{"title":"在高血压和衰老期间,去除外膜不会改变主动脉α 1d -肾上腺素受体的反应","authors":"J. H. Gómez-Zamudio, R. Villalobos-Molina","doi":"10.1111/j.1474-8673.2009.00432.x","DOIUrl":null,"url":null,"abstract":"<div>\n \n <p> <b>1</b> The aim of the current study was to characterize the α<sub>1</sub>-adrenergic receptors (α<sub>1</sub>-ARs) present in the isolated tunica media of aorta, in normotensive Wistar Kyoto (WKY) and spontaneously hypertensive (SHR) rats during the course of ageing and hypertension (rats of 1, 3, 6 and 12 months of age). In all vessels, endothelium was removed.</p>\n <p> <b>2</b> In isolated aortic rings, phenylephrine increased contraction in a concentration- and age-dependent manner and was impaired in old SHR compared with WKY rats.</p>\n <p> <b>3</b> The α<sub>1</sub>-AR selective antagonist prazosin showed high affinity (p<i>A</i><sub>2</sub>) in vessels from both rat strains.</p>\n <p> <b>4</b> The potency of the α<sub>1A</sub>-AR selective antagonists, RS 100329 (5-methyl-3-[3-[4-[2-(2,2,2,-trifluoroethoxy) phenyl]-1-piperazinyl] propyl]-2,4-(1H)-pyrimidinedione) and 5-methylurapidil in antagonizing aortic phenylephrine-responses was low.</p>\n <p> <b>5</b> The α<sub>1D</sub>-AR selective antagonist, BMY 7378 (8-[2-[4-(2-methoxyphenyl)-1 piperazynil] ethyl]-8-azaspiro [4.5] decane-7,9-dione) potently blocked phenylephrine-induced responses in aorta from both strains and at all ages.</p>\n <p> <b>6</b> Adventitia removal decreased <i>E</i><sub>max</sub> in older rats and modified the relative affinity (p<i>D</i><sub>2</sub>), but did not affect the affinity of the selective antagonists.</p>\n <p> <b>7</b> The results suggest that aorta tunica α<sub>1D</sub>-AR is the main subtype involved in phenylephrine-induced contraction of rat aorta, while α<sub>1A</sub>-AR plays only a minor role.</p>\n <p> <b>8</b> Ageing and hypertension did not modify α<sub>1</sub>-ARs in the blood vessel and the tunica adventitia does not seem to participate in contraction, even though α<sub>1</sub>-ARs are expressed.</p>\n </div>","PeriodicalId":100151,"journal":{"name":"Autonomic and Autacoid Pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2009-06-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1111/j.1474-8673.2009.00432.x","citationCount":"1","resultStr":"{\"title\":\"Adventitia removal does not modify the α1D-adrenoceptors response in aorta during hypertension and ageing\",\"authors\":\"J. H. Gómez-Zamudio, R. Villalobos-Molina\",\"doi\":\"10.1111/j.1474-8673.2009.00432.x\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div>\\n \\n <p> <b>1</b> The aim of the current study was to characterize the α<sub>1</sub>-adrenergic receptors (α<sub>1</sub>-ARs) present in the isolated tunica media of aorta, in normotensive Wistar Kyoto (WKY) and spontaneously hypertensive (SHR) rats during the course of ageing and hypertension (rats of 1, 3, 6 and 12 months of age). In all vessels, endothelium was removed.</p>\\n <p> <b>2</b> In isolated aortic rings, phenylephrine increased contraction in a concentration- and age-dependent manner and was impaired in old SHR compared with WKY rats.</p>\\n <p> <b>3</b> The α<sub>1</sub>-AR selective antagonist prazosin showed high affinity (p<i>A</i><sub>2</sub>) in vessels from both rat strains.</p>\\n <p> <b>4</b> The potency of the α<sub>1A</sub>-AR selective antagonists, RS 100329 (5-methyl-3-[3-[4-[2-(2,2,2,-trifluoroethoxy) phenyl]-1-piperazinyl] propyl]-2,4-(1H)-pyrimidinedione) and 5-methylurapidil in antagonizing aortic phenylephrine-responses was low.</p>\\n <p> <b>5</b> The α<sub>1D</sub>-AR selective antagonist, BMY 7378 (8-[2-[4-(2-methoxyphenyl)-1 piperazynil] ethyl]-8-azaspiro [4.5] decane-7,9-dione) potently blocked phenylephrine-induced responses in aorta from both strains and at all ages.</p>\\n <p> <b>6</b> Adventitia removal decreased <i>E</i><sub>max</sub> in older rats and modified the relative affinity (p<i>D</i><sub>2</sub>), but did not affect the affinity of the selective antagonists.</p>\\n <p> <b>7</b> The results suggest that aorta tunica α<sub>1D</sub>-AR is the main subtype involved in phenylephrine-induced contraction of rat aorta, while α<sub>1A</sub>-AR plays only a minor role.</p>\\n <p> <b>8</b> Ageing and hypertension did not modify α<sub>1</sub>-ARs in the blood vessel and the tunica adventitia does not seem to participate in contraction, even though α<sub>1</sub>-ARs are expressed.</p>\\n </div>\",\"PeriodicalId\":100151,\"journal\":{\"name\":\"Autonomic and Autacoid Pharmacology\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2009-06-22\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1111/j.1474-8673.2009.00432.x\",\"citationCount\":\"1\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Autonomic and Autacoid Pharmacology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://onlinelibrary.wiley.com/doi/10.1111/j.1474-8673.2009.00432.x\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Autonomic and Autacoid Pharmacology","FirstCategoryId":"1085","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1111/j.1474-8673.2009.00432.x","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Adventitia removal does not modify the α1D-adrenoceptors response in aorta during hypertension and ageing
1 The aim of the current study was to characterize the α1-adrenergic receptors (α1-ARs) present in the isolated tunica media of aorta, in normotensive Wistar Kyoto (WKY) and spontaneously hypertensive (SHR) rats during the course of ageing and hypertension (rats of 1, 3, 6 and 12 months of age). In all vessels, endothelium was removed.
2 In isolated aortic rings, phenylephrine increased contraction in a concentration- and age-dependent manner and was impaired in old SHR compared with WKY rats.
3 The α1-AR selective antagonist prazosin showed high affinity (pA2) in vessels from both rat strains.
4 The potency of the α1A-AR selective antagonists, RS 100329 (5-methyl-3-[3-[4-[2-(2,2,2,-trifluoroethoxy) phenyl]-1-piperazinyl] propyl]-2,4-(1H)-pyrimidinedione) and 5-methylurapidil in antagonizing aortic phenylephrine-responses was low.
5 The α1D-AR selective antagonist, BMY 7378 (8-[2-[4-(2-methoxyphenyl)-1 piperazynil] ethyl]-8-azaspiro [4.5] decane-7,9-dione) potently blocked phenylephrine-induced responses in aorta from both strains and at all ages.
6 Adventitia removal decreased Emax in older rats and modified the relative affinity (pD2), but did not affect the affinity of the selective antagonists.
7 The results suggest that aorta tunica α1D-AR is the main subtype involved in phenylephrine-induced contraction of rat aorta, while α1A-AR plays only a minor role.
8 Ageing and hypertension did not modify α1-ARs in the blood vessel and the tunica adventitia does not seem to participate in contraction, even though α1-ARs are expressed.