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Radioiodinated 2'-Iododiazepam: A Potential Imaging Agent for SPECT Investigations of Benzodiazepine Receptors

Faculty of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan
Environmental Health Science Laboratory, Sumitomo Chemical Company Ltd., Osaka, Japan

Correspondence: For correspondence or reprints contact: Akira Yokoyama, PhD, Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University, Yoshida Shimoadachi-cho, Sakyo-ku, Kyoto 606-01, Japan

ABSTRACT

2'-Iododiazepam (2'-IDZ) is the diazepam analogue iodinated at the 2'-position of C-5 phenyl ring which was synthesized and evaluated as a potential radiopharmaceutical for investigating brain benzodiazepine receptors by SPECT. The ¹²⁵I-2'-iododiazepam was synthenized by halogen exchange reaction and purified by HPLC. In vitro competitive binding studies with ³H-diazepam, using rat cortical synaptosomal membranes, showed that the affinity of 2'-IDZ for benzodiazepam receptors was higher than that in diazepam and flumazenil (RO15-1788). Bio-distribution studies in mice showed that the brain uptake of 2'-iododiazepam was rapid and profound, and in the brain higher accumulation was found in the cortex than in other regions. Furthermore, the cortical uptake was displaced by benzodiazepinergic compounds. In vivo uptake was assessed by autoradiographic studies. Thus, 2'-iododiazepam bound to benzodiazepine receptors in vivo and therefore holds great potential for in vivo benzodiazepine receptor studies.

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				C. I. Okocha, F. Kapczinski, N. Lassen, and M. H. Lader Central benzodiazepine receptor imaging and quantitation with single photon emission computerised tomography: SPECT J Psychopharmacol, January 1, 1995; 9(4): 369 - 380. [Abstract] [PDF]