[In vivo autoradiographic benzodiazepine receptor imaging with 125I-iomazenil (Ro 16-0154)].

The biodistribution of 125I-Iomazenil (Ro 16-0154), a benzodiazepine receptor antagonist, was examined using in vivo autoradiography of gerbil brain. 125I-Iomazenil was administrated i.v. into male gerbils, and autoradiography was prepared from coronary sections of the animals decapitated at 5, 60, 120 and 180 min after injection. Initial uptake images (5 min) of 125I-Iomazenil were thought to show blood flow distribution. On the images obtained 120-180 min after administration, high activity of 125I-Iomazenil was observed in the cerebral cortex, amygdala, hippocampus, globus pallidus, thalamus, hypothalamus, superior colliculus, substantia nigra and cerebellar cortex in the areas of which benzodiazepine receptor concentration was reported to be high. However, low activity was observed in the caudate-putamen. Accumulation of 125I-Iomazenil was blocked by pre-administration of flumazenil. 123I-Ro 16-0154 has a high potentiality for benzodiazepine receptor mapping by SPECT.