## Abstract Various approaches to the synthesis of tritiumβlabelled BIIL 260 with high specific radioactivity were investigated. Attempts to incorporate tritium directly into BIIL 260 were made by solidβphase isotope exchange with tritium gas and by isotope exchange with tritiated water which yield
Preparation of tritium-labelled meta-aminolevamisole of high specific radioactivity by catalytic dehalogenation
β 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
No coin nor oath required. For personal study only.
β¦ 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
π SIMILAR VOLUMES
Since its introduction to medicine several years ago, diphenylhydantoin (DPH) has been widely used in the treatment of epilespy, both in adults and children.( 2) The effects of the drug is well correlated with the plasma levels. high levels have adverse effects. ( 3 )
A simple and rapid method of preparing 1251-labeled secretin of high specific radioactivity has been developed. Synthetic porcine secretin was iodinated with Na[rz51] by a modification of the chloramine T method. Purification and separation of labeled from unlabeled secretin was achieved by chromato