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Synthesis of a 125I labelled azido-substituted glibenclamide analogue for photoaffinity labelling of the sulfonylurea receptor

✍ Scribed by Franz Chudziak; Mathias Schwanstecher; Hartmut Laatsch; Uwe Panten


Publisher
John Wiley and Sons
Year
1994
Tongue
French
Weight
286 KB
Volume
34
Category
Article
ISSN
0022-2135

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✦ Synopsis


Abstract

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).


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