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Synthesis of a 125 I labelled azido‐substituted glibenclamide analogue for photoaffinity labelling of the sulfonylurea receptor
Author(s) -
Chudziak Franz,
Schwanstecher Mathias,
Laatsch Hartmut,
Panten Uwe
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.2580340713
Subject(s) - chemistry , glibenclamide , sulfonylurea , labelling , yield (engineering) , chloramine t , receptor , photoaffinity labeling , ligand (biochemistry) , stereochemistry , chemical synthesis , biochemistry , organic chemistry , in vitro , medicine , endocrinology , insulin , materials science , metallurgy , diabetes mellitus
N‐{4‐(2‐{4‐Azido‐2‐hydroxy‐5‐[ 125 I]iodobenzamido}ethyl)benzenesul]‐N′‐cyclohexylurea has been prepared as a novel photoaffinity ligand for the sulfonylurea receptor. This involved synthesis of a 4‐azidosalicyloyl analogue of glibenclamide and treatment of the analogue with Na 125 I and chloramine‐T. Purification by HPLC gave the radiolabelled sulfonylurea in 56% radiochemical yield and high specific activity (2130 Ci/mmol).