SYNTHESIS, CHROMATOGRAPHY AND TISSUE DISTRIBUTION OF METHYL-C-11-MORPHINE AND METHYL-C-11-HEROIN

被引:11
作者
KLOSTER, G [1 ]
RODER, E [1 ]
MACHULLA, HJ [1 ]
机构
[1] UNIV BONN,INST PHARMAZEUT,D-5300 BONN 1,FED REP GER
关键词
Animal Experiments; Carbon‐11; Heroin; Morphine;
D O I
10.1002/jlcr.2580160310
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
11C‐Morphine was prepared by methylation of normorphine with 11CH3I. Acetylation of this compound yields heroin. The radiochemical yield is 9% for morphine and 4% for heroin at a specific activity of 1.63 mCi/μmole. Synthesis time including purification by hplc is 18 min for 11C‐morphine and 36 min for 11C‐heroin, respectively. The tissue distribution of both these compounds was determined in rats at different times after an i.v. injection. The main accumulation of activity is in the small intestine, followed by kidney and liver. Little activity was detected in the brain. Copyright © 1979 John Wiley & Sons, Ltd.
引用
收藏
页码:441 / 448
页数:8
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