SYNTHESIS OF A RADIOTRACER FOR STUDYING KAPPA-SUBTYPE OPIATE RECEPTORS - N-[C-11-METHYL]-N-(TRANS-2-PYRROLIDINYL-CYCLOHEXYL)-3,4-DICHLOROPHENYLACETAMIDE ([C-11](+/-)U-50488H)

被引:12
|
作者
NOBLE, GD
DANNALS, RF
RAVERT, HT
WILSON, AA
WAGNER, HN
机构
[1] JOHNS HOPKINS UNIV,DIV NUCL MED,615 N WOLFE ST,BALTIMORE,MD 21218
[2] JOHNS HOPKINS UNIV,DIV RADIAT HLTH SCI,BALTIMORE,MD 21218
关键词
RADIOTRACER; SYNTHESIS; KAPPA OPIATE RECEPTOR; C-11; POSITRON EMISSION TOMOGRAPHY;
D O I
10.1002/jlcr.2580310202
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
The radiochemical synthesis of a kappa-subtype opiate receptor ligand, [C-11](+/-)U-50488H, was accomplished either in two steps or by direct methylation with [C-11]iodomethane. The radiotracer was purified using reversed phase semipreparative HPLC. The average specific activity was 1830 mCi/mu-mole (calculated at the end-of-synthesis; EOS) for the direct methylation and 2140 mCi/mu-mole EOS for the two-step one-pot synthesis. The average time of synthesis including formulation was approximately 22 minutes for the direct methylation and 27 minutes for the two-step one-pot synthesis.
引用
收藏
页码:81 / 89
页数:9
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