Vasorelaxant effects of the potassium channel opener SR 47063 on the isolated human saphenous vein and rat aorta
Autor(a) principal: | |
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Data de Publicação: | 2000 |
Outros Autores: | |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Brazilian Journal of Medical and Biological Research |
Texto Completo: | http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2000000800013 |
Resumo: | The vasorelaxant effects of SR 47063 (4-(2-cyanimino-1,2-dihydropyrid-1-yl)-2,2-dimethyl-6-nitrochromene), a new K+-channel opener structurally related to levcromakalim, were examined in isolated human saphenous vein (HSV) and rat aorta (RA). HSV or RA rings were precontracted with either KCl or noradrenaline and cumulative relaxant concentration-response curves were obtained for SR 47063 (0.1 nM to 1 µM) in the presence or absence of 3 µM glibenclamide. SR 47063 potently relaxed HSV and RA precontracted with 20 mM (but not 60 mM) KCl or 10 µM noradrenaline in a concentration-dependent manner, showing slightly greater activity in the aorta. The potency of the effect of SR 47063 on HSV and RA was 12- and 58-fold greater, respectively, than that reported for the structurally related K+-channel opener levcromakalim. The vasorelaxant action of SR 47063 in both blood vessels was strongly inhibited by 3 µM glibenclamide, consistent with a mechanism of action involving ATP-dependent K+-channels. |
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Brazilian Journal of Medical and Biological Research |
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Vasorelaxant effects of the potassium channel opener SR 47063 on the isolated human saphenous vein and rat aortaSR 47063K+-channelhuman saphenous veinK ATPrat aortalevcromakalimglibenclamideThe vasorelaxant effects of SR 47063 (4-(2-cyanimino-1,2-dihydropyrid-1-yl)-2,2-dimethyl-6-nitrochromene), a new K+-channel opener structurally related to levcromakalim, were examined in isolated human saphenous vein (HSV) and rat aorta (RA). HSV or RA rings were precontracted with either KCl or noradrenaline and cumulative relaxant concentration-response curves were obtained for SR 47063 (0.1 nM to 1 µM) in the presence or absence of 3 µM glibenclamide. SR 47063 potently relaxed HSV and RA precontracted with 20 mM (but not 60 mM) KCl or 10 µM noradrenaline in a concentration-dependent manner, showing slightly greater activity in the aorta. The potency of the effect of SR 47063 on HSV and RA was 12- and 58-fold greater, respectively, than that reported for the structurally related K+-channel opener levcromakalim. The vasorelaxant action of SR 47063 in both blood vessels was strongly inhibited by 3 µM glibenclamide, consistent with a mechanism of action involving ATP-dependent K+-channels.Associação Brasileira de Divulgação Científica2000-08-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2000000800013Brazilian Journal of Medical and Biological Research v.33 n.8 2000reponame:Brazilian Journal of Medical and Biological Researchinstname:Associação Brasileira de Divulgação Científica (ABDC)instacron:ABDC10.1590/S0100-879X2000000800013info:eu-repo/semantics/openAccessCriddle,D.N.de Moura,R.S.eng2000-07-31T00:00:00Zoai:scielo:S0100-879X2000000800013Revistahttps://www.bjournal.org/https://old.scielo.br/oai/scielo-oai.phpbjournal@terra.com.br||bjournal@terra.com.br1414-431X0100-879Xopendoar:2000-07-31T00:00Brazilian Journal of Medical and Biological Research - Associação Brasileira de Divulgação Científica (ABDC)false |
dc.title.none.fl_str_mv |
Vasorelaxant effects of the potassium channel opener SR 47063 on the isolated human saphenous vein and rat aorta |
title |
Vasorelaxant effects of the potassium channel opener SR 47063 on the isolated human saphenous vein and rat aorta |
spellingShingle |
Vasorelaxant effects of the potassium channel opener SR 47063 on the isolated human saphenous vein and rat aorta Criddle,D.N. SR 47063 K+-channel human saphenous vein K ATP rat aorta levcromakalim glibenclamide |
title_short |
Vasorelaxant effects of the potassium channel opener SR 47063 on the isolated human saphenous vein and rat aorta |
title_full |
Vasorelaxant effects of the potassium channel opener SR 47063 on the isolated human saphenous vein and rat aorta |
title_fullStr |
Vasorelaxant effects of the potassium channel opener SR 47063 on the isolated human saphenous vein and rat aorta |
title_full_unstemmed |
Vasorelaxant effects of the potassium channel opener SR 47063 on the isolated human saphenous vein and rat aorta |
title_sort |
Vasorelaxant effects of the potassium channel opener SR 47063 on the isolated human saphenous vein and rat aorta |
author |
Criddle,D.N. |
author_facet |
Criddle,D.N. de Moura,R.S. |
author_role |
author |
author2 |
de Moura,R.S. |
author2_role |
author |
dc.contributor.author.fl_str_mv |
Criddle,D.N. de Moura,R.S. |
dc.subject.por.fl_str_mv |
SR 47063 K+-channel human saphenous vein K ATP rat aorta levcromakalim glibenclamide |
topic |
SR 47063 K+-channel human saphenous vein K ATP rat aorta levcromakalim glibenclamide |
description |
The vasorelaxant effects of SR 47063 (4-(2-cyanimino-1,2-dihydropyrid-1-yl)-2,2-dimethyl-6-nitrochromene), a new K+-channel opener structurally related to levcromakalim, were examined in isolated human saphenous vein (HSV) and rat aorta (RA). HSV or RA rings were precontracted with either KCl or noradrenaline and cumulative relaxant concentration-response curves were obtained for SR 47063 (0.1 nM to 1 µM) in the presence or absence of 3 µM glibenclamide. SR 47063 potently relaxed HSV and RA precontracted with 20 mM (but not 60 mM) KCl or 10 µM noradrenaline in a concentration-dependent manner, showing slightly greater activity in the aorta. The potency of the effect of SR 47063 on HSV and RA was 12- and 58-fold greater, respectively, than that reported for the structurally related K+-channel opener levcromakalim. The vasorelaxant action of SR 47063 in both blood vessels was strongly inhibited by 3 µM glibenclamide, consistent with a mechanism of action involving ATP-dependent K+-channels. |
publishDate |
2000 |
dc.date.none.fl_str_mv |
2000-08-01 |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2000000800013 |
url |
http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2000000800013 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
10.1590/S0100-879X2000000800013 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
text/html |
dc.publisher.none.fl_str_mv |
Associação Brasileira de Divulgação Científica |
publisher.none.fl_str_mv |
Associação Brasileira de Divulgação Científica |
dc.source.none.fl_str_mv |
Brazilian Journal of Medical and Biological Research v.33 n.8 2000 reponame:Brazilian Journal of Medical and Biological Research instname:Associação Brasileira de Divulgação Científica (ABDC) instacron:ABDC |
instname_str |
Associação Brasileira de Divulgação Científica (ABDC) |
instacron_str |
ABDC |
institution |
ABDC |
reponame_str |
Brazilian Journal of Medical and Biological Research |
collection |
Brazilian Journal of Medical and Biological Research |
repository.name.fl_str_mv |
Brazilian Journal of Medical and Biological Research - Associação Brasileira de Divulgação Científica (ABDC) |
repository.mail.fl_str_mv |
bjournal@terra.com.br||bjournal@terra.com.br |
_version_ |
1754302930539773952 |