BROMINE-75-LABELED 1,4-BENZODIAZEPINES - POTENTIAL AGENTS FOR THE MAPPING OF BENZODIAZEPINE RECEPTORS INVIVO - CONCISE COMMUNICATION

  • 1 January 1983
    • journal article
    • research article
    • Vol. 24  (5) , 417-422
Abstract
Different 1,4-benzodiazepines [4], labeled at C-7 with the 1.6-h positron emitter 75Br or the 57-h gamma emitter 77Br, as potential radiopharmaceuticals for the mapping of cerebral benzodiazepine receptor areas. The triazene method was used and optimized. Yields at the no-carrier-added level were 20%. 7-[75Br]-5-(2-fluorophenyl)-1-methyl-1,3-dihydro-2H-1,4-benzodiazepine-2-one (75Br BFB) was isolated with a minimum specific activity of 20,000 Ci/mmol. Biodistribution in mice shows that BFB is taken up rapidly by the brain and is retained there at useful concentrations for significant periods of time. The maximum uptake is observed at 0.25 min. Brain-to-blood concentration ratios are larger than 2 during the interval (0.25-10 min) investigated.

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