Characteristics of Adrenoceptors and [3H]Nitrendipine Receptors of Porcine Vascular Smooth Muscle: Differences Between Coronary Artery and Aorta
Characteristics of the bindings of [H](−)dihydroalprenolol, [I](−) iodocyanopindolol, [H]prazosin, [H]yohimbine, and [H]nitrendipine to porcine coronary membranes were investigated and the results compared with studies of porcine aortic membranes. In the equilibrium binding study carried out in sarc...
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| Veröffentlicht in: | Circ. Res.; (United States) 1987-06, Vol.60 (6), p.837-844 |
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| creator | Nishimura, Junji Kanaide, Hideo Nakamura, Motoomi |
| description | Characteristics of the bindings of [H](−)dihydroalprenolol, [I](−) iodocyanopindolol, [H]prazosin, [H]yohimbine, and [H]nitrendipine to porcine coronary membranes were investigated and the results compared with studies of porcine aortic membranes. In the equilibrium binding study carried out in sarcolemma-enriched fractions, there were no major differences in the Kd values of these radioligands between coronary artery and aorta. However, the densities of/β-, α1, and α2-adrenocetors and [H]nitrendipine receptors of coronary artery were 258, 12, 12, and 561 fmol/mg protein, respectively, while those of aorta were 37,525,1,000, and 215 fmol/mg protein. β-Adrenergic agonists competed with [H](−)dihydroalprenolol binding sites in coronary artery, the order of potency being (−)isoproterenol > (−)norepinephrine > (−)epinephrine > (+)isoproterenol. In case of aorta, the order was (−)isoproterenol > (−)epinephrine > (−)norepinephrine. The competition by (±)bisoprolol β,-selective antagonist) and ICI 118,5510β2-selective antagonist) for [I](–)iodocyanopindolol binding sites in coronary artery resulted in nonlinear Hofstee plots (β1β2 = 90%10%). In case of aorta, linear Hofstee plots were obtained. From these results, we conclude that (1) coronary β- receptors in pigs are predominately of β1-type, while those of aorta are of %bT2-type; (2) regarding the relative population of adrenoceptors, coronary artery is β-dominant (β/α = 11), while aorta is α- dominant (β/α = 0.02); (3) compared withα-adrenoceptors, coronary artery has a greater number of [H]nitrendipine binding sites (nitrendipine/α-adrenoceptor = 23) than aorta (nitrendipine/α-adrenoceptor = 0.14). |
| doi_str_mv | 10.1161/01.RES.60.6.837 |
| format | Article |
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In the equilibrium binding study carried out in sarcolemma-enriched fractions, there were no major differences in the Kd values of these radioligands between coronary artery and aorta. However, the densities of/β-, α1, and α2-adrenocetors and [H]nitrendipine receptors of coronary artery were 258, 12, 12, and 561 fmol/mg protein, respectively, while those of aorta were 37,525,1,000, and 215 fmol/mg protein. β-Adrenergic agonists competed with [H](−)dihydroalprenolol binding sites in coronary artery, the order of potency being (−)isoproterenol > (−)norepinephrine > (−)epinephrine > (+)isoproterenol. In case of aorta, the order was (−)isoproterenol > (−)epinephrine > (−)norepinephrine. The competition by (±)bisoprolol β,-selective antagonist) and ICI 118,5510β2-selective antagonist) for [I](–)iodocyanopindolol binding sites in coronary artery resulted in nonlinear Hofstee plots (β1β2 = 90%10%). In case of aorta, linear Hofstee plots were obtained. From these results, we conclude that (1) coronary β- receptors in pigs are predominately of β1-type, while those of aorta are of %bT2-type; (2) regarding the relative population of adrenoceptors, coronary artery is β-dominant (β/α = 11), while aorta is α- dominant (β/α = 0.02); (3) compared withα-adrenoceptors, coronary artery has a greater number of [H]nitrendipine binding sites (nitrendipine/α-adrenoceptor = 23) than aorta (nitrendipine/α-adrenoceptor = 0.14).</description><identifier>ISSN: 0009-7330</identifier><identifier>EISSN: 1524-4571</identifier><identifier>DOI: 10.1161/01.RES.60.6.837</identifier><identifier>PMID: 3036396</identifier><identifier>CODEN: CIRUAL</identifier><language>eng</language><publisher>Hagerstown, MD: American Heart Association, Inc</publisher><subject>550201 - Biochemistry- Tracer Techniques ; ANIMALS ; AORTA ; Aorta - metabolism ; ARTERIES ; AUTONOMIC NERVOUS SYSTEM AGENTS ; BASIC BIOLOGICAL SCIENCES ; Binding Sites ; BIOCHEMICAL REACTION KINETICS ; Biological and medical sciences ; BLOOD VESSELS ; Blood vessels and receptors ; BODY ; Calcium Channels ; CARDIOVASCULAR SYSTEM ; CELL CONSTITUENTS ; CELL MEMBRANES ; COMPARATIVE EVALUATIONS ; CORONARIES ; Coronary Vessels - metabolism ; Dihydroalprenolol - metabolism ; DOMESTIC ANIMALS ; DRUGS ; Fundamental and applied biological sciences. Psychology ; Iodocyanopindolol ; ISOTOPE APPLICATIONS ; KINETICS ; LABELLED COMPOUNDS ; LIGANDS ; MAMMALS ; MEMBRANE PROTEINS ; MEMBRANES ; Muscle, Smooth, Vascular - metabolism ; MUSCLES ; Nitrendipine - metabolism ; ORGANIC COMPOUNDS ; ORGANS ; Pindolol - analogs & derivatives ; Pindolol - metabolism ; Prazosin - metabolism ; PROTEINS ; REACTION KINETICS ; RECEPTORS ; Receptors, Adrenergic - metabolism ; Receptors, Nicotinic - metabolism ; SWINE ; SYMPATHOMIMETICS ; TRACER TECHNIQUES ; Tritium ; TRITIUM COMPOUNDS ; VERTEBRATES ; Vertebrates: cardiovascular system ; Yohimbine - metabolism</subject><ispartof>Circ. Res.; (United States), 1987-06, Vol.60 (6), p.837-844</ispartof><rights>1987 American Heart Association, Inc.</rights><rights>1988 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4706-d1c919da3d1bfb09a2b9a71b84adf13182b39b9c0651bca90f392a8700d7b58a3</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,885,3687,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=7461339$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/3036396$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink><backlink>$$Uhttps://www.osti.gov/biblio/6075493$$D View this record in Osti.gov$$Hfree_for_read</backlink></links><search><creatorcontrib>Nishimura, Junji</creatorcontrib><creatorcontrib>Kanaide, Hideo</creatorcontrib><creatorcontrib>Nakamura, Motoomi</creatorcontrib><creatorcontrib>Kyushu Univ., Japan</creatorcontrib><title>Characteristics of Adrenoceptors and [3H]Nitrendipine Receptors of Porcine Vascular Smooth Muscle: Differences Between Coronary Artery and Aorta</title><title>Circ. Res.; (United States)</title><addtitle>Circ Res</addtitle><description>Characteristics of the bindings of [H](−)dihydroalprenolol, [I](−) iodocyanopindolol, [H]prazosin, [H]yohimbine, and [H]nitrendipine to porcine coronary membranes were investigated and the results compared with studies of porcine aortic membranes. In the equilibrium binding study carried out in sarcolemma-enriched fractions, there were no major differences in the Kd values of these radioligands between coronary artery and aorta. However, the densities of/β-, α1, and α2-adrenocetors and [H]nitrendipine receptors of coronary artery were 258, 12, 12, and 561 fmol/mg protein, respectively, while those of aorta were 37,525,1,000, and 215 fmol/mg protein. β-Adrenergic agonists competed with [H](−)dihydroalprenolol binding sites in coronary artery, the order of potency being (−)isoproterenol > (−)norepinephrine > (−)epinephrine > (+)isoproterenol. In case of aorta, the order was (−)isoproterenol > (−)epinephrine > (−)norepinephrine. The competition by (±)bisoprolol β,-selective antagonist) and ICI 118,5510β2-selective antagonist) for [I](–)iodocyanopindolol binding sites in coronary artery resulted in nonlinear Hofstee plots (β1β2 = 90%10%). In case of aorta, linear Hofstee plots were obtained. From these results, we conclude that (1) coronary β- receptors in pigs are predominately of β1-type, while those of aorta are of %bT2-type; (2) regarding the relative population of adrenoceptors, coronary artery is β-dominant (β/α = 11), while aorta is α- dominant (β/α = 0.02); (3) compared withα-adrenoceptors, coronary artery has a greater number of [H]nitrendipine binding sites (nitrendipine/α-adrenoceptor = 23) than aorta (nitrendipine/α-adrenoceptor = 0.14).</description><subject>550201 - Biochemistry- Tracer Techniques</subject><subject>ANIMALS</subject><subject>AORTA</subject><subject>Aorta - metabolism</subject><subject>ARTERIES</subject><subject>AUTONOMIC NERVOUS SYSTEM AGENTS</subject><subject>BASIC BIOLOGICAL SCIENCES</subject><subject>Binding Sites</subject><subject>BIOCHEMICAL REACTION KINETICS</subject><subject>Biological and medical sciences</subject><subject>BLOOD VESSELS</subject><subject>Blood vessels and receptors</subject><subject>BODY</subject><subject>Calcium Channels</subject><subject>CARDIOVASCULAR SYSTEM</subject><subject>CELL CONSTITUENTS</subject><subject>CELL MEMBRANES</subject><subject>COMPARATIVE EVALUATIONS</subject><subject>CORONARIES</subject><subject>Coronary Vessels - metabolism</subject><subject>Dihydroalprenolol - metabolism</subject><subject>DOMESTIC ANIMALS</subject><subject>DRUGS</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Iodocyanopindolol</subject><subject>ISOTOPE APPLICATIONS</subject><subject>KINETICS</subject><subject>LABELLED COMPOUNDS</subject><subject>LIGANDS</subject><subject>MAMMALS</subject><subject>MEMBRANE PROTEINS</subject><subject>MEMBRANES</subject><subject>Muscle, Smooth, Vascular - metabolism</subject><subject>MUSCLES</subject><subject>Nitrendipine - metabolism</subject><subject>ORGANIC COMPOUNDS</subject><subject>ORGANS</subject><subject>Pindolol - analogs & derivatives</subject><subject>Pindolol - metabolism</subject><subject>Prazosin - metabolism</subject><subject>PROTEINS</subject><subject>REACTION KINETICS</subject><subject>RECEPTORS</subject><subject>Receptors, Adrenergic - metabolism</subject><subject>Receptors, Nicotinic - metabolism</subject><subject>SWINE</subject><subject>SYMPATHOMIMETICS</subject><subject>TRACER TECHNIQUES</subject><subject>Tritium</subject><subject>TRITIUM COMPOUNDS</subject><subject>VERTEBRATES</subject><subject>Vertebrates: cardiovascular system</subject><subject>Yohimbine - metabolism</subject><issn>0009-7330</issn><issn>1524-4571</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1987</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo9kU9v1DAQxS0EKtvCmROShVBvScdxYsfclqVQpPJHLXBByHKcidaQjRfb0arfgo-Ml116svzmN2808wh5xqBkTLALYOXN5W0poBRly-UDsmBNVRd1I9lDsgAAVUjO4TE5jfEnAKt5pU7ICQcuuBIL8me1NsHYhMHF5GykfqDLPuDkLW6TD5Gaqaff-dWPjy5luXdbNyG9wf_lzH_2we7FbybaeTSB3m68T2v6YY52xFf0jRsGzL0WI32NaYc40ZUPfjLhji5Dnn33b8rSh2SekEeDGSM-Pb5n5Ovbyy-rq-L607v3q-V1YWsJouiZVUz1hvesGzpQpuqUkaxra9MPjLO26rjqlAXRsM4aBQNXlWklQC-7pjX8jLw4-Pq8t47WJbRr66cJbdICZFMrnqHzA7QN_veMMemNixbH0Uzo56ilbFqu2iaDFwfQBh9jwEFvg9vk_TQDvQ9KA9M5qOyshc5B5Y7nR-u522B_zx-TyfWXx3q-qhmHYCbr4j0ma8E4VxmrD9jOj_mQ8dc47zDoNZoxrXXOHziwqmAqry7yr9hLgv8F8qasZg</recordid><startdate>198706</startdate><enddate>198706</enddate><creator>Nishimura, Junji</creator><creator>Kanaide, Hideo</creator><creator>Nakamura, Motoomi</creator><general>American Heart Association, 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><scope>OTOTI</scope></search><sort><creationdate>198706</creationdate><title>Characteristics of Adrenoceptors and [3H]Nitrendipine Receptors of Porcine Vascular Smooth Muscle: Differences Between Coronary Artery and Aorta</title><author>Nishimura, Junji ; Kanaide, Hideo ; Nakamura, Motoomi</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4706-d1c919da3d1bfb09a2b9a71b84adf13182b39b9c0651bca90f392a8700d7b58a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1987</creationdate><topic>550201 - Biochemistry- Tracer Techniques</topic><topic>ANIMALS</topic><topic>AORTA</topic><topic>Aorta - metabolism</topic><topic>ARTERIES</topic><topic>AUTONOMIC NERVOUS SYSTEM AGENTS</topic><topic>BASIC BIOLOGICAL SCIENCES</topic><topic>Binding Sites</topic><topic>BIOCHEMICAL REACTION KINETICS</topic><topic>Biological and medical sciences</topic><topic>BLOOD VESSELS</topic><topic>Blood vessels and receptors</topic><topic>BODY</topic><topic>Calcium Channels</topic><topic>CARDIOVASCULAR SYSTEM</topic><topic>CELL CONSTITUENTS</topic><topic>CELL MEMBRANES</topic><topic>COMPARATIVE EVALUATIONS</topic><topic>CORONARIES</topic><topic>Coronary Vessels - metabolism</topic><topic>Dihydroalprenolol - metabolism</topic><topic>DOMESTIC ANIMALS</topic><topic>DRUGS</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Iodocyanopindolol</topic><topic>ISOTOPE APPLICATIONS</topic><topic>KINETICS</topic><topic>LABELLED COMPOUNDS</topic><topic>LIGANDS</topic><topic>MAMMALS</topic><topic>MEMBRANE PROTEINS</topic><topic>MEMBRANES</topic><topic>Muscle, Smooth, Vascular - metabolism</topic><topic>MUSCLES</topic><topic>Nitrendipine - metabolism</topic><topic>ORGANIC COMPOUNDS</topic><topic>ORGANS</topic><topic>Pindolol - analogs & derivatives</topic><topic>Pindolol - metabolism</topic><topic>Prazosin - metabolism</topic><topic>PROTEINS</topic><topic>REACTION KINETICS</topic><topic>RECEPTORS</topic><topic>Receptors, Adrenergic - metabolism</topic><topic>Receptors, Nicotinic - metabolism</topic><topic>SWINE</topic><topic>SYMPATHOMIMETICS</topic><topic>TRACER TECHNIQUES</topic><topic>Tritium</topic><topic>TRITIUM COMPOUNDS</topic><topic>VERTEBRATES</topic><topic>Vertebrates: cardiovascular system</topic><topic>Yohimbine - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Nishimura, Junji</creatorcontrib><creatorcontrib>Kanaide, Hideo</creatorcontrib><creatorcontrib>Nakamura, Motoomi</creatorcontrib><creatorcontrib>Kyushu Univ., Japan</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><collection>OSTI.GOV</collection><jtitle>Circ. Res.; (United States)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Nishimura, Junji</au><au>Kanaide, Hideo</au><au>Nakamura, Motoomi</au><aucorp>Kyushu Univ., Japan</aucorp><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Characteristics of Adrenoceptors and [3H]Nitrendipine Receptors of Porcine Vascular Smooth Muscle: Differences Between Coronary Artery and Aorta</atitle><jtitle>Circ. Res.; (United States)</jtitle><addtitle>Circ Res</addtitle><date>1987-06</date><risdate>1987</risdate><volume>60</volume><issue>6</issue><spage>837</spage><epage>844</epage><pages>837-844</pages><issn>0009-7330</issn><eissn>1524-4571</eissn><coden>CIRUAL</coden><abstract>Characteristics of the bindings of [H](−)dihydroalprenolol, [I](−) iodocyanopindolol, [H]prazosin, [H]yohimbine, and [H]nitrendipine to porcine coronary membranes were investigated and the results compared with studies of porcine aortic membranes. In the equilibrium binding study carried out in sarcolemma-enriched fractions, there were no major differences in the Kd values of these radioligands between coronary artery and aorta. However, the densities of/β-, α1, and α2-adrenocetors and [H]nitrendipine receptors of coronary artery were 258, 12, 12, and 561 fmol/mg protein, respectively, while those of aorta were 37,525,1,000, and 215 fmol/mg protein. β-Adrenergic agonists competed with [H](−)dihydroalprenolol binding sites in coronary artery, the order of potency being (−)isoproterenol > (−)norepinephrine > (−)epinephrine > (+)isoproterenol. In case of aorta, the order was (−)isoproterenol > (−)epinephrine > (−)norepinephrine. The competition by (±)bisoprolol β,-selective antagonist) and ICI 118,5510β2-selective antagonist) for [I](–)iodocyanopindolol binding sites in coronary artery resulted in nonlinear Hofstee plots (β1β2 = 90%10%). In case of aorta, linear Hofstee plots were obtained. From these results, we conclude that (1) coronary β- receptors in pigs are predominately of β1-type, while those of aorta are of %bT2-type; (2) regarding the relative population of adrenoceptors, coronary artery is β-dominant (β/α = 11), while aorta is α- dominant (β/α = 0.02); (3) compared withα-adrenoceptors, coronary artery has a greater number of [H]nitrendipine binding sites (nitrendipine/α-adrenoceptor = 23) than aorta (nitrendipine/α-adrenoceptor = 0.14).</abstract><cop>Hagerstown, MD</cop><pub>American Heart Association, Inc</pub><pmid>3036396</pmid><doi>10.1161/01.RES.60.6.837</doi><tpages>8</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | Circ. Res.; (United States), 1987-06, Vol.60 (6), p.837-844 |
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| subjects | 550201 - Biochemistry- Tracer Techniques ANIMALS AORTA Aorta - metabolism ARTERIES AUTONOMIC NERVOUS SYSTEM AGENTS BASIC BIOLOGICAL SCIENCES Binding Sites BIOCHEMICAL REACTION KINETICS Biological and medical sciences BLOOD VESSELS Blood vessels and receptors BODY Calcium Channels CARDIOVASCULAR SYSTEM CELL CONSTITUENTS CELL MEMBRANES COMPARATIVE EVALUATIONS CORONARIES Coronary Vessels - metabolism Dihydroalprenolol - metabolism DOMESTIC ANIMALS DRUGS Fundamental and applied biological sciences. Psychology Iodocyanopindolol ISOTOPE APPLICATIONS KINETICS LABELLED COMPOUNDS LIGANDS MAMMALS MEMBRANE PROTEINS MEMBRANES Muscle, Smooth, Vascular - metabolism MUSCLES Nitrendipine - metabolism ORGANIC COMPOUNDS ORGANS Pindolol - analogs & derivatives Pindolol - metabolism Prazosin - metabolism PROTEINS REACTION KINETICS RECEPTORS Receptors, Adrenergic - metabolism Receptors, Nicotinic - metabolism SWINE SYMPATHOMIMETICS TRACER TECHNIQUES Tritium TRITIUM COMPOUNDS VERTEBRATES Vertebrates: cardiovascular system Yohimbine - metabolism |
| title | Characteristics of Adrenoceptors and [3H]Nitrendipine Receptors of Porcine Vascular Smooth Muscle: Differences Between Coronary Artery and Aorta |
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