Woods S W, Seibyl J P, Goddard A W, Dey H M, Zoghbi S S, Germine M, Baldwin R M, Smith E O, Charney D S, Heninger G R
Dept. of Psychiatry, Yale University School of Medicine, New Haven, CT 06519.
Psychiatry Res. 1992 Aug;45(2):67-77. doi: 10.1016/0925-4927(92)90001-k.
Previous work suggests that iomazenil (formerly known as Ro 16-0154) is a useful ligand for static imaging of the benzodiazepine (BZ) receptor with single photon emission computed tomography (SPECT). The present study evaluated the feasibility of dynamic SPECT imaging of cerebral radioactivity following intravenous [123I]iomazenil injection in healthy human subjects, in preparation for future receptor quantitation studies. Maximal brain uptake was reached approximately 25-30 minutes after i.v. administration of the radioligand and represented approximately 12% of the injected dose. The regional distribution of radioactive densities was consistent with the known distribution of BZ receptors in human brain, with highest uptake localized over the occipital area. Washout of cortical radioactivity was regionally variable but relatively slow, with a half-life of approximately 4 hours after the time of peak radioactivity. In summary, [123I]iomazenil is a promising SPECT radioligand for the BZ receptor, with high brain uptake, relatively slow washout of radioactivity, and appropriate regional distribution.
先前的研究表明，碘西尼（曾用名Ro 16 - 0154）是一种用于单光子发射计算机断层扫描（SPECT）对苯二氮䓬（BZ）受体进行静态成像的有效配体。本研究评估了在健康人体静脉注射[123I]碘西尼后，进行脑放射性动态SPECT成像的可行性，为未来的受体定量研究做准备。静脉注射放射性配体后约25 - 30分钟达到最大脑摄取量，约占注射剂量的12%。放射性密度的区域分布与人类大脑中已知的BZ受体分布一致，最高摄取量位于枕叶区域。皮质放射性的清除在区域上存在差异，但相对较慢，在放射性峰值出现后约4小时的半衰期。总之，[123I]碘西尼是一种有前景的用于BZ受体的SPECT放射性配体，具有高脑摄取、放射性清除相对较慢以及合适的区域分布。
