Vasorelaxing properties of some phenylacridine type potassium channel openers in isolated rabbit thoracic arteries

In this study, 12 new 2,2,7,7-tetramethyl-9-aryl-2,3,4,5,6,7,9,10-octahydro-1,8-acridindione derivatives were synthesised and their effects on vascular potassium channels and mechanism of induced relaxations on phenylephrine-induced contractile responses in isolated rabbit thoracic arteries was inve...

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Veröffentlicht in:	European journal of medicinal chemistry 2002-06, Vol.37 (6), p.519-523
Hauptverfasser:	BERKAN, Öcal, SARAC, Bülent, SIMSEK, Rahime, YILDIRIM, Sahin, SARIOGLU, Yusuf, SAFAK, Cihat
Format:	Artikel
Sprache:	eng
Schlagworte:	Acridindione Acridines - chemical synthesis Acridines - pharmacology Animals Aorta, Thoracic - drug effects Biological and medical sciences Cardiovascular system Glyburide - pharmacology Hypoglycemic Agents - pharmacology In Vitro Techniques Kinetics Magnetic Resonance Spectroscopy Male Medical sciences Molecular Weight Muscle, Smooth, Vascular - drug effects Pharmacology. Drug treatments Phenylephrine - antagonists & inhibitors Pinacidil - pharmacology Potassium channel openers Potassium Channels - agonists Rabbits Synthesis Tetraethylammonium Compounds - pharmacology Vasoconstrictor Agents - antagonists & inhibitors Vasodilator Agents - chemical synthesis Vasodilator Agents - pharmacology Vasodilator agents. Cerebral vasodilators
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Zusammenfassung:	In this study, 12 new 2,2,7,7-tetramethyl-9-aryl-2,3,4,5,6,7,9,10-octahydro-1,8-acridindione derivatives were synthesised and their effects on vascular potassium channels and mechanism of induced relaxations on phenylephrine-induced contractile responses in isolated rabbit thoracic arteries was investigated. Pinacidil was used as standard potassium channel openers in this study. Compounds 1– 12 and pinacidil exerted concentration-dependent relaxation responses precontracted phenylephrine in the aortic rings with the efficacy order: 11>pinacidil> 7> 2> 8> 3> 1> 4> 10> 6> 9> 5> 12.
ISSN:	0223-5234 1768-3254
DOI:	10.1016/S0223-5234(02)01374-0