Bromination and subsequent catalytic tritiation of thienylalanine and 4-methyltyrosine residues in the bradykinin analog RMP-7
✍ Scribed by Alan Akiyama; Gary F. Musso; Janet L. Smart; Christopher Lang; Julie Ann Straub
- Book ID
- 102901514
- Publisher
- John Wiley and Sons
- Year
- 1994
- Tongue
- French
- Weight
- 538 KB
- Volume
- 34
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
A two step strategy was devised for the synthesis of ^3^H‐RMP‐7 for use in pharmacokinetic studies. First, RMP‐7 was brominated predominantly on the thiophene ring of thienylalanine using Br~2~ in AcOH. Then, reductive tritiation of the brominated RMP‐7 using ^3^H~2~ and Pd/C yielded ^3^H‐RMP‐7 (specific activity 1 Ci/mmol; 96% radiochemical purity). An HPLC based assay using on‐line radioactivity detection was developed for in vivo pharmacokinetic studies of ^3^H‐RMP‐7. Rapid clearance from the blood and metabolism of RMP‐7 to des‐Arg^1^‐RMP‐7 was observed in vivo in rats.