ORIGINAL ARTICLE. Differential effects of sulphonylureas on the vasodilatory response evoked by KATP channel openers

Autor:	Denis Ravel, Jean Auclair, Gervais Néliat, Eliete Bouskela, Nigel Levens, Michel Félétou
Rok vydání:	2003
Předmět:	Pharmacology medicine.medical_specialty Vasodilation Glibenclamide chemistry.chemical_compound Glimepiride Endocrinology chemistry In vivo Cheek pouch Internal medicine medicine Diazoxide Pharmacology (medical) Gliclazide Cromakalim medicine.drug
Zdroj:	Fundamental and Clinical Pharmacology. 17:61-69
ISSN:	1472-8206 0767-3981
DOI:	10.1046/j.1472-8206.2003.00144.x
Popis:	The potency of three sulphonylureas, glibenclamide, glimepiride and gliclazide in antagonizing the vasorelaxant action of openers of adenosine triphosphate (ATP)-regulated K+ channel (KATP) was studied in vivo and in vitro in micro- and macrovessels, respectively. In the hamster cheek pouch, the vasodilatation and the increase in vascular diameter and blood flow induced by diazoxide were markedly reduced by the addition of either glibenclamide or glimepiride (0.8 microm) while they were not affected by gliclazide up to 12 microm. Similarly, in rat and guinea-pig isolated aortic rings, glibenclamide, glimepiride and gliclazide reduced the vasodilator activity of cromakalim. However, the inhibitory effect of gliclazide was considerably less when compared with either glimepiride or glibenclamide. These results suggest that, in contrast to glibenclamide and glimepiride, therapeutically relevant concentrations of gliclazide do not block the vascular effects produced by KATP channel openers in various in vitro and in vivo animal models.
Databáze:	OpenAIRE
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