Characterisation of sulphonylurea and ATP-regulated K+ channels in rat pancreatic A-cells.

We have monitored whole-cell and single channel ATP-sensitive K+ (KATP) currents in isolated rat glucagon-secreting pancreatic A-cells. Tolbutamide produced a concentration-dependent decrease in the whole-cell KATP conductance (Ki = 6 microM) and initiated action potential firing. The K+ channel ope...

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Main Authors: Bokvist, K, Olsen, H, Høy, M, Gotfredsen, C, Holmes, W, Buschard, K, Rorsman, P, Gromada, J
格式: Journal article
語言:English
出版: 1999
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author Bokvist, K
Olsen, H
Høy, M
Gotfredsen, C
Holmes, W
Buschard, K
Rorsman, P
Gromada, J
author_facet Bokvist, K
Olsen, H
Høy, M
Gotfredsen, C
Holmes, W
Buschard, K
Rorsman, P
Gromada, J
author_sort Bokvist, K
collection OXFORD
description We have monitored whole-cell and single channel ATP-sensitive K+ (KATP) currents in isolated rat glucagon-secreting pancreatic A-cells. Tolbutamide produced a concentration-dependent decrease in the whole-cell KATP conductance (Ki = 6 microM) and initiated action potential firing. The K+ channel opener diazoxide, but not cromakalim or pinacidil, inhibited electrical activity and increased the whole-cell K+ conductance fourfold. ATP applied to the intracellular face of the membrane inhibited KATP channel activity with a Ki of 17 microM, an effect that could be counteracted by Mg-ADP and Mg-GDP. GTP and UTP did not affect KATP channel activity. Phosphatidylinositol 4,5-bisphosphate activated KATP channels inhibited by ATP after a delay of 90 s. In situ hybridisation demonstrated the expression of the mRNA encoding KATP channel subunits Kir6.2 and SUR1 but not Kir6.1 and SUR2. We conclude that rat pancreatic A-cells express KATP channels with the nucleotide-, sulphonylurea- and K+ channel-opener sensitivities expected for a channel formed by Kir6.2 and SUR1 subunits.
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spelling oxford-uuid:4b9740f1-85fa-4f09-b227-20bc78d4facb2022-03-26T15:44:33ZCharacterisation of sulphonylurea and ATP-regulated K+ channels in rat pancreatic A-cells.Journal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:4b9740f1-85fa-4f09-b227-20bc78d4facbEnglishSymplectic Elements at Oxford1999Bokvist, KOlsen, HHøy, MGotfredsen, CHolmes, WBuschard, KRorsman, PGromada, JWe have monitored whole-cell and single channel ATP-sensitive K+ (KATP) currents in isolated rat glucagon-secreting pancreatic A-cells. Tolbutamide produced a concentration-dependent decrease in the whole-cell KATP conductance (Ki = 6 microM) and initiated action potential firing. The K+ channel opener diazoxide, but not cromakalim or pinacidil, inhibited electrical activity and increased the whole-cell K+ conductance fourfold. ATP applied to the intracellular face of the membrane inhibited KATP channel activity with a Ki of 17 microM, an effect that could be counteracted by Mg-ADP and Mg-GDP. GTP and UTP did not affect KATP channel activity. Phosphatidylinositol 4,5-bisphosphate activated KATP channels inhibited by ATP after a delay of 90 s. In situ hybridisation demonstrated the expression of the mRNA encoding KATP channel subunits Kir6.2 and SUR1 but not Kir6.1 and SUR2. We conclude that rat pancreatic A-cells express KATP channels with the nucleotide-, sulphonylurea- and K+ channel-opener sensitivities expected for a channel formed by Kir6.2 and SUR1 subunits.
spellingShingle Bokvist, K
Olsen, H
Høy, M
Gotfredsen, C
Holmes, W
Buschard, K
Rorsman, P
Gromada, J
Characterisation of sulphonylurea and ATP-regulated K+ channels in rat pancreatic A-cells.
title Characterisation of sulphonylurea and ATP-regulated K+ channels in rat pancreatic A-cells.
title_full Characterisation of sulphonylurea and ATP-regulated K+ channels in rat pancreatic A-cells.
title_fullStr Characterisation of sulphonylurea and ATP-regulated K+ channels in rat pancreatic A-cells.
title_full_unstemmed Characterisation of sulphonylurea and ATP-regulated K+ channels in rat pancreatic A-cells.
title_short Characterisation of sulphonylurea and ATP-regulated K+ channels in rat pancreatic A-cells.
title_sort characterisation of sulphonylurea and atp regulated k channels in rat pancreatic a cells
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