冠醚法标记肾上腺显影剂NCL-6-I的动力学研究

STUDY OF KINETICS IN LABELLING THE ADRENAL IMAGING AGENT NCL-6-I BY THE CROWN ETHER METHOD

摘要: <正> 一、前言 6β-碘甲基-19-去甲胆固醇(简写NCL-6-I)的放射性碘标记物是目前临床常用的肾上腺显影剂。标记方法有丙酮法、丙酮-乙腈法、乙醇法及乙腈法,近来又采用熔融法和冠醚法等。熔融法和冠醚法都具有反应快速和产额高等特点。但迄今为止,关于冠醚法标记过程的反应动力学缺乏系统的研究。冠醚法标记方法分两类:(1)冠醚催化交换(简写为CEC),冠醚以催化量加入反应溶剂;(2)冠醚介质交换(简写为CEM)。标记物一般只有1-5mg,冠醚一般在20mg以上,冠醚既作为相转移催化剂,又
- 6β-碘甲基-19-去甲胆固醇 /
- 放射性卤化作用 /
- 动力学 /
- 冠醚法
Abstract: Radioiodination of NCL-6-I is achieved by means of the crown ether method. Kinetics in the 18-C-6 crown ether medium is investigated. The results indicate that the isotopic exchange reaction between NCL-6-I and Na 125I is a second order reaction. The rate constant of reaction is determined by a straight line between -In (1-F) and t. Our results show that the crown ether labelling method is characterized by high yield, rapidity and conveniece.
- NCL-6-1 /
- Radiohalogenation /
- Kinetics /
- Crown ether method.

[1]	Beierwaltes,W.H.et al., Adrenal Cortical Compounds,in Radiopharmaceuticals: Structure-Activity Relationships,ed.by Spencer,R.P.,Grune and Stratton Inc.,New York,1981,p.395．
[2]	Gross,M.D.et al.,Clin.Nucl.Med.,9,264(1984) .
[3]	Kojima,M.et al.,J.Nucl.Med.,16,666(1975) .
[4]	Kamoi,I.,et al.,J.Nucl.Med.,17,389(1980) .
[5]	Basmadjian,G.P.et al.,J.Lab.Compd.,11,427(1975) .
[6]	Ito,T.et al.,Yakugaku Zasshi,103,644(1983) .
[7]	朱瑞森等,中华核医学杂志,3,106(1983) 。
[8]	Liu,B.L.et al.,Int.J.Appl.Radiat Isot,36,561(1985) .
[9]	Liu,B.L.et al.,Radiotsotopes 30,275(1981) .
[10]	Liu,B.L.et al.,Radioisotopes,30,391(1981) .
[11]	平冈道夫,化合物--特性应用,讲谈社,东京,1978;英文版,1982．
[12]	翁皓珉等,核化学与放射化学,5,154(1983) .
[13]	刘伯里等,核化学与放射化学,6,120,1(1984) .
[14]	刘伯里,陈仕平,核化学与放射化学,7,155(1985) .
[15]	Coenen,H.H.et al,J.Nucl.Med,26,37(1985) .
[16]	刘伯里等,核化学与放射化学,4,100(1982) .
[17]	国毓智等,核化学与放射化学,5,1(1983) .
[18]	刘伯里等,核化学与放射化学,5,224(1983) .
[19]	刘伯里等,核化学与放射化学,6,243(1984) .
[20]	陈仕平等,核化学与放射化学,7,222(1985) .
[21]	王积善;高等有机化学,北京,人民教育出版社,1980年,第111页.
[22]	Reichardt,C.,Solvent Effects in Organic Chemistry,Verlag Chemie,Weinheim,New York,1978．
[23]	Chen,S.P,and Liu,B.L.,J.Radioanal.Nucl.Chem.Letters,126,279(1988) .