Preparation of a bromine-76 labelled analogue of epibatidine: A potent ligand for nicotinic acetylcholine receptor studies

M. Kassiou, C. Loc'h, F. Dolle, J. L. Musachio, L. Dolci, C. Crouzel, R. F. Dannals, B. Mazière

Research output: Contribution to journalArticle

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°C. The tracer purified by RP-HPLC was obtained in 70% radiochemical yield with a specific radioactivity of 20GBq/μmol. Radiochemical and chemical purities measured by radio-TLC and HPLC were >98%.

Original languageEnglish (US)
Pages (from-to)713-717
Number of pages5
JournalApplied Radiation and Isotopes
Volume57
Issue number5
DOIs
StatePublished - Nov 1 2002

Keywords

  • Bromine-76
  • Epibatidine
  • Nicotinic acetylcholine receptors
  • PET

ASJC Scopus subject areas

  • Radiation

Fingerprint Dive into the research topics of 'Preparation of a bromine-76 labelled analogue of epibatidine: A potent ligand for nicotinic acetylcholine receptor studies'. Together they form a unique fingerprint.

  • Cite this