An approach for assaying benzodiazepine receptor binding with radioiodinated ligand: 125I-labeled diazepam derivative |
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Authors: | H Saji Y Iida K Ariyoshi I Nakatsuka M Kataoka A Yoshitake A Yokoyama |
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Affiliation: | Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University, Japan. |
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Abstract: | [125I]2'-Iododiazepam (IDZ) was prepared and its application in a benzodiazepine receptor binding assay was studied. [125I]2'-IDZ binds to the rat cortical membrane with a high affinity (Kd, 0.66 nM). Various benzodiazepines showed competition with [125I]2'-IDZ for the binding sites in the rat cortical membrane, and the specificity of its binding correlated well with that of [3H]diazepam (r = 0.992, p < 0.001). These findings suggested that [125I]2'-IDZ binds to the same sites as [3H]diazepam and indicated that [125I]2'-IDZ can be used in a benzodiazepine receptor assay. |
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