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...
Main Authors: | , , , , |
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Format: | Journal article |
Language: | English |
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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. |
first_indexed | 2024-03-06T21:17:06Z |
format | Journal article |
id | oxford-uuid:4024758f-a903-462c-83eb-6fd8189f4563 |
institution | University of Oxford |
language | English |
last_indexed | 2024-03-06T21:17:06Z |
publishDate | 1989 |
publisher | Springer-Verlag |
record_format | dspace |
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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