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Structure-Activity Relationships of KATP Channel Openers

[ Vol. 6 , Issue. 10 ]


Raimund Mannhold   Pages 1031 - 1047 ( 17 )


Given their many physiological functions, KATP channels represent promising drug targets. Sulfonylureas like glibenclamide block KATP channels; they are used in the therapy of type 2 diabetes. Openers of KATP channels (KCOs) e.g. relax smooth muscle and induce hypotension. KCOs are chemically heterogeneous and include as different classes as the benzopyrans, cyanoguanidines, thioformamides, thiadiazines and pyridyl nitrates. Examples for new chemical entities more recently developed as KCOs include cyclobutenediones, dihydropyridine related structures, and tertiary carbinols. Structure-activity relationships of the main chemical classes of KCOs are discussed.


KATP channel openers (KCOs), structure-activity relationships, benzopyrans, cyanoguanidines, thioformamides, diazoxide, cyclobutenediones, dihydropyridine related structures, tertiary carbinols


Department of LaserMedicine, Molecular Drug Research Group, Heinrich-Heine-Universitat,UniversitatsstraBe 1, 40225 Dusseldorf, Germany.

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