Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
An Approach for Assaying Benzodiazepine Receptor Binding with Radioiodinated Ligand : 125I-Labeled Diazepam Derivative
佐治 英郎飯田 靖彦有吉 和彦中塚 巌片岡 正樹吉武 彬横山 陽
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1993 年 16 巻 5 号 p. 513-515

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[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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