioid receptors.
abstract: 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.
authors.affiliation: Department of Environmental Health Sciences, Johns Hopkins University School of Hygiene and Public Health, Baltimore, MD 21205.
authors.forename: J R
authors.initials: JR
authors.lastname: Lever
authors.forename: S M
authors.initials: SM
authors.lastname: Mazza
authors.forename: R F
authors.initials: RF
authors.lastname: Dannals
authors.forename: H T
authors.initials: HT
authors.lastname: Ravert
authors.forename: A A
authors.initials: AA
authors.lastname: Wilson
authors.forename: H N
authors.initials: HN
authors.lastname: Wagner
mesh_terms: D002047:Buprenorphine; D002250:Carbon Radioisotopes; D007553:Isotope Labeling / Q000379:methods; D011957:Receptors, Opioid; D014055:Tomography, Emission-Computed
chemical_list: D002250:Carbon Radioisotopes; D011957:Receptors, Opioid; D002047:Buprenorphine