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Bromination and subsequent catalytic tritiation of thienylalanine and 4-methyltyrosine residues in the bradykinin analog RMP-7



Bromination and subsequent catalytic tritiation of thienylalanine and 4-methyltyrosine residues in the bradykinin analog RMP-7



Journal of Labelled Compounds and Radiopharmaceuticals 34(12): 1217-1226



A two step strategy was devised for the synthesis of 3H-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 3H-2 and Pd/C yielded 3H-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 3H-RMP-7. Rapid clearance from the blood and metabolism of RMP-7 to des-Arg-1-RMP-7 was observed in vivo in rats.

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Accession: 008246275

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DOI: 10.1002/jlcr.2580341211


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