The ATP- and tolbutamide-sensitivity of the ATP-sensitive K-channel from human pancreatic B cells.

The ATP- and sulphonylurea-sensitivity of the ATP-sensitive K-channel was measured in human pancreatic B cells. In inside-out patches, half-maximal inhibition of channel activity was produced by 10 mumol/l ATP (with 2 mM Mg2+) and ATP-inhibition was partially antagonised by ADP. A significantly lowe...

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Main Authors: Ashcroft, F, Kakei, M, Gibson, J, Gray, D, Sutton, R
Format: Journal article
Language:English
Published: Springer-Verlag 1989
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author Ashcroft, F
Kakei, M
Gibson, J
Gray, D
Sutton, R
author_facet Ashcroft, F
Kakei, M
Gibson, J
Gray, D
Sutton, R
author_sort Ashcroft, F
collection OXFORD
description The ATP- and sulphonylurea-sensitivity of the ATP-sensitive K-channel was measured in human pancreatic B cells. In inside-out patches, half-maximal inhibition of channel activity was produced by 10 mumol/l ATP (with 2 mM Mg2+) and ATP-inhibition was partially antagonised by ADP. A significantly lower sensitivity to ATP was found in whole-cell recordings. Tolbutamide inhibited whole-cell ATP-sensitive K-currents half-maximally at 18 mumol/l; the sensitivity to tolbutamide was somewhat less in the inside-out patch. Ca-activated K-channels were unaffected by tolbutamide (10 mmol/l). These results resemble those found for rodent B cells and suggest that sulphonylureas exert their therapeutic effects in Type 2 (non-insulin dependent) diabetes by inhibition of the ATP-sensitive K-channel.
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spelling oxford-uuid:4024758f-a903-462c-83eb-6fd8189f45632022-03-26T14:36:22ZThe ATP- and tolbutamide-sensitivity of the ATP-sensitive K-channel from human pancreatic B cells.Journal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:4024758f-a903-462c-83eb-6fd8189f4563EnglishSymplectic Elements at OxfordSpringer-Verlag1989Ashcroft, FKakei, MGibson, JGray, DSutton, RThe ATP- and sulphonylurea-sensitivity of the ATP-sensitive K-channel was measured in human pancreatic B cells. In inside-out patches, half-maximal inhibition of channel activity was produced by 10 mumol/l ATP (with 2 mM Mg2+) and ATP-inhibition was partially antagonised by ADP. A significantly lower sensitivity to ATP was found in whole-cell recordings. Tolbutamide inhibited whole-cell ATP-sensitive K-currents half-maximally at 18 mumol/l; the sensitivity to tolbutamide was somewhat less in the inside-out patch. Ca-activated K-channels were unaffected by tolbutamide (10 mmol/l). These results resemble those found for rodent B cells and suggest that sulphonylureas exert their therapeutic effects in Type 2 (non-insulin dependent) diabetes by inhibition of the ATP-sensitive K-channel.
spellingShingle Ashcroft, F
Kakei, M
Gibson, J
Gray, D
Sutton, R
The ATP- and tolbutamide-sensitivity of the ATP-sensitive K-channel from human pancreatic B cells.
title The ATP- and tolbutamide-sensitivity of the ATP-sensitive K-channel from human pancreatic B cells.
title_full The ATP- and tolbutamide-sensitivity of the ATP-sensitive K-channel from human pancreatic B cells.
title_fullStr The ATP- and tolbutamide-sensitivity of the ATP-sensitive K-channel from human pancreatic B cells.
title_full_unstemmed The ATP- and tolbutamide-sensitivity of the ATP-sensitive K-channel from human pancreatic B cells.
title_short The ATP- and tolbutamide-sensitivity of the ATP-sensitive K-channel from human pancreatic B cells.
title_sort atp and tolbutamide sensitivity of the atp sensitive k channel from human pancreatic b cells
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