Torizuka K, Uemura K, Toru M, Shinohara Y, Nishimura T, Yonekura Y, Nakagawara J, Matsuda H, Sakai F, Matsuda K, Fukuyama H, Morimoto K
Fukui Medical School, Japan.
Kaku Igaku. 1996 Mar;33(3):303-18.
Iomazenil (IMZ) is a partial inverse agonist of central-type benzodiazepine receptors (BZR) which binds specifically to BZR with high affinity. A multi-center Phase 3 clinical study was performed to evaluate the clinical usefulness of 123I-IMZ-SPECT in the diagnosis of brain disorders in 169 patients with degenerative neurological diseases and 37 patients with mental disorders such as neurotic, stress-related and somatoform disorders. In dementia, the decrease in activity in late images, obtained three hours after administration of 123I-IMZ, correlated negatively with the dementia score. In Parkinson's disease and spinocerebellar degeneration. 123I-IMZ showed a more profound decrease in uptake in late images than seen in the cerebral blood flow (CBF) images, and this decrease was in proportion to the duration and severity of the illness. In mental disorders, the ratio of the late to early image counts showed a negative correlation with Hamilton's anxiety scale in all regions in the brain cortices. In panic disorders, the ratio of the cerebral count to the cerebellar count in the late images correlated negatively with the severity of the attack in the frontal, temporal and parietal cortices. These results suggest that 123I-IMZ-SPECT enables us to evaluate the neuronal damage in degenerative diseases and the decrease in the BZR binding potential in mental disorders.
碘西尼(IMZ)是一种中枢型苯二氮䓬受体(BZR)的部分反向激动剂,它以高亲和力特异性结合BZR。进行了一项多中心3期临床研究,以评估123I-IMZ-SPECT在169例退行性神经疾病患者和37例精神障碍患者(如神经症、与应激相关和躯体形式障碍)的脑部疾病诊断中的临床实用性。在痴呆症中,注射123I-IMZ三小时后获得的晚期图像中活性降低与痴呆评分呈负相关。在帕金森病和脊髓小脑变性中,123I-IMZ晚期图像中的摄取降低比脑血流量(CBF)图像中更明显,且这种降低与疾病的持续时间和严重程度成比例。在精神障碍中,晚期与早期图像计数的比值在大脑皮层的所有区域均与汉密尔顿焦虑量表呈负相关。在惊恐障碍中,晚期图像中大脑计数与小脑计数的比值在额叶、颞叶和顶叶皮层与发作严重程度呈负相关。这些结果表明,123I-IMZ-SPECT使我们能够评估退行性疾病中的神经元损伤以及精神障碍中BZR结合潜能的降低。