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
Hauptverfasser: NAGATOMO, TAKAFUMI, TAJIRI, AKIRA, NAKAMURA, TAKASHI, HOKIBARA, REI, TANAKA, YUKO, AONO, JUNICHIRO, TSUCHIHASHI, HIROSHI
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container_end_page 1632
container_issue 4
container_start_page 1629
container_title Chemical & pharmaceutical bulletin
container_volume 35
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. 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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. 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Drug treatments</topic><topic>Prazosin - analogs &amp; 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 &amp; 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 &amp; 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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