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The preparation and characterization of [ 3 H] histamine.2HCl at high specific activity 1
Author(s) -
Filer Crist N.,
Ahern David G.
Publication year - 1987
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.2580240602
Subject(s) - chemistry , histamine , acetonitrile , tritium , imidazole , radioligand , histidine , radiochemistry , medicinal chemistry , stereochemistry , nuclear chemistry , organic chemistry , biochemistry , receptor , pharmacology , enzyme , nuclear physics , medicine , physics
Abstract [ 3 H] Histamine.2HCl will continue to play a key role in establishing the neurotransmitter status of histamine.2HCl. To more consistently achieve high specific activity in the preparation of the radioligand and incorporate as much tritium into the stable side chain positions as possible, we explored the use of alternative tritiation precursors. Imidazole 4‐acetonitrile ( 5 ) and 2,5‐diiodoimidazole‐4‐acetonitrile ( 6 ) were catalytically reduced with tritium gas and the radiolabeling specificity of the resulting [ 3 H] histamine.2HCl produced was confirmed by 3 H NMR.