Synthesis and activity on rat aorta rings and rat pancreatic β-cells of ring-opened analogues of benzopyran-type potassium channel activators
Copyright policy )Synthesis and activity on rat aorta rings and rat pancreatic β-cells of ring-opened analogues of benzopyran-type potassium channel activators
Ring-opened analogues of dihydrobenzopyran potassium channel openers (PCOs) were prepared and evaluated as putative PCOs on rat aorta rings (myorelaxant effect) and rat pancreatic beta-cells (inhibition of insulin secretion). These derivatives are characterized by the presence of a sulfonylurea, a urea or an amide function. Some compounds bearing an arylurea moiety provoked vasorelaxant effects and a marked inhibition of insulin release. Derivatives bearing a sulfonylurea or an amide function were, however, poorly active on both tissues. Structure-activity relationships and apparent tissue selectivity are discussed.
- Université Libre de Bruxelles Belgium
- University of Liège Belgium
- University of Jijel Algeria
Cromakalim, Potassium Channels, Muscle Relaxation, Benzopyrans -- chemistry, Wistar, In Vitro Techniques, Sciences de la santé humaine, Cromakalim -- analogs & derivatives, Insulin Antagonists, Potassium channel opener, Insulin-Secreting Cells, Chromans -- chemical synthesis, Insulin Secretion, Benzopyrans -- pharmacology, Insulin -- secretion, Aorta -- metabolism, Animals, Insulin, Benzopyrans, Human health sciences, Chromans, Rats, Wistar, Inhibition of insulin secretion, Pharmacy, pharmacology & toxicology, Aorta, Aorta -- drug effects, Ring-opened cromakalim analogues, Potassium Channels -- metabolism, Vasorelaxant effect, Pharmacie, pharmacologie & toxicologie, Sciences bio-médicales et agricoles, Rats, Chromans -- chemistry, Cromakalim -- pharmacology, Insulin-Secreting Cells -- metabolism, Insulin-Secreting Cells -- drug effects, Insulin Antagonists -- pharmacology, Benzopyrans -- chemical synthesis, Chromans -- pharmacology, Insulin Antagonists -- chemical synthesis, Insulin-Secreting Cells -- secretion, Muscle Relaxation -- drug effects
Cromakalim, Potassium Channels, Muscle Relaxation, Benzopyrans -- chemistry, Wistar, In Vitro Techniques, Sciences de la santé humaine, Cromakalim -- analogs & derivatives, Insulin Antagonists, Potassium channel opener, Insulin-Secreting Cells, Chromans -- chemical synthesis, Insulin Secretion, Benzopyrans -- pharmacology, Insulin -- secretion, Aorta -- metabolism, Animals, Insulin, Benzopyrans, Human health sciences, Chromans, Rats, Wistar, Inhibition of insulin secretion, Pharmacy, pharmacology & toxicology, Aorta, Aorta -- drug effects, Ring-opened cromakalim analogues, Potassium Channels -- metabolism, Vasorelaxant effect, Pharmacie, pharmacologie & toxicologie, Sciences bio-médicales et agricoles, Rats, Chromans -- chemistry, Cromakalim -- pharmacology, Insulin-Secreting Cells -- metabolism, Insulin-Secreting Cells -- drug effects, Insulin Antagonists -- pharmacology, Benzopyrans -- chemical synthesis, Chromans -- pharmacology, Insulin Antagonists -- chemical synthesis, Insulin-Secreting Cells -- secretion, Muscle Relaxation -- drug effects
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