Abstract

Phentolamine and related imidazolines inhibit K ATP channel activity in the pancreatic β cell. In the present study, the effects of several imidazoline-based compounds were examined upon K ATP channel activity in guinea pig ventricular myocytes. Phentolamine produced a potent inhibition of K ATP channel activity when examined in either excised inside-out patches or in the whole-cell configuration. This effect was unrelated to phentolamine's ability to antagonise α-adrenoceptors since the non-selective α-adrenoceptor antagonists, benextramine and phenoxybenzamine, failed to affect channel activity. Furthermore, the α-adrenoceptor agonist clonidine together with several related imidazolines inhibited channel activity. This suggests that imidazoline compounds modulate K ATP channel activity in guinea pig ventricular myocytes and this may have clinical implications for the use of such agents as hypoglycemic drugs.

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