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Synthesis, chromatography and tissue distribution of methyl‐ 11 c‐morphine and methyl‐ 11 C‐heroin
Author(s) -
Kloster G.,
Machulla H.J.,
Röder E.
Publication year - 1979
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580160310
Subject(s) - chemistry , morphine , heroin , high performance liquid chromatography , methylation , distribution (mathematics) , kidney , chromatography , acetylation , pharmacology , biochemistry , drug , endocrinology , medicine , mathematical analysis , mathematics , gene
11 C‐Morphine was prepared by methylation of normorphine with 11 CH 3 I. 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 11 C‐morphine and 36 min for 11 C‐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.