Preparation of a bromine-76 labelled analogue of epibatidine: a potent ligand for nicotinic acetylcholine receptor studies.
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%.
Kassiou
M
M
Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Camperdown, NSW, Australia. mkassiou@med.usyd.edu.au
Loc'h
C
C
Dolle
F
F
Musachio
J L
JL
Dolci
L
L
Crouzel
C
C
Dannals
R F
RF
Mazière
B
B
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
D019086:Bridged Bicyclo Compounds, Heterocyclic; D001967:Bromine Radioisotopes; D008024:Ligands; D011725:Pyridines; D019275:Radiopharmaceuticals; D011978:Receptors, Nicotinic; C470033:norchlorobromoepibatidine; C082748:epibatidine