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The preparation of a 11C-labelled 5-lipoxygenase product. 5(S)-hydroxy-6(R)-(N-[1-11C]acetyl)cysteinyl-7,9-trans-11,14-ciseicosatetraenoic acid

✍ Scribed by Franz Oberdorfer; Thilo Siegel; Albrecht Guhlmann; Dietrich Keppler; Wolfgang Maier-Borst

Publisher
John Wiley and Sons
Year
1992
Tongue
French
Weight
451 KB
Volume
31
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

5(S)‐Hydroxy‐6(R)‐(N‐[1‐^11^C]acetyl)cysteinyl‐7,9‐trans‐11,14‐cis‐eicosatetraenoic acid (N‐[1‐^11^C]acetyl leukotriene E~4~) was prepared by the reaction of leukotriene E~4~ and [1‐^11^C]acetyl chloride. The product was obtained with 1.3% yield, based on [1‐^11^C]acetyl chloride. The preparation required 50 min from the end of radioisotope production. The chemical and radiochemical purity of an injectable dose of N‐[1‐^11^C]acetyl leukotriene E~4~ was 95%. The remaining impurities were the 11‐trans isomer primarily and the sulfoxides of 5(S)‐hydroxy‐6(R,S)‐(N‐[1‐^11^C]acetyl)cysteinyl‐7,9‐trans‐11‐(cis,trans)‐14‐cis‐eicosatetraenoic acid. The stereochemistry of the sulfoxides at C‐6 and at the C‐11 double bond respectively was not identified. The average specific activity of the carrier added preparation was 2 GBq/μmol at the time of application.

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