Adrenergic and Serotonergic Receptor-Blocking Potencies of Terazosin, a New Antihypertensive Agent, as Assessed by Radioligand Binding Assay
To assess the antihypertensive effect of terazosin, 2 [4- (tetrahydro-2-furanyl) carbonyl-l-piperazinyl] -6, 7-dimethoxy-4-quinazolinamine hydrochloride dihydrate, the inhibitory potency of terazosin on 3H-prazosin, 3H-p-aminoclonidine, 3H-dihydroalprenolol (3H-DHA), 3H-serotonin and 3H-ketanserin b...
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Veröffentlicht in: | Chemical & pharmaceutical bulletin 1987/04/25, Vol.35(4), pp.1629-1632 |
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creator | NAGATOMO, TAKAFUMI TAJIRI, AKIRA NAKAMURA, TAKASHI HOKIBARA, REI TANAKA, YUKO AONO, JUNICHIRO TSUCHIHASHI, HIROSHI |
description | To assess the antihypertensive effect of terazosin, 2 [4- (tetrahydro-2-furanyl) carbonyl-l-piperazinyl] -6, 7-dimethoxy-4-quinazolinamine hydrochloride dihydrate, the inhibitory potency of terazosin on 3H-prazosin, 3H-p-aminoclonidine, 3H-dihydroalprenolol (3H-DHA), 3H-serotonin and 3H-ketanserin bindings to α1-, α2-and β-adrenergic receptors and 5HT1 and 5HT2 (serotonergic) receptors was examined by using the radioligand binding method. The results were compared with those for prazosin and bunazosin. Dog brain and aorta were used in the present study. A high inhibition of 3H-prazosin binding to α1-adrenoceptors in dog aorta by terazosin was observed, but the inhibitions of 3H-DHA, 3H-p-aminoclonidine, 3H-serotonin and 3H-ketanserin bindings by this drug were very weak. l-Terazosin showed the greatest inhibitory effect on 3H-prazosin binding to α1-adrenoceptors in dog aorta and brain. These results suggest that an inhibitory effect of terazosin at α1-aradrenoceptor binding sites may contribute to the hypotensive effect; the α2-and β-adrenoceptors and the serotonergic binding sites do not appear to be involved. |
doi_str_mv | 10.1248/cpb.35.1629 |
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The results were compared with those for prazosin and bunazosin. Dog brain and aorta were used in the present study. A high inhibition of 3H-prazosin binding to α1-adrenoceptors in dog aorta by terazosin was observed, but the inhibitions of 3H-DHA, 3H-p-aminoclonidine, 3H-serotonin and 3H-ketanserin bindings by this drug were very weak. l-Terazosin showed the greatest inhibitory effect on 3H-prazosin binding to α1-adrenoceptors in dog aorta and brain. These results suggest that an inhibitory effect of terazosin at α1-aradrenoceptor binding sites may contribute to the hypotensive effect; the α2-and β-adrenoceptors and the serotonergic binding sites do not appear to be involved.</description><identifier>ISSN: 0009-2363</identifier><identifier>EISSN: 1347-5223</identifier><identifier>DOI: 10.1248/cpb.35.1629</identifier><identifier>PMID: 2888542</identifier><identifier>CODEN: CPBTAL</identifier><language>eng</language><publisher>Tokyo: The Pharmaceutical Society of Japan</publisher><subject>Adrenergic alpha-Antagonists - pharmacology ; alpha-adrenoceptor ; Animals ; antagonist ; Antihypertensive agents ; aorta ; Biological and medical sciences ; brain ; Brain Chemistry - drug effects ; Cardiovascular system ; dog ; Dogs ; In Vitro Techniques ; Male ; Medical sciences ; Pharmacology. Drug treatments ; Prazosin - analogs & derivatives ; Prazosin - pharmacology ; Radioligand Assay ; radioligand binding assay ; Receptors, Adrenergic - drug effects ; Receptors, Serotonin - drug effects ; serotonergic receptor</subject><ispartof>Chemical and Pharmaceutical Bulletin, 1987/04/25, Vol.35(4), pp.1629-1632</ispartof><rights>The Pharmaceutical Society of Japan</rights><rights>1988 INIST-CNRS</rights><rights>Copyright Japan Science and Technology Agency 1987</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,1883,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=7674000$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2888542$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>NAGATOMO, TAKAFUMI</creatorcontrib><creatorcontrib>TAJIRI, AKIRA</creatorcontrib><creatorcontrib>NAKAMURA, TAKASHI</creatorcontrib><creatorcontrib>HOKIBARA, REI</creatorcontrib><creatorcontrib>TANAKA, YUKO</creatorcontrib><creatorcontrib>AONO, JUNICHIRO</creatorcontrib><creatorcontrib>TSUCHIHASHI, HIROSHI</creatorcontrib><title>Adrenergic and Serotonergic Receptor-Blocking Potencies of Terazosin, a New Antihypertensive Agent, as Assessed by Radioligand Binding Assay</title><title>Chemical & pharmaceutical bulletin</title><addtitle>Chem. Pharm. Bull.</addtitle><description>To assess the antihypertensive effect of terazosin, 2 [4- (tetrahydro-2-furanyl) carbonyl-l-piperazinyl] -6, 7-dimethoxy-4-quinazolinamine hydrochloride dihydrate, the inhibitory potency of terazosin on 3H-prazosin, 3H-p-aminoclonidine, 3H-dihydroalprenolol (3H-DHA), 3H-serotonin and 3H-ketanserin bindings to α1-, α2-and β-adrenergic receptors and 5HT1 and 5HT2 (serotonergic) receptors was examined by using the radioligand binding method. The results were compared with those for prazosin and bunazosin. Dog brain and aorta were used in the present study. A high inhibition of 3H-prazosin binding to α1-adrenoceptors in dog aorta by terazosin was observed, but the inhibitions of 3H-DHA, 3H-p-aminoclonidine, 3H-serotonin and 3H-ketanserin bindings by this drug were very weak. l-Terazosin showed the greatest inhibitory effect on 3H-prazosin binding to α1-adrenoceptors in dog aorta and brain. These results suggest that an inhibitory effect of terazosin at α1-aradrenoceptor binding sites may contribute to the hypotensive effect; the α2-and β-adrenoceptors and the serotonergic binding sites do not appear to be involved.</description><subject>Adrenergic alpha-Antagonists - pharmacology</subject><subject>alpha-adrenoceptor</subject><subject>Animals</subject><subject>antagonist</subject><subject>Antihypertensive agents</subject><subject>aorta</subject><subject>Biological and medical sciences</subject><subject>brain</subject><subject>Brain Chemistry - drug effects</subject><subject>Cardiovascular system</subject><subject>dog</subject><subject>Dogs</subject><subject>In Vitro Techniques</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Prazosin - analogs & derivatives</subject><subject>Prazosin - pharmacology</subject><subject>Radioligand Assay</subject><subject>radioligand binding assay</subject><subject>Receptors, Adrenergic - drug effects</subject><subject>Receptors, Serotonin - drug effects</subject><subject>serotonergic receptor</subject><issn>0009-2363</issn><issn>1347-5223</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1987</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpdkV1rFDEUhoModa1eeS0EFK-cNZkkM5PLadUqFJVar4d8nJlmnU3GZFZZf0N_dLPs0IIQEpLn4ZxwXoReUrKmJW_em0mvmVjTqpSP0IoyXheiLNljtCKEyKJkFXuKnqW0IaQUpGYn6KRsmkbwcoVuWxvBQxycwcpb_ANimMPycAUGpjnE4mwM5pfzA_4eZvDGQcKhx9cQ1b-QnH-HFf4Kf3HrZ3eznyBmKbk_gNsB_Jxpwm1KkJfFeo-vlHVhdMOh35nz9lA4c7V_jp70akzwYjlP0c9PH6_PPxeX3y6-nLeXxYZTORd9BT2hWvfUaMWNlLqUrBKC00bqpteUa66shcZyxaTlklBZGcrzzShLDDtFb491pxh-7yDN3dYlA-OoPIRd6hpKaCUqkcXX_4mbsIs-_62jvCKUk1qQbL1arJ3egu2m6LYq7rtlyJm_WbhKRo19VHmE6V6rq5rnoLL24aht0qwGuOcqzs6M0OWYqRRNx0THj9sh8Qd8o2IHnt0BfVmj6w</recordid><startdate>19870401</startdate><enddate>19870401</enddate><creator>NAGATOMO, TAKAFUMI</creator><creator>TAJIRI, AKIRA</creator><creator>NAKAMURA, TAKASHI</creator><creator>HOKIBARA, REI</creator><creator>TANAKA, YUKO</creator><creator>AONO, JUNICHIRO</creator><creator>TSUCHIHASHI, HIROSHI</creator><general>The Pharmaceutical Society of Japan</general><general>Maruzen</general><general>Japan Science and Technology Agency</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7TK</scope><scope>7TM</scope><scope>7U9</scope><scope>H94</scope><scope>7X8</scope></search><sort><creationdate>19870401</creationdate><title>Adrenergic and Serotonergic Receptor-Blocking Potencies of Terazosin, a New Antihypertensive Agent, as Assessed by Radioligand Binding Assay</title><author>NAGATOMO, TAKAFUMI ; TAJIRI, AKIRA ; NAKAMURA, TAKASHI ; HOKIBARA, REI ; TANAKA, YUKO ; AONO, JUNICHIRO ; TSUCHIHASHI, HIROSHI</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-j419t-f6ef01bbf1cba4c99b2936554189b8fb14b4adde8d4a39d490196c144a3cad0c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1987</creationdate><topic>Adrenergic alpha-Antagonists - pharmacology</topic><topic>alpha-adrenoceptor</topic><topic>Animals</topic><topic>antagonist</topic><topic>Antihypertensive agents</topic><topic>aorta</topic><topic>Biological and medical sciences</topic><topic>brain</topic><topic>Brain Chemistry - drug effects</topic><topic>Cardiovascular system</topic><topic>dog</topic><topic>Dogs</topic><topic>In Vitro Techniques</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Prazosin - analogs & derivatives</topic><topic>Prazosin - pharmacology</topic><topic>Radioligand Assay</topic><topic>radioligand binding assay</topic><topic>Receptors, Adrenergic - drug effects</topic><topic>Receptors, Serotonin - drug effects</topic><topic>serotonergic receptor</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>NAGATOMO, TAKAFUMI</creatorcontrib><creatorcontrib>TAJIRI, AKIRA</creatorcontrib><creatorcontrib>NAKAMURA, TAKASHI</creatorcontrib><creatorcontrib>HOKIBARA, REI</creatorcontrib><creatorcontrib>TANAKA, YUKO</creatorcontrib><creatorcontrib>AONO, JUNICHIRO</creatorcontrib><creatorcontrib>TSUCHIHASHI, HIROSHI</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>Neurosciences Abstracts</collection><collection>Nucleic Acids Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Chemical & pharmaceutical bulletin</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>NAGATOMO, TAKAFUMI</au><au>TAJIRI, AKIRA</au><au>NAKAMURA, TAKASHI</au><au>HOKIBARA, REI</au><au>TANAKA, YUKO</au><au>AONO, JUNICHIRO</au><au>TSUCHIHASHI, HIROSHI</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Adrenergic and Serotonergic Receptor-Blocking Potencies of Terazosin, a New Antihypertensive Agent, as Assessed by Radioligand Binding Assay</atitle><jtitle>Chemical & pharmaceutical bulletin</jtitle><addtitle>Chem. Pharm. Bull.</addtitle><date>1987-04-01</date><risdate>1987</risdate><volume>35</volume><issue>4</issue><spage>1629</spage><epage>1632</epage><pages>1629-1632</pages><issn>0009-2363</issn><eissn>1347-5223</eissn><coden>CPBTAL</coden><abstract>To assess the antihypertensive effect of terazosin, 2 [4- (tetrahydro-2-furanyl) carbonyl-l-piperazinyl] -6, 7-dimethoxy-4-quinazolinamine hydrochloride dihydrate, the inhibitory potency of terazosin on 3H-prazosin, 3H-p-aminoclonidine, 3H-dihydroalprenolol (3H-DHA), 3H-serotonin and 3H-ketanserin bindings to α1-, α2-and β-adrenergic receptors and 5HT1 and 5HT2 (serotonergic) receptors was examined by using the radioligand binding method. The results were compared with those for prazosin and bunazosin. Dog brain and aorta were used in the present study. A high inhibition of 3H-prazosin binding to α1-adrenoceptors in dog aorta by terazosin was observed, but the inhibitions of 3H-DHA, 3H-p-aminoclonidine, 3H-serotonin and 3H-ketanserin bindings by this drug were very weak. l-Terazosin showed the greatest inhibitory effect on 3H-prazosin binding to α1-adrenoceptors in dog aorta and brain. These results suggest that an inhibitory effect of terazosin at α1-aradrenoceptor binding sites may contribute to the hypotensive effect; the α2-and β-adrenoceptors and the serotonergic binding sites do not appear to be involved.</abstract><cop>Tokyo</cop><pub>The Pharmaceutical Society of Japan</pub><pmid>2888542</pmid><doi>10.1248/cpb.35.1629</doi><tpages>4</tpages><oa>free_for_read</oa></addata></record> |
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subjects | Adrenergic alpha-Antagonists - pharmacology alpha-adrenoceptor Animals antagonist Antihypertensive agents aorta Biological and medical sciences brain Brain Chemistry - drug effects Cardiovascular system dog Dogs In Vitro Techniques Male Medical sciences Pharmacology. Drug treatments Prazosin - analogs & derivatives Prazosin - pharmacology Radioligand Assay radioligand binding assay Receptors, Adrenergic - drug effects Receptors, Serotonin - drug effects serotonergic receptor |
title | Adrenergic and Serotonergic Receptor-Blocking Potencies of Terazosin, a New Antihypertensive Agent, as Assessed by Radioligand Binding Assay |
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