open access

Vol 2, Supp. C (2001): Practical Diabetology
Review articles (submitted)
Published online: 2001-10-22
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New insights into the tissue specificity of sulphonylureas

Peter Proks, Frances M. Ashcroft

open access

Vol 2, Supp. C (2001): Practical Diabetology
Review articles (submitted)
Published online: 2001-10-22

Abstract

Sulphonylureas stimulate insulin secretion in type-2 diabetic patients by closing ATP-sensitive (KATP) potassium channels in the plasma membrane of pancreatic b-cells. This effect is mediated by binding of the drug to the sulphonylurea receptor (SUR 1) subunit of the channel. KATP channels are formed of two different types of subunit: a pore-forming subunit (usually Kir 6.2) and a sulphonylurea receptor subunit (SUR), which associate in a 4:4 heteromeric complex. Several different isoforms of SUR are known and KATP channels in different tissues possess different types of SUR subunit (SUR 1 in b-cells, SUR 2A in heart, and SUR 2B in smooth muscle). The sulphonylurea-sensitivity of KATP channels varies with the type of SUR subunit: thus, gliclazide and tolbutamide potently block the b-cell, but not the cardiac or smooth muscle types of KATP channel. In contrast, glibenclamide and glimepiride block all three types of KATP channel with similar potency.

Abstract

Sulphonylureas stimulate insulin secretion in type-2 diabetic patients by closing ATP-sensitive (KATP) potassium channels in the plasma membrane of pancreatic b-cells. This effect is mediated by binding of the drug to the sulphonylurea receptor (SUR 1) subunit of the channel. KATP channels are formed of two different types of subunit: a pore-forming subunit (usually Kir 6.2) and a sulphonylurea receptor subunit (SUR), which associate in a 4:4 heteromeric complex. Several different isoforms of SUR are known and KATP channels in different tissues possess different types of SUR subunit (SUR 1 in b-cells, SUR 2A in heart, and SUR 2B in smooth muscle). The sulphonylurea-sensitivity of KATP channels varies with the type of SUR subunit: thus, gliclazide and tolbutamide potently block the b-cell, but not the cardiac or smooth muscle types of KATP channel. In contrast, glibenclamide and glimepiride block all three types of KATP channel with similar potency.
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Keywords

pochodna sulfonylomocznika; wydzielanie insuliny; cukrzyca

About this article
Title

New insights into the tissue specificity of sulphonylureas

Journal

Clinical Diabetology

Issue

Vol 2, Supp. C (2001): Practical Diabetology

Pages

1-6

Published online

2001-10-22

Keywords

pochodna sulfonylomocznika
wydzielanie insuliny
cukrzyca

Authors

Peter Proks
Frances M. Ashcroft

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