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Preparation of tritium-labelled meta-aminolevamisole of high specific radioactivity by catalytic dehalogenation

✍ Scribed by James A. Lewis; Ian Paterson


Publisher
John Wiley and Sons
Year
1984
Tongue
French
Weight
603 KB
Volume
21
Category
Article
ISSN
0022-2135

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✦ Synopsis


We describe the synthesis o f tritiated meta-aminolevamisole (MAL) of high specific radioactivity. iodinated with iodine monochloride in aqueous hydrochloric acid. The major reaction product, L[-]2,3,5,6-tetrahydro-6-(5-amino-2-iodophenyl)imidazo [2,1 -b]thiazole, was catalytically dehalogenated with carrier-free tritium gas in methanolic potassium hydroxide over 10% palladium-carbog. After extraction and chromatography, a radioactive species ( [ HI-MAL) was identified wit$ the same chromatographic mobility as unlabelled MAL. activity in contracting nematode muscle as authentic unlabelled MAL, co-chromatographs with unlabelled MAL in three different TLC systems and is about 90% radiochemically pure. By bioassay and fompetitive inhibition studies, the specific radioactivity o f [ HI-MAL appears greaijer than 15 Ci/mole and is probably close to 29 CJnmole. detecting a high affinity, saturable binding activity in extracts of the nematode Caenorhabditis elegans. m b e l l e d MAL was [ HI-MAL possesses the same high biological


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