title: Preparation of a bromine-76 labelled analogue of epibatidine: a potent ligand for nicotinic acetylcholine receptor studies.
abstract: Epibatidine analogues have been labelled with I-123 for single photon emission computed tomography and with short half-life positron emitters (C-11 and F-18) for PET. For easier radiopharmacological studies the bromo analogue of epibatidine (norchlorobromoepibatidine or exo-7-azabicyclo-2-(2-bromo-5-pyridyl)-[2.2.1]heptane) was labelled with Br-76, a longer half-life positron emitter, (T1/2 = 16.2h). [76Br]-norchlorobromoepibatidine was prepared by using a Cu+ assisted bromodeiodination exchange from the iodo analogue in reducing conditions at 190 degrees C. The tracer purified by RP-HPLC was obtained in 70% radiochemical yield with a specific radioactivity of 20 GBq/micromol. Radiochemical and chemical purities measured by radio-TLC and HPLC were >98%.
authors.affiliation: Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Camperdown, NSW, Australia. mkassiou@med.usyd.edu.au
authors.forename: M
authors.initials: M
authors.lastname: Kassiou
authors.forename: C
authors.initials: C
authors.lastname: Loc'h
authors.forename: F
authors.initials: F
authors.lastname: Dolle
authors.forename: J L
authors.initials: JL
authors.lastname: Musachio
authors.forename: L
authors.initials: L
authors.lastname: Dolci
authors.forename: C
authors.initials: C
authors.lastname: Crouzel
authors.forename: R F
authors.initials: RF
authors.lastname: Dannals
authors.forename: B
authors.initials: B
authors.lastname: Mazière
mesh_terms: D000818:Animals; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D001967:Bromine Radioisotopes / Q000302:isolation & purification*; D066298:In Vitro Techniques; D008024:Ligands; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D011854:Radiochemistry; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D011978:Receptors, Nicotinic / Q000378:metabolism*; D014055:Tomography, Emission-Computed
chemical_list: D019086:Bridged Bicyclo Compounds, Heterocyclic; D001967:Bromine Radioisotopes; D008024:Ligands; D011725:Pyridines; D019275:Radiopharmaceuticals; D011978:Receptors, Nicotinic; C470033:norchlorobromoepibatidine; C082748:epibatidine