Vasorelaxant effects of the potassium channel opener SR 47063 on the isolated human saphenous vein and rat aorta

AUTOR(ES)

Criddle, D.N., de Moura, R.S.

FONTE

Brazilian Journal of Medical and Biological Research

DATA DE PUBLICAÇÃO

2000-08

RESUMO

The vasorelaxant effects of SR 47063 (4-(2-cyanimino-1,2-dihydropyrid-1-yl)-2,2-dimethyl-6-nitrochromene), a new K+-channel opener structurally related to levcromakalim, were examined in isolated human saphenous vein (HSV) and rat aorta (RA). HSV or RA rings were precontracted with either KCl or noradrenaline and cumulative relaxant concentration-response curves were obtained for SR 47063 (0.1 nM to 1 µM) in the presence or absence of 3 µM glibenclamide. SR 47063 potently relaxed HSV and RA precontracted with 20 mM (but not 60 mM) KCl or 10 µM noradrenaline in a concentration-dependent manner, showing slightly greater activity in the aorta. The potency of the effect of SR 47063 on HSV and RA was 12- and 58-fold greater, respectively, than that reported for the structurally related K+-channel opener levcromakalim. The vasorelaxant action of SR 47063 in both blood vessels was strongly inhibited by 3 µM glibenclamide, consistent with a mechanism of action involving ATP-dependent K+-channels.

Documentos Relacionados

• Effects of vasoactive neuropeptides on human saphenous vein.
• The vasorelaxant effect of H2S as a novel endogenous gaseous KATP channel opener
• Effects of in vitro Amitriptyline, Fluoxetine, Tranylcypromine and Venlafaxine on Saphenous Vein Grafts
• Effects of membrane potential and muscarine on potassium M-channel kinetics in rat sympathetic neurones.
• Effects of raised extracellular potassium on the excitability of, and hormone release from, the isolated rat neurohypophysis.