{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2024,11,1]],"date-time":"2024-11-01T04:10:43Z","timestamp":1730434243441,"version":"3.28.0"},"reference-count":36,"publisher":"Oxford University Press (OUP)","issue":"3","license":[{"start":{"date-parts":[[2002,3,1]],"date-time":"2002-03-01T00:00:00Z","timestamp":1014940800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/academic.oup.com\/journals\/pages\/open_access\/funder_policies\/chorus\/standard_publication_model"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"published-print":{"date-parts":[[2002,3,1]]},"abstract":"<jats:title>Abstract<\/jats:title>\n               <jats:p>The actions of agents which modulate ATP-sensitive potassium (KATP) channels in excitable cells were investigated in an in-vitro preparation of mouse ileum from which the mucosa was removed. A range of potassium channel openers of diverse structure, cromakalim (0.1\u2013100 \u03bcM), pinacidil (0.1\u2013200 \u03bcM) and its analogue P1060 (0.1\u2013200 \u03bcM), SDZ PCO400 ((-)-(3S,4R)-3,4-dihydro-3-hydroxy-2,2-dimethyl-4-(3-oxo-cyclopent-1-enyloxy)-2H-1-benzopyran-6-carbonitrile) (0.3\u201360 \u03bcM), caused concentration-related reduction in twitch height of electrical field stimulated ileum. P1060 and SDZ PCO400 were the most potent agents; diazoxide (0.1\u2013100 \u03bcM) was without effect. The order of inhibitory potency, based on EC50 values (concentration of a relaxant producing 50% of the maximum inhibition of twitch) was: P1060 = SDZ PCO400 &amp;gt; cromakalim &amp;gt; pinacidil. The relaxant effect of the potassium channel openers was antagonised by the sulfonylureas glibenclamide (0.1-1.0 \u03bcM) and glipizide (3\u201330 \u03bcM) but the nature of the antagonism differed. Antagonism of P1060 and SDZ PCO400 by glibenclamide appeared to be competitive whereas the antagonism of relaxation induced by cromakalim and pinacidil was apparently not competitive. Both phentolamine (1\u201310 \u03bcM) and tolbutamide (100\u2013300 \u03bcM) showed competitive antagonism of the actions of pinacidil while yohimbine (1\u201320 \u03bcM) did not antagonise relaxation and appeared to have actions at sites other than the KATP channel in this preparation. The relative effectiveness of the antagonists on pinacidil-induced relaxation was found to be: glibenclamide &amp;gt;phentolamine &amp;gt;tolbutamide &amp;gt;yohimbine, which is in agreement with studies in other tissues. The results show that many structurally diverse potassium channel openers are potent relaxants of mouse ileum. These observations are consistent with the existence of ATP-dependent K+ channels in murine intestinal muscle which, however, differ somewhat in properties from those reported for vascular muscle and pancreatic \u03b2-cells.<\/jats:p>","DOI":"10.1211\/0022357021778501","type":"journal-article","created":{"date-parts":[[2002,10,11]],"date-time":"2002-10-11T20:14:04Z","timestamp":1034367244000},"page":"425-433","source":"Crossref","is-referenced-by-count":3,"title":["Characterisation of the effects of potassium channel modulating agents on mouse intestinal smooth muscle"],"prefix":"10.1093","volume":"54","author":[{"given":"Chi-Kong","family":"Yeung","sequence":"first","affiliation":[{"name":"The School of Pharmacy, University of Bradford , West Yorkshire, BD7 1DP,","place":["UK"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Janice R","family":"McCurrie","sequence":"additional","affiliation":[{"name":"The School of Pharmacy, University of Bradford , West Yorkshire, BD7 1DP,","place":["UK"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Diana","family":"Wood","sequence":"additional","affiliation":[{"name":"The School of Pharmacy, University of Bradford , West Yorkshire, BD7 1DP,","place":["UK"]}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"286","published-online":{"date-parts":[[2002,3,1]]},"reference":[{"key":"2024103109374846700_cit1","doi-asserted-by":"crossref","first-page":"373","DOI":"10.1016\/0014-2999(90)94202-9","article-title":"Mechanisms of pinacidil-induced vasodilation","volume":"190","author":"Anabuki","year":"1990","journal-title":"Eur. 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