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Bromine-75-Labeled 1,4-Benzodiazepines: Potential Agents for the Mapping of Benzodiazepine Receptors In Vivo: Concise Communication

Institut für Chemie 1: Nuklearchemie der KFA Jülich GmbH, D-5170 Jülich, FRG

Correspondence: For reprints contact: Dr. Gerhard Stöcklin, Institut für Chemie l, Nuklearchemie der KFA Jülich GmbH. D-5170 Jülich, FRG.

ABSTRACT

We have prepared four different 1,4-benzodiazepines, labeled at C-7 with the1.6-hr positron emitter Br-75 or the 57-hr gamma emitter Br-77, as potential radiopharmaceuticalsfor 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 (Br-75 BFB) was isolated with a minimum specific activity of 20,000CI/mmole. 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 to 10 min) investigated.

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