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Vasorelaxant effects of the potassium channel opener SR 47063 on the isolated human saphenous vein and rat aorta BJMBR
Criddle,D.N.; de Moura,R.S..
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...
Tipo: Info:eu-repo/semantics/article Palavras-chave: SR 47063; K+-channel; Human saphenous vein; K ATP; Rat aorta; Levcromakalim; Glibenclamide.
Ano: 2000 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2000000800013
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The methyl ester of rosuvastatin elicited an endothelium-independent and 3-hydroxy-3-methylglutaryl coenzyme A reductase-independent relaxant effect in rat aorta BJMBR
López-Canales,J.S.; López-Sanchez,P.; Perez-Alvarez,V.M.; Wens-Flores,I.; Polanco,A.C.; Castillo-Henkel,E.; Castillo-Henkel,C..
The relaxant effect of the methyl ester of rosuvastatin was evaluated on aortic rings from male Wistar rats (250-300 g, 6 rats for each experimental group) with and without endothelium precontracted with 1.0 µM phenylephrine. The methyl ester presented a slightly greater potency than rosuvastatin in relaxing aortic rings, with log IC50 values of -6.88 and -6.07 M, respectively. Unlike rosuvastatin, the effect of its methyl ester was endothelium-independent. Pretreatment with 10 µM indomethacin did not inhibit, and pretreatment with 1 mM mevalonate only modestly inhibited the relaxant effect of the methyl ester. Nω-nitro-L-arginine methyl ester (L-NAME, 10 µM), the selective nitric oxide-2 (NO-2) inhibitor 1400 W (10 µM), tetraethylammonium (TEA, 10 mM),...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Rat aorta; Rosuvastatin methyl ester; Endothelium-independent relaxation; Potassium channels; NOS-2.
Ano: 2011 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2011000500009
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Gap junctions in isolated rat aorta: evidence for contractile responses that exhibit a differential dependence on intercellular communication BJMBR
Christ,G.J.; Brink,P.R..
Connexin43 (Cx43) is a major gap junction protein present in the Fischer-344 rat aorta. Previous studies have identified conditions under which selective disruption of intercellular communication with heptanol caused a significant, readily reversible and time-dependent diminution in the magnitude of <FONT FACE="Symbol">a</font>1-adrenergic contractions in isolated rat aorta. These observations have indentified a significant role for gap junctions in modulating vascular smooth muscle tone. The goal of these steady-state studies was to utilize isolated rat aortic rings to further evaluate the contribution of intercellular junctions to contractions elicited by cellular activation in response to several other vascular spasmogens. The effects of...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Gap junctions; Connexin43; Rat aorta; Vascular smooth muscle; Intercellular communication.
Ano: 2000 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2000000400008
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Inhibition of PKC-dependent extracellular Ca2+ entry contributes to the depression of contractile activity in long-term pressure-overloaded endothelium-denuded rat aortas BJMBR
Padilla,J.; López,R.M.; López,P.; Castillo,M.C.; Querejeta,E.; Ruiz,A.; Castillo,E.F..
We examined the contractile responsiveness of rat thoracic aortas under pressure overload after long-term suprarenal abdominal aortic coarctation (lt-Srac). Endothelium-dependent angiotensin II (ANG II) type 2 receptor (AT2R)-mediated depression of contractions to ANG II has been reported in short-term (1 week) pressure-overloaded rat aortas. Contractility was evaluated in the aortic rings of rats subjected to lt-Srac or sham surgery (Sham) for 8 weeks. ANG I and II levels and AT2R protein expression in the aortas of lt-Srac and Sham rats were also evaluated. lt-Srac attenuated the contractions of ANG II and phenylephrine in the aortas in an endothelium-independent manner. However, lt-Srac did not influence the transient contractions induced in...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Long-term pressure overload; Rat aorta; Protein kinase C.
Ano: 2014 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2014000900789
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Pharmacological study of the mechanisms involved in the vasodilator effect produced by the acute application of triiodothyronine to rat aortic rings BJMBR
Lozano-Cuenca,J.; López-Canales,O.A.; Aguilar-Carrasco,J.C.; Villagrana-Zesati,J.R.; López-Mayorga,R.M.; Castillo-Henkel,E.F.; López-Canales,J.S..
A relationship between thyroid hormones and the cardiovascular system has been well established in the literature. The present in vitro study aimed to investigate the mechanisms involved in the vasodilator effect produced by the acute application of 10-8–10-4 M triiodothyronine (T3) to isolated rat aortic rings. Thoracic aortic rings from 80 adult male Wistar rats were isolated and mounted in tissue chambers filled with Krebs-Henseleit bicarbonate buffer in order to analyze the influence of endothelial tissue, inhibitors and blockers on the vascular effect produced by T3. T3 induced a vasorelaxant response in phenylephrine-precontracted rat aortic rings at higher concentrations (10-4.5–10-4.0 M). This outcome was unaffected by 3.1×10-7 M glibenclamide,...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Triiodothyronine; Rat aorta; Vasorelaxation; NO-cGMP/PKG pathway; K+ channels.
Ano: 2016 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2016000800604
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Possible mechanisms involved in the vasorelaxant effect produced by clobenzorex in aortic segments of rats BJMBR
Lozano-Cuenca,J.; González-Hernández,A.; López-Canales,O.A.; Villagrana-Zesati,J.R.; Rodríguez-Choreão,J.D.; Morín-Zaragoza,R.; Castillo-Henkel,E.F.; López-Canales,J.S..
Clobenzorex is a metabolic precursor of amphetamine indicated for the treatment of obesity. Amphetamines have been involved with cardiovascular side effects such as hypertension and pulmonary arterial hypertension. The aim of the present study was to investigate whether the direct application of 10–9–10–5 M clobenzorex on isolated phenylephrine-precontracted rat aortic rings produces vascular effects, and if so, what mechanisms may be involved. Clobenzorex produced an immediate concentration-dependent vasorelaxant effect at the higher concentrations (10–7.5–10–5 M). The present outcome was not modified by 10–6 M atropine (an antagonist of muscarinic acetylcholine receptors), 3.1×10–7 M glibenclamide (an ATP-sensitive K+ channel blocker), 10–3 M...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Clobenzorex; Rat aorta; Vasorelaxation; NO-cGMP; PKG pathway; K+ channels.
Ano: 2017 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2017000900605
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Possible mechanisms involved in the effect of the subchronic administration of rosuvastatin on endothelial function in rats with metabolic syndrome BJMBR
Lozano-Cuenca,J.; Valencia-Hernández,I.; López-Canales,O.A.; Flores-Herrera,H.; López-Mayorga,R.M.; Castillo-Henkel,E.F.; López-Canales,J.S..
Metabolic syndrome is a multifaceted condition associated with a greater risk of various disorders (e.g., diabetes and heart disease). In a rat model of metabolic syndrome, an acute in vitro application of rosuvastatin causes relaxation of aortic rings. Since the outcome of a subchronic rosuvastatin treatment is unknown, the present study explored its effect on acetylcholine-induced vasorelaxation of aortic rings from rats with metabolic syndrome. Animals were submitted to a 16-week treatment, including a standard diet, a cafeteria-style diet (CAF-diet), or a CAF-diet with daily rosuvastatin treatment (10 mg/kg). After confirming the development of metabolic syndrome in rats, aortic segments were extracted from these animals (those treated with...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Rosuvastatin; Metabolic syndrome; Rat aorta; Vasorelaxation; NO; K+ channel.
Ano: 2020 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2020000200607
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Mechanisms involved in the vasorelaxant effects produced by the acute application of amfepramone in vitro to rat aortic rings BJMBR
López-Canales,J.S.; Lozano-Cuenca,J.; Muãoz-Islas,E.; Aguilar-Carrasco,J.C.; López-Canales,O.A.; López-Mayorga,R.M.; Castillo-Henkel,E.F.; Valencia-Hernández,I.; Castillo-Henkel,C..
Amfepramone (diethylpropion) is an appetite-suppressant drug used for the treatment of overweight and obesity. It has been suggested that the systemic and central activity of amfepramone produces cardiovascular effects such as transient ischemic attacks and primary pulmonary hypertension. However, it is not known whether amfepramone produces immediate vascular effects when applied in vitro to rat aortic rings and, if so, what mechanisms may be involved. We analyzed the effect of amfepramone on phenylephrine-precontracted rat aortic rings with or without endothelium and the influence of inhibitors or blockers on this effect. Amfepramone produced a concentration-dependent vasorelaxation in phenylephrine-precontracted rat aortic rings that was not affected by...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Cardiovascular pharmacology; Amfepramone; Obesity; Rat aorta; Nitric oxide; Potassium channels.
Ano: 2015 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2015000600537
Registros recuperados: 8
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