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Glibenclamide is a competitive antagonist of the thromboxane A2 receptor in dog coronary artery in vitro
1 Glibenclamide, a sulphonylurea oral hypoglycaemic agent is a widely used antagonist of cromakalim‐activated K+ channels in smooth muscle. 2 In isolated ring segments of the large circumflex coronary artery from the dog, glibenclamide (1–30 μm) caused a concentration‐dependent reduction in both spo...
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| Published in: | British journal of pharmacology 1990-06, Vol.100 (2), p.375-378 |
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| Language: | English |
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| container_end_page | 378 |
| container_issue | 2 |
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| container_title | British journal of pharmacology |
| container_volume | 100 |
| creator | Cocks, Thomas M. King, Susannah J. Angus, James A. |
| description | 1
Glibenclamide, a sulphonylurea oral hypoglycaemic agent is a widely used antagonist of cromakalim‐activated K+ channels in smooth muscle.
2
In isolated ring segments of the large circumflex coronary artery from the dog, glibenclamide (1–30 μm) caused a concentration‐dependent reduction in both spontaneous isometric force and contractions induced by U46619, a thromboxane A2‐mimetic.
3
Glibenclamide behaved as a competitive antagonist of U46619 with an estimated pKB (‐log KB) value of 6.2 by Schild regression analysis (slope 1.07).
4
Glibenclamide (30 μm) was apparently selective since it had no effect on the concentration‐contraction curves to endothelin‐1, noradrenaline or KCl.
5
We suggest that this additional property of glibenclamide should be considered in any smooth muscle study where active force is raised by either the exogenous application or endogenous generation of thromboxane A2. |
| doi_str_mv | 10.1111/j.1476-5381.1990.tb15812.x |
| format | article |
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Glibenclamide, a sulphonylurea oral hypoglycaemic agent is a widely used antagonist of cromakalim‐activated K+ channels in smooth muscle.
2
In isolated ring segments of the large circumflex coronary artery from the dog, glibenclamide (1–30 μm) caused a concentration‐dependent reduction in both spontaneous isometric force and contractions induced by U46619, a thromboxane A2‐mimetic.
3
Glibenclamide behaved as a competitive antagonist of U46619 with an estimated pKB (‐log KB) value of 6.2 by Schild regression analysis (slope 1.07).
4
Glibenclamide (30 μm) was apparently selective since it had no effect on the concentration‐contraction curves to endothelin‐1, noradrenaline or KCl.
5
We suggest that this additional property of glibenclamide should be considered in any smooth muscle study where active force is raised by either the exogenous application or endogenous generation of thromboxane A2.</description><identifier>ISSN: 0007-1188</identifier><identifier>EISSN: 1476-5381</identifier><identifier>DOI: 10.1111/j.1476-5381.1990.tb15812.x</identifier><identifier>PMID: 2143093</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid ; Animals ; Coronary Vessels - drug effects ; Coronary Vessels - metabolism ; Dogs ; Endothelins ; Endothelium, Vascular - drug effects ; Endothelium, Vascular - physiology ; Female ; Glyburide - pharmacology ; In Vitro Techniques ; Isometric Contraction ; Male ; Muscle Contraction - drug effects ; Muscle, Smooth, Vascular - drug effects ; Muscle, Smooth, Vascular - metabolism ; Norepinephrine - pharmacology ; Peptides - pharmacology ; Potassium Chloride - pharmacology ; Prostaglandin Endoperoxides, Synthetic - antagonists & inhibitors ; Prostaglandin Endoperoxides, Synthetic - pharmacology ; Receptors, Prostaglandin - antagonists & inhibitors ; Receptors, Thromboxane ; Thromboxane A2 - metabolism ; Tolbutamide - pharmacology</subject><ispartof>British journal of pharmacology, 1990-06, Vol.100 (2), p.375-378</ispartof><rights>1990 British Pharmacological Society</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1917442/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1917442/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,723,776,780,881,27901,27902,53766,53768</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2143093$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Cocks, Thomas M.</creatorcontrib><creatorcontrib>King, Susannah J.</creatorcontrib><creatorcontrib>Angus, James A.</creatorcontrib><title>Glibenclamide is a competitive antagonist of the thromboxane A2 receptor in dog coronary artery in vitro</title><title>British journal of pharmacology</title><addtitle>Br J Pharmacol</addtitle><description>1
Glibenclamide, a sulphonylurea oral hypoglycaemic agent is a widely used antagonist of cromakalim‐activated K+ channels in smooth muscle.
2
In isolated ring segments of the large circumflex coronary artery from the dog, glibenclamide (1–30 μm) caused a concentration‐dependent reduction in both spontaneous isometric force and contractions induced by U46619, a thromboxane A2‐mimetic.
3
Glibenclamide behaved as a competitive antagonist of U46619 with an estimated pKB (‐log KB) value of 6.2 by Schild regression analysis (slope 1.07).
4
Glibenclamide (30 μm) was apparently selective since it had no effect on the concentration‐contraction curves to endothelin‐1, noradrenaline or KCl.
5
We suggest that this additional property of glibenclamide should be considered in any smooth muscle study where active force is raised by either the exogenous application or endogenous generation of thromboxane A2.</description><subject>15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid</subject><subject>Animals</subject><subject>Coronary Vessels - drug effects</subject><subject>Coronary Vessels - metabolism</subject><subject>Dogs</subject><subject>Endothelins</subject><subject>Endothelium, Vascular - drug effects</subject><subject>Endothelium, Vascular - physiology</subject><subject>Female</subject><subject>Glyburide - pharmacology</subject><subject>In Vitro Techniques</subject><subject>Isometric Contraction</subject><subject>Male</subject><subject>Muscle Contraction - drug effects</subject><subject>Muscle, Smooth, Vascular - drug effects</subject><subject>Muscle, Smooth, Vascular - metabolism</subject><subject>Norepinephrine - pharmacology</subject><subject>Peptides - pharmacology</subject><subject>Potassium Chloride - pharmacology</subject><subject>Prostaglandin Endoperoxides, Synthetic - antagonists & inhibitors</subject><subject>Prostaglandin Endoperoxides, Synthetic - pharmacology</subject><subject>Receptors, Prostaglandin - antagonists & inhibitors</subject><subject>Receptors, Thromboxane</subject><subject>Thromboxane A2 - metabolism</subject><subject>Tolbutamide - pharmacology</subject><issn>0007-1188</issn><issn>1476-5381</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1990</creationdate><recordtype>article</recordtype><recordid>eNpVkcFu1DAQhi0EKkvhEZAsDtySemwnji-ItoIWqRIc4GzZyWTXqyQOjnfZvj3edrUCS6Ox5vP8Y_sn5AOwEvK62pYgVV1UooEStGZlclA1wMvDC7I6o5dkxRhTBUDTvCZvlmXLWIaquiAXHKRgWqzI5m7wDqd2sKPvkPqFWtqGccbkk98jtVOy6zD5JdHQ07TBHDGMLhzshPSa04gtzilE6ifahXVujmGy8ZHamDCnXN77FMNb8qq3w4LvTvmS_Pr65eftffHw_e7b7fVDMfOm4gWvheqAIci2q11bcyXavq86aBzjQqPshey0ck5VmrFKcVbbnmvOpRZOOSkuyadn3XnnRuxanFK0g5mjH_OtTLDe_E8mvzHrsDegQUnJs8DHk0AMv3e4JDP6pcVhyA8Ou8UorUEoIfLB9_9OOo84_W3mn5_5Hz_g4xkDM0cTzdYcnTJHp8zRRHMy0RzMzY_7p634CzXSkwk</recordid><startdate>199006</startdate><enddate>199006</enddate><creator>Cocks, Thomas M.</creator><creator>King, Susannah J.</creator><creator>Angus, James A.</creator><general>Blackwell Publishing Ltd</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope><scope>5PM</scope></search><sort><creationdate>199006</creationdate><title>Glibenclamide is a competitive antagonist of the thromboxane A2 receptor in dog coronary artery in vitro</title><author>Cocks, Thomas M. ; King, Susannah J. ; Angus, James A.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p2852-2637d10e14cd6bc6273cff5d18b0239e4f34d97bb7590057206af2922493b7b43</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1990</creationdate><topic>15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid</topic><topic>Animals</topic><topic>Coronary Vessels - drug effects</topic><topic>Coronary Vessels - metabolism</topic><topic>Dogs</topic><topic>Endothelins</topic><topic>Endothelium, Vascular - drug effects</topic><topic>Endothelium, Vascular - physiology</topic><topic>Female</topic><topic>Glyburide - pharmacology</topic><topic>In Vitro Techniques</topic><topic>Isometric Contraction</topic><topic>Male</topic><topic>Muscle Contraction - drug effects</topic><topic>Muscle, Smooth, Vascular - drug effects</topic><topic>Muscle, Smooth, Vascular - metabolism</topic><topic>Norepinephrine - pharmacology</topic><topic>Peptides - pharmacology</topic><topic>Potassium Chloride - pharmacology</topic><topic>Prostaglandin Endoperoxides, Synthetic - antagonists & inhibitors</topic><topic>Prostaglandin Endoperoxides, Synthetic - pharmacology</topic><topic>Receptors, Prostaglandin - antagonists & inhibitors</topic><topic>Receptors, Thromboxane</topic><topic>Thromboxane A2 - metabolism</topic><topic>Tolbutamide - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Cocks, Thomas M.</creatorcontrib><creatorcontrib>King, Susannah J.</creatorcontrib><creatorcontrib>Angus, James A.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>British journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Cocks, Thomas M.</au><au>King, Susannah J.</au><au>Angus, James A.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Glibenclamide is a competitive antagonist of the thromboxane A2 receptor in dog coronary artery in vitro</atitle><jtitle>British journal of pharmacology</jtitle><addtitle>Br J Pharmacol</addtitle><date>1990-06</date><risdate>1990</risdate><volume>100</volume><issue>2</issue><spage>375</spage><epage>378</epage><pages>375-378</pages><issn>0007-1188</issn><eissn>1476-5381</eissn><abstract>1
Glibenclamide, a sulphonylurea oral hypoglycaemic agent is a widely used antagonist of cromakalim‐activated K+ channels in smooth muscle.
2
In isolated ring segments of the large circumflex coronary artery from the dog, glibenclamide (1–30 μm) caused a concentration‐dependent reduction in both spontaneous isometric force and contractions induced by U46619, a thromboxane A2‐mimetic.
3
Glibenclamide behaved as a competitive antagonist of U46619 with an estimated pKB (‐log KB) value of 6.2 by Schild regression analysis (slope 1.07).
4
Glibenclamide (30 μm) was apparently selective since it had no effect on the concentration‐contraction curves to endothelin‐1, noradrenaline or KCl.
5
We suggest that this additional property of glibenclamide should be considered in any smooth muscle study where active force is raised by either the exogenous application or endogenous generation of thromboxane A2.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>2143093</pmid><doi>10.1111/j.1476-5381.1990.tb15812.x</doi><tpages>4</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | British journal of pharmacology, 1990-06, Vol.100 (2), p.375-378 |
| issn | 0007-1188 1476-5381 |
| language | eng |
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| source | PubMed Central |
| subjects | 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid Animals Coronary Vessels - drug effects Coronary Vessels - metabolism Dogs Endothelins Endothelium, Vascular - drug effects Endothelium, Vascular - physiology Female Glyburide - pharmacology In Vitro Techniques Isometric Contraction Male Muscle Contraction - drug effects Muscle, Smooth, Vascular - drug effects Muscle, Smooth, Vascular - metabolism Norepinephrine - pharmacology Peptides - pharmacology Potassium Chloride - pharmacology Prostaglandin Endoperoxides, Synthetic - antagonists & inhibitors Prostaglandin Endoperoxides, Synthetic - pharmacology Receptors, Prostaglandin - antagonists & inhibitors Receptors, Thromboxane Thromboxane A2 - metabolism Tolbutamide - pharmacology |
| title | Glibenclamide is a competitive antagonist of the thromboxane A2 receptor in dog coronary artery in vitro |
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