Endothelin ETA and ETB receptors mediate vascular smooth muscle contraction
1 We have investigated the receptors mediating endothelin‐induced contraction of rabbit isolated jugular vein (RJV) and rat isolated thoracic aorta (RTA). 2 Endothelin‐1 (ET‐1) and endothelin‐3 (ET‐3) contracted RJV preparations with similar potency (EC50 values ∼ 1 nm), whereas, ET‐1 (EC50:4.5 nm)...
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| Veröffentlicht in: | British journal of pharmacology 1992-11, Vol.107 (3), p.858-860 |
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| container_title | British journal of pharmacology |
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| creator | Sumner, Michael J. Cannon, Toby R. Mundin, Jason W. White, David G. Watts, Ian S. |
| description | 1
We have investigated the receptors mediating endothelin‐induced contraction of rabbit isolated jugular vein (RJV) and rat isolated thoracic aorta (RTA).
2
Endothelin‐1 (ET‐1) and endothelin‐3 (ET‐3) contracted RJV preparations with similar potency (EC50 values ∼ 1 nm), whereas, ET‐1 (EC50:4.5 nm) was ∼ 80 fold more potent than ET‐3 in contracting RTA. In addition, the ETB receptor‐selective agonist [Ala1,3,11,15]ET‐l contracted RJV (EC50:2.1 nm) but not RTA.
3
The ETA receptor antagonist, BQ123, competitively antagonized (pA2 6.93) the contraction of RTA produced by ET‐1, but had no effect (at 10 μm) on the contractile effects of either ET‐1, ET‐3 or [Ala1,3,11,15]ET‐1 in RJV.
4
These data suggest that both ETA and ETB receptors can mediate vascular smooth muscle contraction. |
| doi_str_mv | 10.1111/j.1476-5381.1992.tb14537.x |
| format | Article |
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We have investigated the receptors mediating endothelin‐induced contraction of rabbit isolated jugular vein (RJV) and rat isolated thoracic aorta (RTA).
2
Endothelin‐1 (ET‐1) and endothelin‐3 (ET‐3) contracted RJV preparations with similar potency (EC50 values ∼ 1 nm), whereas, ET‐1 (EC50:4.5 nm) was ∼ 80 fold more potent than ET‐3 in contracting RTA. In addition, the ETB receptor‐selective agonist [Ala1,3,11,15]ET‐l contracted RJV (EC50:2.1 nm) but not RTA.
3
The ETA receptor antagonist, BQ123, competitively antagonized (pA2 6.93) the contraction of RTA produced by ET‐1, but had no effect (at 10 μm) on the contractile effects of either ET‐1, ET‐3 or [Ala1,3,11,15]ET‐1 in RJV.
4
These data suggest that both ETA and ETB receptors can mediate vascular smooth muscle contraction.</description><identifier>ISSN: 0007-1188</identifier><identifier>EISSN: 1476-5381</identifier><identifier>DOI: 10.1111/j.1476-5381.1992.tb14537.x</identifier><identifier>PMID: 1472978</identifier><identifier>CODEN: BJPCBM</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>Animals ; Aorta, Thoracic - drug effects ; Biological and medical sciences ; Blood vessels and receptors ; BQ123 ; Endothelin ; Endothelins - pharmacology ; ETA antagonist ; Fundamental and applied biological sciences. Psychology ; In Vitro Techniques ; Isometric Contraction - drug effects ; Jugular Veins - drug effects ; Muscle Contraction - drug effects ; Muscle, Smooth - drug effects ; Muscle, Smooth, Vascular - drug effects ; Peptides, Cyclic - pharmacology ; Rabbits ; receptor subtypes ; Receptors, Endothelin - drug effects ; vascular smooth muscle contraction ; Vertebrates: cardiovascular system</subject><ispartof>British journal of pharmacology, 1992-11, Vol.107 (3), p.858-860</ispartof><rights>1992 British Pharmacological Society</rights><rights>1993 INIST-CNRS</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/PMC1907760/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1907760/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,723,776,780,881,27901,27902,53766,53768</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=4490469$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/1472978$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Sumner, Michael J.</creatorcontrib><creatorcontrib>Cannon, Toby R.</creatorcontrib><creatorcontrib>Mundin, Jason W.</creatorcontrib><creatorcontrib>White, David G.</creatorcontrib><creatorcontrib>Watts, Ian S.</creatorcontrib><title>Endothelin ETA and ETB receptors mediate vascular smooth muscle contraction</title><title>British journal of pharmacology</title><addtitle>Br J Pharmacol</addtitle><description>1
We have investigated the receptors mediating endothelin‐induced contraction of rabbit isolated jugular vein (RJV) and rat isolated thoracic aorta (RTA).
2
Endothelin‐1 (ET‐1) and endothelin‐3 (ET‐3) contracted RJV preparations with similar potency (EC50 values ∼ 1 nm), whereas, ET‐1 (EC50:4.5 nm) was ∼ 80 fold more potent than ET‐3 in contracting RTA. In addition, the ETB receptor‐selective agonist [Ala1,3,11,15]ET‐l contracted RJV (EC50:2.1 nm) but not RTA.
3
The ETA receptor antagonist, BQ123, competitively antagonized (pA2 6.93) the contraction of RTA produced by ET‐1, but had no effect (at 10 μm) on the contractile effects of either ET‐1, ET‐3 or [Ala1,3,11,15]ET‐1 in RJV.
4
These data suggest that both ETA and ETB receptors can mediate vascular smooth muscle contraction.</description><subject>Animals</subject><subject>Aorta, Thoracic - drug effects</subject><subject>Biological and medical sciences</subject><subject>Blood vessels and receptors</subject><subject>BQ123</subject><subject>Endothelin</subject><subject>Endothelins - pharmacology</subject><subject>ETA antagonist</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>In Vitro Techniques</subject><subject>Isometric Contraction - drug effects</subject><subject>Jugular Veins - drug effects</subject><subject>Muscle Contraction - drug effects</subject><subject>Muscle, Smooth - drug effects</subject><subject>Muscle, Smooth, Vascular - drug effects</subject><subject>Peptides, Cyclic - pharmacology</subject><subject>Rabbits</subject><subject>receptor subtypes</subject><subject>Receptors, Endothelin - drug effects</subject><subject>vascular smooth muscle contraction</subject><subject>Vertebrates: cardiovascular system</subject><issn>0007-1188</issn><issn>1476-5381</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1992</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpVUdtOxCAUJEaj6-UTTBpjfNsKCxR4Me5u1ks00Yf1mVBKlQ0ta2m9_L1Um1V5GZKZM2dyBoATBFMU3_kqRYRlY4o5SpEQk7TNEaGYpR9bYLShtsEIQsjGCHG-B_ZDWEEYSUZ3wW7EiWB8BO4WdeHbF-NsnSyW00TVRcRZ0hht1q1vQlKZwqrWJG8q6M6pJgmVjxNJ1QXtTKJ93TZKt9bXh2CnVC6YowEPwNPVYjm_Gd8_XN_Op_fjFeYxD-cYYcxZmXNFIMGIU4IKgmiMh0qYiyLnuChwoRiEOcsyxDNNBcmzXJhSIHwALn58110e02nTJ3By3dhKNZ_SKyv_M7V9kc_-TSIBGctgNDgbDBr_2pnQysoGbZxTtfFdkAxjSiEVUXj8d9NmxXC-yJ8OfDyOcmWjam3DRkaIgCTrbS5_ZO_Wmc9fFyj7OuWq98tk35ns65RDnfJDzh5vvr_4C8P2lFI</recordid><startdate>199211</startdate><enddate>199211</enddate><creator>Sumner, Michael J.</creator><creator>Cannon, Toby R.</creator><creator>Mundin, Jason W.</creator><creator>White, David G.</creator><creator>Watts, Ian S.</creator><general>Blackwell Publishing Ltd</general><general>Nature Publishing</general><scope>IQODW</scope><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>199211</creationdate><title>Endothelin ETA and ETB receptors mediate vascular smooth muscle contraction</title><author>Sumner, Michael J. ; Cannon, Toby R. ; Mundin, Jason W. ; White, David G. ; Watts, Ian S.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-j3807-88313387fb8a404318541d4150011f0b9db83dd3da700b766186c594b6b9ef913</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1992</creationdate><topic>Animals</topic><topic>Aorta, Thoracic - drug effects</topic><topic>Biological and medical sciences</topic><topic>Blood vessels and receptors</topic><topic>BQ123</topic><topic>Endothelin</topic><topic>Endothelins - pharmacology</topic><topic>ETA antagonist</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>In Vitro Techniques</topic><topic>Isometric Contraction - drug effects</topic><topic>Jugular Veins - drug effects</topic><topic>Muscle Contraction - drug effects</topic><topic>Muscle, Smooth - drug effects</topic><topic>Muscle, Smooth, Vascular - drug effects</topic><topic>Peptides, Cyclic - pharmacology</topic><topic>Rabbits</topic><topic>receptor subtypes</topic><topic>Receptors, Endothelin - drug effects</topic><topic>vascular smooth muscle contraction</topic><topic>Vertebrates: cardiovascular system</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Sumner, Michael J.</creatorcontrib><creatorcontrib>Cannon, Toby R.</creatorcontrib><creatorcontrib>Mundin, Jason W.</creatorcontrib><creatorcontrib>White, David G.</creatorcontrib><creatorcontrib>Watts, Ian S.</creatorcontrib><collection>Pascal-Francis</collection><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>Sumner, Michael J.</au><au>Cannon, Toby R.</au><au>Mundin, Jason W.</au><au>White, David G.</au><au>Watts, Ian S.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Endothelin ETA and ETB receptors mediate vascular smooth muscle contraction</atitle><jtitle>British journal of pharmacology</jtitle><addtitle>Br J Pharmacol</addtitle><date>1992-11</date><risdate>1992</risdate><volume>107</volume><issue>3</issue><spage>858</spage><epage>860</epage><pages>858-860</pages><issn>0007-1188</issn><eissn>1476-5381</eissn><coden>BJPCBM</coden><abstract>1
We have investigated the receptors mediating endothelin‐induced contraction of rabbit isolated jugular vein (RJV) and rat isolated thoracic aorta (RTA).
2
Endothelin‐1 (ET‐1) and endothelin‐3 (ET‐3) contracted RJV preparations with similar potency (EC50 values ∼ 1 nm), whereas, ET‐1 (EC50:4.5 nm) was ∼ 80 fold more potent than ET‐3 in contracting RTA. In addition, the ETB receptor‐selective agonist [Ala1,3,11,15]ET‐l contracted RJV (EC50:2.1 nm) but not RTA.
3
The ETA receptor antagonist, BQ123, competitively antagonized (pA2 6.93) the contraction of RTA produced by ET‐1, but had no effect (at 10 μm) on the contractile effects of either ET‐1, ET‐3 or [Ala1,3,11,15]ET‐1 in RJV.
4
These data suggest that both ETA and ETB receptors can mediate vascular smooth muscle contraction.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>1472978</pmid><doi>10.1111/j.1476-5381.1992.tb14537.x</doi><tpages>3</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Animals Aorta, Thoracic - drug effects Biological and medical sciences Blood vessels and receptors BQ123 Endothelin Endothelins - pharmacology ETA antagonist Fundamental and applied biological sciences. Psychology In Vitro Techniques Isometric Contraction - drug effects Jugular Veins - drug effects Muscle Contraction - drug effects Muscle, Smooth - drug effects Muscle, Smooth, Vascular - drug effects Peptides, Cyclic - pharmacology Rabbits receptor subtypes Receptors, Endothelin - drug effects vascular smooth muscle contraction Vertebrates: cardiovascular system |
| title | Endothelin ETA and ETB receptors mediate vascular smooth muscle contraction |
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