Structure-activity relationships of K(ATP) channel openers.
Given their many physiological functions, K(ATP) channels represent promising drug targets. Sulfonylureas like glibenclamide block K(ATP) channels; they are used in the therapy of type 2 diabetes. Openers of K(ATP) 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.
Mannhold
Raimund
R
Department of Laser Medicine, Molecular Drug Research Group, Heinrich-Heine-Universität, Universitätsstrasse 1, 40225 Düsseldorf, Germany. mannhold@uni-duesseldorf.de
D000818:Animals; D001578:Benzopyrans / Q000494:pharmacology; D003503:Cyclobutanes / Q000494:pharmacology; D005559:Formamides / Q000494:pharmacology; D006146:Guanidines / Q000494:pharmacology; D006801:Humans; D000432:Methanol / Q000494:pharmacology; D015221:Potassium Channels / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013829:Thiadiazines / Q000494:pharmacology
D001578:Benzopyrans; D003503:Cyclobutanes; D005559:Formamides; D006146:Guanidines; D015221:Potassium Channels; D013829:Thiadiazines; C117780:mitochondrial K(ATP) channel; C009463:thioformamide; C004711:dicyandiamido; D000432:Methanol