An improved method for the preparation of [11C]verapamil

被引:29
作者
Wegman, TD [1 ]
Maas, B [1 ]
Elsinga, PH [1 ]
Vaalburg, W [1 ]
机构
[1] Univ Groningen Hosp, Positron Emiss Tomog Ctr, PET, NL-9700 RB Groningen, Netherlands
关键词
multidrug resistance (MDR); P-glycoprotein; C-11]verapamil; positron emission tomography;
D O I
10.1016/S0969-8043(02)00143-4
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
This paper describes an improved preparation of [C-11]verapamil by reaction of [C-11]methyl triflate with desmethylverapamil. The optimal reaction temperature, amount of precursor and reaction time were assessed. With this method [C-11]verapamil can be prepared with a reproducible radiochemical yield of 66+/-4% (EOB, based on [C-11]methyltriflate). Total synthesis time was 60 min. Radiochemical purity was >99% and specific activities varied between 5 and 30TBq/mmol. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:505 / 507
页数:3
相关论文
共 11 条
[1]  
Elsinga PH, 1996, J NUCL MED, V37, P1571
[2]   EXPRESSION OF A MULTIDRUG-RESISTANCE GENE IN HUMAN-TUMORS AND TISSUES [J].
FOJO, AT ;
UEDA, K ;
SLAMON, DJ ;
POPLACK, DG ;
GOTTESMAN, MM ;
PASTAN, I .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1987, 84 (01) :265-269
[3]   Complete in vivo reversal of P-glycoprotein pump function in the blood-brain barrier visualized with positron emission tomography [J].
Hendrikse, NH ;
Schinkel, AH ;
De Vries, EGE ;
Fluks, E ;
Van der Graaf, WTA ;
Willemsen, ATM ;
Vaalburg, W ;
Franssen, EJF .
BRITISH JOURNAL OF PHARMACOLOGY, 1998, 124 (07) :1413-1418
[4]   AN ONLINE METHOD FOR THE PREPARATION OF NCA [(CH3)-C-11]TRIFLUOROMETHANESULFONIC ACID METHYL-ESTER [J].
HOLSCHBACH, M ;
SCHULLER, M .
APPLIED RADIATION AND ISOTOPES, 1993, 44 (05) :897-898
[5]   An alternative synthesis of [11C]raclopride for routine use [J].
Ishiwata, K ;
Ishii, S ;
Senda, M .
ANNALS OF NUCLEAR MEDICINE, 1999, 13 (03) :195-197
[6]   A simple loop method for the automated preparation of [11C]raclopride from [11C]methyl triflate [J].
Iwata, R ;
Pascali, C ;
Bogni, A ;
Miyake, Y ;
Yanai, K ;
Ido, T .
APPLIED RADIATION AND ISOTOPES, 2001, 55 (01) :17-22
[7]  
JEWETT DM, 1992, APPL RADIAT ISOTOPES, V43, P1383
[8]   MULTIDRUG-RESISTANCE IN HUMAN CANCER [J].
LEHNERT, M .
JOURNAL OF NEURO-ONCOLOGY, 1994, 22 (03) :239-243
[9]  
Lemaire C., 1995, Journal of Labelled Compounds and Radiopharmaceuticals, V37, P723
[10]  
LUURTSEMA G, 2001, J LABELLED COMPDS RA, V44, P313