Bossuyt A, Morgan G F, offlaton M, Pirotte R, Chirico A, Clemens P, Vandenbroeck P, Thornback J R
Department of Nuclear Medicine, A.Z.-V.U.B., Brussels, Belgium.
J Nucl Med. 1991 Mar;32(3):399-403.
The lipophilic neutral complex [99mTc][TcO(MRP20)] [MRP20 is (N-(2(1H pyrolylmethyl]N'-(4-pentene-3-one-2)ethane-1,2-diamine)] is known to cross the blood-brain barrier in non-primate animals. We report here its in vivo biodistribution, radiation dosimetry, and single-photon emission computed tomography (SPECT) characteristics in man. Following i.v. administration of 15-25 mCi of the tracer, the maximum uptake of activity in the brain peaked at 1 min p.i. Fifteen minutes p.i., the percentage retained in the brain was 5.2 +/- 1.6, which remained fairly constant over 24 hr. Blood clearance was relatively slow with an apparent affinity of the compound for the cellular fraction of the blood, however, soft-tissue and facial activity cleared at a rate four times faster than that of the brain. SPECT images obtained at 15 min, 1 hr, 3 hr, 7 hr, and 24 hr p.i. showed no redistribution of the tracer within the brain. The dosimetry is favorable for administration of 25-30 mCi of MRP20. Our results indicate that this compound is rapidly extracted and retained by the brain and may be used for SPECT imaging of regional blood flow.
亲脂性中性络合物[99mTc][TcO(MRP20)] [MRP20为(N-(2-(1H-吡咯基甲基)]N'-(4-戊烯-3-酮-2)-乙烷-1,2-二胺)]已知可在非灵长类动物中穿过血脑屏障。我们在此报告其在人体中的体内生物分布、辐射剂量学及单光子发射计算机断层扫描(SPECT)特征。静脉注射15 - 25 mCi示踪剂后，脑内放射性活度的最大摄取在注射后1分钟达到峰值。注射后15分钟，脑内保留的百分比为5.2±1.6，在24小时内保持相当稳定。血液清除相对较慢，该化合物对血液细胞部分有明显亲和力，然而，软组织和面部放射性活度的清除速度比脑快四倍。注射后15分钟、1小时、3小时、7小时和24小时获得的SPECT图像显示示踪剂在脑内无重新分布。剂量学结果有利于给予25 - 30 mCi的MRP20。我们的结果表明，该化合物可被脑快速摄取并保留，可用于区域血流的SPECT成像。
