Block of ATP-sensitive K+ channels in isolated mouse pancreatic beta-cells by 2,3-butanedione monoxime.
1. The patch-clamp technique has been used to examine the action of the chemical phosphatase 2,3-butanedione monoxime (BDM) on ATP-sensitive K+ channels (KATP-channels) from mouse isolated pancreatic beta-cells in the absence of ATP and Mg2+. 2. BDM reversibly inhibited whole-cell KATP-currents with...
| Main Authors: | , , |
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| Format: | Journal article |
| Language: | English |
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1994
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| _version_ | 1797105688221057024 |
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| author | Smith, P Williams, B Ashcroft, F |
| author_facet | Smith, P Williams, B Ashcroft, F |
| author_sort | Smith, P |
| collection | OXFORD |
| description | 1. The patch-clamp technique has been used to examine the action of the chemical phosphatase 2,3-butanedione monoxime (BDM) on ATP-sensitive K+ channels (KATP-channels) from mouse isolated pancreatic beta-cells in the absence of ATP and Mg2+. 2. BDM reversibly inhibited whole-cell KATP-currents with a concentration for half maximal inhibition (K(i)) of 15 +/- 1 mM and a Hill coefficient (n) of 2.5 +/- 0.2 (n = 4). 3. In outside-out patches, external BDM reversibly reduced the activity of single KATP-channels with an affinity similar to that observed in whole-cell recordings (K(i) = 11 +/- 3 mM, n = 2.0 +/- 0.3, n = 7). In inside-out patches, internally applied BDM also reversibly blocked the activity of KATP-channels (K(i) = 31 +/- 2 mM, n = 2.2 +/- 0.4, n = 8). In both excised patch configurations, BDM decreased the mean open life-time and the burst duration, thereby producing a decrease in the channel open probability. The drug had no effect on the short intraburst closed times. 4. BDM had no effect on the single-channel current amplitude. 5. The results suggest that BDM blocks the KATP-channel directly, by mechanisms independent of channel dephosphorylation. |
| first_indexed | 2024-03-07T06:50:54Z |
| format | Journal article |
| id | oxford-uuid:fc852347-ef4a-4f54-a454-4c41a0c74ca0 |
| institution | University of Oxford |
| language | English |
| last_indexed | 2024-03-07T06:50:54Z |
| publishDate | 1994 |
| record_format | dspace |
| spelling | oxford-uuid:fc852347-ef4a-4f54-a454-4c41a0c74ca02022-03-27T13:21:26ZBlock of ATP-sensitive K+ channels in isolated mouse pancreatic beta-cells by 2,3-butanedione monoxime.Journal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:fc852347-ef4a-4f54-a454-4c41a0c74ca0EnglishSymplectic Elements at Oxford1994Smith, PWilliams, BAshcroft, F1. The patch-clamp technique has been used to examine the action of the chemical phosphatase 2,3-butanedione monoxime (BDM) on ATP-sensitive K+ channels (KATP-channels) from mouse isolated pancreatic beta-cells in the absence of ATP and Mg2+. 2. BDM reversibly inhibited whole-cell KATP-currents with a concentration for half maximal inhibition (K(i)) of 15 +/- 1 mM and a Hill coefficient (n) of 2.5 +/- 0.2 (n = 4). 3. In outside-out patches, external BDM reversibly reduced the activity of single KATP-channels with an affinity similar to that observed in whole-cell recordings (K(i) = 11 +/- 3 mM, n = 2.0 +/- 0.3, n = 7). In inside-out patches, internally applied BDM also reversibly blocked the activity of KATP-channels (K(i) = 31 +/- 2 mM, n = 2.2 +/- 0.4, n = 8). In both excised patch configurations, BDM decreased the mean open life-time and the burst duration, thereby producing a decrease in the channel open probability. The drug had no effect on the short intraburst closed times. 4. BDM had no effect on the single-channel current amplitude. 5. The results suggest that BDM blocks the KATP-channel directly, by mechanisms independent of channel dephosphorylation. |
| spellingShingle | Smith, P Williams, B Ashcroft, F Block of ATP-sensitive K+ channels in isolated mouse pancreatic beta-cells by 2,3-butanedione monoxime. |
| title | Block of ATP-sensitive K+ channels in isolated mouse pancreatic beta-cells by 2,3-butanedione monoxime. |
| title_full | Block of ATP-sensitive K+ channels in isolated mouse pancreatic beta-cells by 2,3-butanedione monoxime. |
| title_fullStr | Block of ATP-sensitive K+ channels in isolated mouse pancreatic beta-cells by 2,3-butanedione monoxime. |
| title_full_unstemmed | Block of ATP-sensitive K+ channels in isolated mouse pancreatic beta-cells by 2,3-butanedione monoxime. |
| title_short | Block of ATP-sensitive K+ channels in isolated mouse pancreatic beta-cells by 2,3-butanedione monoxime. |
| title_sort | block of atp sensitive k channels in isolated mouse pancreatic beta cells by 2 3 butanedione monoxime |
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