Pharmacological property of a new potassium channel opener, TCV-295 in vitro.
نویسندگان
چکیده
منابع مشابه
Stoichiometry of potassium channel opener action.
Potassium channel openers (KCOs; e.g., P1075, pinacidil) exert their effects on excitable cells by opening ATP-sensitive potassium channels. These channels are heteromultimers composed with a 4:4 stoichiometry of an inwardly rectifying K(+) channel subunit plus a regulatory subunit comprising the receptor sites for hypoglycemic sulfonylureas and KCOs (a sulfonylurea receptor). To elucidate stoi...
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OBJECTIVE Endothelial dysfunction is an early risk factor for cardiovascular disease and hypertension. Mechanisms that participate in endothelial dysfunction include reduced nitric oxide (NO) generation and increased endothelin-1 (ET-1) generation. Endothelial ATP-sensitive potassium (K(ATP)) channels are responsible for maintaining the resting potential of endothelial cells and modulating the ...
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In the early 1990s, researchers began looking at potassium channel openers for seizure control. Over the past 10 years, in vitro research and animal studies demonstrated that potassium channel openers could control seizure activity in a dose-dependent way.1-4 Clinical trials are now confirming these findings.5 Among the calcium channel openers that have been studied, the agent retigabine has co...
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Bovine adrenal zona fasciculata cells express a novel K+ current (IAC) that sets the resting potential while it couples adrenocorticotropin and angiotensin II receptors to membrane depolarization and cortisol secretion. IAC is distinctive among K+ channels both in its activation by ATP and its inhibition by cyclic AMP. Whole-cell and single-channel patch-clamp recording was used to establish a ...
متن کاملNovel potassium channel opener prodrugs with a slow onset and prolonged duration of action.
(-)-(3S,4R,1'R,6'S)-4-(4-Benzyl-5-oxo-3,4-diazabicyclo[4.1.0]hept-2-en-2 -yloxy)-3,4-dihydro-3-hydroxy-2,2-dimethyl-2H-1-benzopyran-6-carbo nitrile and its derivatives with a modified benzyl group were synthesized with the objective of discovering novel ATP-sensitive potassium channel openers (PCOs) with a slow onset of action and a reduced tendency to induce tachycardia. Among the compounds sy...
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ژورنال
عنوان ژورنال: Japanese Journal of Pharmacology
سال: 1993
ISSN: 0021-5198
DOI: 10.1016/s0021-5198(19)51750-4