Imidazoline Receptors in the Heart: Characterization, Distribution, and Regulation
Imidazoline receptors were identified in cardiac tissues of various species. Imidazoline receptors were immunolocalized in the rat heart. Membrane binding and autoradiography on frozen heart sections using 0.5 n M para-iodoclonidine (I-PIC) revealed that binding was equally and concentration-depende...
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Veröffentlicht in: | Journal of cardiovascular pharmacology 2002-06, Vol.39 (6), p.875-883 |
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description | Imidazoline receptors were identified in cardiac tissues of various species. Imidazoline receptors were immunolocalized in the rat heart. Membrane binding and autoradiography on frozen heart sections using 0.5 n M para-iodoclonidine (I-PIC) revealed that binding was equally and concentration-dependently inhibited by epinephrine and imidazole-4-acetic acid (IAA), implying I-PIC binding to cardiac α2-adrenergic and I1-receptors, respectively. After irreversible blockade of α2-adrenergic receptors, binding was inhibited by the selective I1-agonist, moxonidine, and the I1-antagonist, efaroxan, in a concentration-dependent (10 to 10M) manner. Calculation of kinetic parameters revealed that in canine left and right atria, I1-receptor Bmax was 13.4 ± 1.7 and 20.1 ± 3.0 fmol/mg protein, respectively. Compared to age-matched normotensive Wistar Kyoto rats, I1-receptors were increased in 12-week-old hypertensive rat (SHR) right (22.6 ± 0.3 to 43.7 ± 4.4 fmol/unit area, p < 0.01) and left atria (13.3 ± 0.6 to 30.2 ± 4.1 fmol/unit area, p < 0.01). Also, compared to corresponding normal controls, Bmax was increased in hearts of hamsters with advanced cardiomyopathy (13.9 ± 0.4 to. 26.0 ± 2.3 fmol/unit area, p < 0.01) and in human ventricles with heart failure (12.6 ± 1.3 to 35.5 ± 2.9 fmol/mg protein, p < 0.003). These studies demonstrate that the heart possesses imidazoline I1-receptors that are up-regulated in the presence of hypertension or heart failure, which would suggest their involvement in cardiovascular regulation. |
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Imidazoline receptors were immunolocalized in the rat heart. Membrane binding and autoradiography on frozen heart sections using 0.5 n M para-iodoclonidine (I-PIC) revealed that binding was equally and concentration-dependently inhibited by epinephrine and imidazole-4-acetic acid (IAA), implying I-PIC binding to cardiac α2-adrenergic and I1-receptors, respectively. After irreversible blockade of α2-adrenergic receptors, binding was inhibited by the selective I1-agonist, moxonidine, and the I1-antagonist, efaroxan, in a concentration-dependent (10 to 10M) manner. Calculation of kinetic parameters revealed that in canine left and right atria, I1-receptor Bmax was 13.4 ± 1.7 and 20.1 ± 3.0 fmol/mg protein, respectively. Compared to age-matched normotensive Wistar Kyoto rats, I1-receptors were increased in 12-week-old hypertensive rat (SHR) right (22.6 ± 0.3 to 43.7 ± 4.4 fmol/unit area, p < 0.01) and left atria (13.3 ± 0.6 to 30.2 ± 4.1 fmol/unit area, p < 0.01). Also, compared to corresponding normal controls, Bmax was increased in hearts of hamsters with advanced cardiomyopathy (13.9 ± 0.4 to. 26.0 ± 2.3 fmol/unit area, p < 0.01) and in human ventricles with heart failure (12.6 ± 1.3 to 35.5 ± 2.9 fmol/mg protein, p < 0.003). These studies demonstrate that the heart possesses imidazoline I1-receptors that are up-regulated in the presence of hypertension or heart failure, which would suggest their involvement in cardiovascular regulation.</description><identifier>ISSN: 0160-2446</identifier><identifier>EISSN: 1533-4023</identifier><identifier>DOI: 10.1097/00005344-200206000-00013</identifier><identifier>PMID: 12021582</identifier><identifier>CODEN: JCPCDT</identifier><language>eng</language><publisher>Philadelphia, PA: Lippincott Williams & Wilkins, Inc</publisher><subject>Animals ; Biological and medical sciences ; Cardiomyopathies - metabolism ; Cell receptors ; Cell structures and functions ; Cricetinae ; Dogs ; Fundamental and applied biological sciences. Psychology ; Heart ; Humans ; Imidazoline Receptors ; Mesocricetus ; Miscellaneous ; Molecular and cellular biology ; Myocardium - chemistry ; Myocardium - metabolism ; Organ Specificity ; Rats ; Rats, Inbred SHR ; Rats, Inbred WKY ; Receptors, Drug - analysis ; Receptors, Drug - metabolism ; Sheep ; Vertebrates: cardiovascular system</subject><ispartof>Journal of cardiovascular pharmacology, 2002-06, Vol.39 (6), p.875-883</ispartof><rights>2002 Lippincott Williams & Wilkins, Inc.</rights><rights>2002 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c5023-cef5606f42ee49a69d8d0366f5999faa953076086aff163ed63fe2cf51daacea3</citedby><cites>FETCH-LOGICAL-c5023-cef5606f42ee49a69d8d0366f5999faa953076086aff163ed63fe2cf51daacea3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf><![CDATA[$$Uhttp://ovidsp.ovid.com/ovidweb.cgi?T=JS&CSC=Y&NEWS=N&PAGE=fulltext&PDF=y&D=ovft&AN=00005344-200206000-00013$$EPDF$$P50$$Gwolterskluwer$$H]]></linktopdf><linktohtml>$$Uhttp://ovidsp.ovid.com/ovidweb.cgi?T=JS&NEWS=n&CSC=Y&PAGE=fulltext&D=ovft&AN=00005344-200206000-00013$$EHTML$$P50$$Gwolterskluwer$$H</linktohtml><link.rule.ids>314,780,784,4608,27923,27924,64565,65332</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=13685238$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/12021582$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>El-Ayoubi, Rouwayda</creatorcontrib><creatorcontrib>Gutkowska, Jolanta</creatorcontrib><creatorcontrib>Regunathan, Soundar</creatorcontrib><creatorcontrib>Mukaddam-Daher, Suhayla</creatorcontrib><title>Imidazoline Receptors in the Heart: Characterization, Distribution, and Regulation</title><title>Journal of cardiovascular pharmacology</title><addtitle>J Cardiovasc Pharmacol</addtitle><description>Imidazoline receptors were identified in cardiac tissues of various species. Imidazoline receptors were immunolocalized in the rat heart. Membrane binding and autoradiography on frozen heart sections using 0.5 n M para-iodoclonidine (I-PIC) revealed that binding was equally and concentration-dependently inhibited by epinephrine and imidazole-4-acetic acid (IAA), implying I-PIC binding to cardiac α2-adrenergic and I1-receptors, respectively. After irreversible blockade of α2-adrenergic receptors, binding was inhibited by the selective I1-agonist, moxonidine, and the I1-antagonist, efaroxan, in a concentration-dependent (10 to 10M) manner. Calculation of kinetic parameters revealed that in canine left and right atria, I1-receptor Bmax was 13.4 ± 1.7 and 20.1 ± 3.0 fmol/mg protein, respectively. Compared to age-matched normotensive Wistar Kyoto rats, I1-receptors were increased in 12-week-old hypertensive rat (SHR) right (22.6 ± 0.3 to 43.7 ± 4.4 fmol/unit area, p < 0.01) and left atria (13.3 ± 0.6 to 30.2 ± 4.1 fmol/unit area, p < 0.01). Also, compared to corresponding normal controls, Bmax was increased in hearts of hamsters with advanced cardiomyopathy (13.9 ± 0.4 to. 26.0 ± 2.3 fmol/unit area, p < 0.01) and in human ventricles with heart failure (12.6 ± 1.3 to 35.5 ± 2.9 fmol/mg protein, p < 0.003). These studies demonstrate that the heart possesses imidazoline I1-receptors that are up-regulated in the presence of hypertension or heart failure, which would suggest their involvement in cardiovascular regulation.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Cardiomyopathies - metabolism</subject><subject>Cell receptors</subject><subject>Cell structures and functions</subject><subject>Cricetinae</subject><subject>Dogs</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Heart</subject><subject>Humans</subject><subject>Imidazoline Receptors</subject><subject>Mesocricetus</subject><subject>Miscellaneous</subject><subject>Molecular and cellular biology</subject><subject>Myocardium - chemistry</subject><subject>Myocardium - metabolism</subject><subject>Organ Specificity</subject><subject>Rats</subject><subject>Rats, Inbred SHR</subject><subject>Rats, Inbred WKY</subject><subject>Receptors, Drug - analysis</subject><subject>Receptors, Drug - metabolism</subject><subject>Sheep</subject><subject>Vertebrates: cardiovascular system</subject><issn>0160-2446</issn><issn>1533-4023</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2002</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp1kU1rGzEQhkVoSJyPvxD20p6yjb53t7fiNHXAEDDtWYy1o1itvOtKu5jm10e13fgUgRDDPK80PCKkYPQzo011R_NSQsqSU8qpzlWZNxMnZMKUEKWkXHwgE8o0LbmU-pxcpPQrE1JV-oycM045UzWfkMXj2rfw0gffYbFAi5uhj6nwXTGssJghxOFLMV1BBDtg9C8w-L67Le59GqJfjvsKujZnn8ew616RUwch4fXhvCQ_H779mM7K-dP3x-nXeWlVHq-06JSm2kmOKBvQTVu3VGjtVNM0DqBRglaa1hqcY1pgq4VDbp1iLYBFEJfk0_7eTez_jJgGs_bJYgjQYT8mU7FKyrpiGaz3oI19ShGd2US_hvjXMGr--TT_fZo3n2bnM0dvDm-MyzW2x-BBYAY-HgBIFoKL0FmfjpzQteKizpzcc9s-ZJHpdxi3GM0KIQwr895_ild2fI0N</recordid><startdate>200206</startdate><enddate>200206</enddate><creator>El-Ayoubi, Rouwayda</creator><creator>Gutkowska, Jolanta</creator><creator>Regunathan, Soundar</creator><creator>Mukaddam-Daher, Suhayla</creator><general>Lippincott Williams & Wilkins, Inc</general><general>Lippincott</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>200206</creationdate><title>Imidazoline Receptors in the Heart: Characterization, Distribution, and Regulation</title><author>El-Ayoubi, Rouwayda ; Gutkowska, Jolanta ; Regunathan, Soundar ; Mukaddam-Daher, Suhayla</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c5023-cef5606f42ee49a69d8d0366f5999faa953076086aff163ed63fe2cf51daacea3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2002</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Cardiomyopathies - metabolism</topic><topic>Cell receptors</topic><topic>Cell structures and functions</topic><topic>Cricetinae</topic><topic>Dogs</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Heart</topic><topic>Humans</topic><topic>Imidazoline Receptors</topic><topic>Mesocricetus</topic><topic>Miscellaneous</topic><topic>Molecular and cellular biology</topic><topic>Myocardium - chemistry</topic><topic>Myocardium - metabolism</topic><topic>Organ Specificity</topic><topic>Rats</topic><topic>Rats, Inbred SHR</topic><topic>Rats, Inbred WKY</topic><topic>Receptors, Drug - analysis</topic><topic>Receptors, Drug - metabolism</topic><topic>Sheep</topic><topic>Vertebrates: cardiovascular system</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>El-Ayoubi, Rouwayda</creatorcontrib><creatorcontrib>Gutkowska, Jolanta</creatorcontrib><creatorcontrib>Regunathan, Soundar</creatorcontrib><creatorcontrib>Mukaddam-Daher, Suhayla</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>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of cardiovascular pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>El-Ayoubi, Rouwayda</au><au>Gutkowska, Jolanta</au><au>Regunathan, Soundar</au><au>Mukaddam-Daher, Suhayla</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Imidazoline Receptors in the Heart: Characterization, Distribution, and Regulation</atitle><jtitle>Journal of cardiovascular pharmacology</jtitle><addtitle>J Cardiovasc Pharmacol</addtitle><date>2002-06</date><risdate>2002</risdate><volume>39</volume><issue>6</issue><spage>875</spage><epage>883</epage><pages>875-883</pages><issn>0160-2446</issn><eissn>1533-4023</eissn><coden>JCPCDT</coden><abstract>Imidazoline receptors were identified in cardiac tissues of various species. Imidazoline receptors were immunolocalized in the rat heart. Membrane binding and autoradiography on frozen heart sections using 0.5 n M para-iodoclonidine (I-PIC) revealed that binding was equally and concentration-dependently inhibited by epinephrine and imidazole-4-acetic acid (IAA), implying I-PIC binding to cardiac α2-adrenergic and I1-receptors, respectively. After irreversible blockade of α2-adrenergic receptors, binding was inhibited by the selective I1-agonist, moxonidine, and the I1-antagonist, efaroxan, in a concentration-dependent (10 to 10M) manner. Calculation of kinetic parameters revealed that in canine left and right atria, I1-receptor Bmax was 13.4 ± 1.7 and 20.1 ± 3.0 fmol/mg protein, respectively. Compared to age-matched normotensive Wistar Kyoto rats, I1-receptors were increased in 12-week-old hypertensive rat (SHR) right (22.6 ± 0.3 to 43.7 ± 4.4 fmol/unit area, p < 0.01) and left atria (13.3 ± 0.6 to 30.2 ± 4.1 fmol/unit area, p < 0.01). Also, compared to corresponding normal controls, Bmax was increased in hearts of hamsters with advanced cardiomyopathy (13.9 ± 0.4 to. 26.0 ± 2.3 fmol/unit area, p < 0.01) and in human ventricles with heart failure (12.6 ± 1.3 to 35.5 ± 2.9 fmol/mg protein, p < 0.003). These studies demonstrate that the heart possesses imidazoline I1-receptors that are up-regulated in the presence of hypertension or heart failure, which would suggest their involvement in cardiovascular regulation.</abstract><cop>Philadelphia, PA</cop><cop>Hagerstown, MD</cop><pub>Lippincott Williams & Wilkins, Inc</pub><pmid>12021582</pmid><doi>10.1097/00005344-200206000-00013</doi><tpages>9</tpages><oa>free_for_read</oa></addata></record> |
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subjects | Animals Biological and medical sciences Cardiomyopathies - metabolism Cell receptors Cell structures and functions Cricetinae Dogs Fundamental and applied biological sciences. Psychology Heart Humans Imidazoline Receptors Mesocricetus Miscellaneous Molecular and cellular biology Myocardium - chemistry Myocardium - metabolism Organ Specificity Rats Rats, Inbred SHR Rats, Inbred WKY Receptors, Drug - analysis Receptors, Drug - metabolism Sheep Vertebrates: cardiovascular system |
title | Imidazoline Receptors in the Heart: Characterization, Distribution, and Regulation |
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