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Bromination and subsequent catalytic tritiation of thienylalanine and 4‐methyltyrosine residues in the bradykinin analog RMP‐7
Author(s) -
Akiyama Alan,
Musso Gary F.,
Smart Janet L.,
Lang Christopher,
Straub Julie Ann
Publication year - 1994
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.2580341211
Subject(s) - chemistry , pharmacokinetics , halogenation , in vivo , catalysis , thiophene , tritium , bradykinin , chemical synthesis , stereochemistry , combinatorial chemistry , in vitro , pharmacology , organic chemistry , biochemistry , receptor , medicine , physics , microbiology and biotechnology , nuclear physics , biology
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.