Biomaterial Database

Vasodilative properties of BPDZ 79, a new potassium channel opener, in isolated aorta. 1997

Z Y Fang, and J Fontaine

Laboratoire de Pharmacologie, Universite Libre de Bruxells, Belgium.

OBJECTIVE To compare the effect of a novel potassium channel opener 3-(1',2',2'-trimethylpropyl)amine-4H-pyrido (2,3-e)-1,2,4-thiadiazine, 1-dioxide (BPDZ 79), with diazoxide on aorta. METHODS Muscle tension of rat aorta was compared with adjacent aortic rings without endothelium. One ring was precontracted with KCl 80 mmol.L-1. Three rings were precontracted with KCl 80 mmol.L-1, and two of them were incubated with glibenclamide (0, 1, and 10 mumol.L-1). 86Rb outflow from rat aorta was measured in the presence of glibenclamide 10 mumol.L-1. RESULTS BPDZ 79 and diazoxide provoked concentration-dependent and endothelium-independent relaxation of the vasoconstriction evoked by KCl 30 mmol.L-1, but not by 80 mmol.L-1. BPDZ 79 showed more potent vasorelaxation and 86Rb outflow than diazoxide. After incubation with glibenclamide (1 and 10 mumol.L-1), an inhibitor of the ATP-sensitive K+ channels, the relaxation induced by BPDZ 79 and diazoxide were decreased with the same pattern. CONCLUSIONS BPDZ 79 is a potent vasodilator by opening potassium channels.

UI	MeSH Term	Description	Entries
D008297	Male		Males
D003981	Diazoxide	A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.	Hyperstat,Proglycem
D004305	Dose-Response Relationship, Drug	The relationship between the dose of an administered drug and the response of the organism to the drug.	Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D005905	Glyburide	An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide	Glibenclamide,Daonil,Diabeta,Euglucon 5,Euglucon N,Glybenclamide,HB-419,HB-420,Maninil,Micronase,Neogluconin,HB 419,HB 420,HB419,HB420
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D001013	Aorta, Thoracic	The portion of the descending aorta proceeding from the arch of the aorta and extending to the DIAPHRAGM, eventually connecting to the ABDOMINAL AORTA.	Aorta, Ascending,Aorta, Descending,Aortic Arch,Aortic Root,Arch of the Aorta,Descending Aorta,Sinotubular Junction,Ascending Aorta,Thoracic Aorta,Aortic Roots,Arch, Aortic,Ascending Aortas,Junction, Sinotubular,Root, Aortic,Sinotubular Junctions
D013829	Thiadiazines
D014664	Vasodilation	The physiological widening of BLOOD VESSELS by relaxing the underlying VASCULAR SMOOTH MUSCLE.	Vasodilatation,Vasorelaxation,Vascular Endothelium-Dependent Relaxation,Endothelium-Dependent Relaxation, Vascular,Relaxation, Vascular Endothelium-Dependent,Vascular Endothelium Dependent Relaxation
D014665	Vasodilator Agents	Drugs used to cause dilation of the blood vessels.	Vasoactive Antagonists,Vasodilator,Vasodilator Agent,Vasodilator Drug,Vasorelaxant,Vasodilator Drugs,Vasodilators,Vasorelaxants,Agent, Vasodilator,Agents, Vasodilator,Antagonists, Vasoactive,Drug, Vasodilator,Drugs, Vasodilator
D015221	Potassium Channels	Cell membrane glycoproteins that are selectively permeable to potassium ions. At least eight major groups of K channels exist and they are made up of dozens of different subunits.	Ion Channels, Potassium,Ion Channel, Potassium,Potassium Channel,Potassium Ion Channels,Channel, Potassium,Channel, Potassium Ion,Channels, Potassium,Channels, Potassium Ion,Potassium Ion Channel