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
Hauptverfasser: El-Ayoubi, Rouwayda, Gutkowska, Jolanta, Regunathan, Soundar, Mukaddam-Daher, Suhayla
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creator El-Ayoubi, Rouwayda
Gutkowska, Jolanta
Regunathan, Soundar
Mukaddam-Daher, Suhayla
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.
doi_str_mv 10.1097/00005344-200206000-00013
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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 &lt; 0.01) and in human ventricles with heart failure (12.6 ± 1.3 to 35.5 ± 2.9 fmol/mg protein, p &lt; 0.003). 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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 &lt; 0.01) and left atria (13.3 ± 0.6 to 30.2 ± 4.1 fmol/unit area, p &lt; 0.01). 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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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