Expedient synthesis and biochemical properties of an [125I]-labeled analogue of glyburide, a radioligand for ATP-inhibited potassium channels

…, JH Krushinski, DE Mais, DC Thompson…

Index: Robertson; Schober; Krushinski; Mais; Thompson; Gehlert Journal of Medicinal Chemistry, 1990 , vol. 33, # 12 p. 3124 - 3126

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Citation Number: 14

Abstract

Because ATP-inhibited K channels are present in vascular smooth muscle and brain tissue in low numbers (ca. 50-300 fmol/mg protein), a number of experiments we envisaged required an easily synthesized sulfonylurea-derived radioligand with a specific activity much greater than can be obtained with tritium-labeled probes (typically 20-100 Ci/mmol). Such an agent would be particularly useful for autoradiographic experiments to reduce the ...