放射性碘化碘氯吉兰作为用于脑部单胺氧化酶A的单光子发射计算机断层扫描放射性药物的评估。

Evaluation of radioiodinated iodoclorgyline as a SPECT radiopharmaceutical for MAO-A in the brain.

作者信息

Hirata M, Magata Y, Ohmomo Y, Saji H, Murakami K, Takagaki T, Yamamura N, Tanaka C, Konishi J, Yokoyama A

机构信息

Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University, Japan.

出版信息

Nucl Med Biol. 1995 Feb;22(2):175-80. doi: 10.1016/0969-8051(94)00105-s.

DOI:10.1016/0969-8051(94)00105-s

PMID:7767310

Abstract

An in vivo estimation of the newly synthesized MAO-A specific inhibitor, [125I]-labeled N-[3(2,4-dichloro-6-iodophenoxy)propyl]-N-methyl-2- propynylamine ([125I]-iodoclorgyline), was performed. Retention of the radioactivity of this radioligand was observed in the brain from 1 h post-injection. Pretreatments with clorgyline and l-deprenyl showed selective binding of [125I]-iodoclorgyline to MAO-A in the brain at 24 h post-injection. Moreover, a good correlation (r = 0.907) between the uptake of [125I]-iodoclorgyline and MAO-A enzyme activity in the cortex was observed in the pretreatment study with several doses of clorgyline. Although improvement to increase the brain/blood ratio is desirable because of slow blood clearance of the radioactivity, radioiodinated iodoclorgyline may serve as a useful SPECT radiopharmaceutical for quantitative analysis of MAO-A in the brain.

摘要

对新合成的单胺氧化酶A（MAO-A）特异性抑制剂——[125I]标记的N-[3(2,4-二氯-6-碘苯氧基)丙基]-N-甲基-2-丙炔胺（[125I] - 碘氯吉兰）进行了体内评估。注射后1小时即在大脑中观察到该放射性配体的放射性滞留。注射后24小时，用氯吉兰和左旋司来吉兰预处理显示[125I] - 碘氯吉兰在大脑中与MAO-A有选择性结合。此外，在使用几种剂量氯吉兰的预处理研究中，观察到[125I] - 碘氯吉兰的摄取与皮质中MAO-A酶活性之间有良好的相关性（r = 0.907）。尽管由于放射性物质的血液清除缓慢，提高脑/血比是可取的，但放射性碘化碘氯吉兰可能作为一种有用的单光子发射计算机断层扫描（SPECT）放射性药物用于大脑中MAO-A的定量分析。