Propranolol-induced relaxation in the rat basilar artery

Çekiç, Edip Güvenç; Soydan, Guray; Guler, Sebile; Babaoğlu, Melih O.; Tuncer, Meral

doi:10.1016/j.vph.2012.12.004

Cited by 10 publications

(10 citation statements)

References 23 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Moreover, propranolol inhibited thromboxane A 2 production induced by cyclosporine A in rat aortae (ORIJI & SCHANZ 2001). There are numerous reports on the calcium influx blocking properties of ß-AR inhibitors in various vascular beds (CEKIC et al 2013;HOSTE & SYS 1998;HAYASHI-MORIMOTO et al 1999;PRIVIERO et al 2007).…”

Section: Discussionmentioning

confidence: 97%

β-adrenergic Antagonists Influence Abdominal Aorta Contractility by Mechanisms not Involving β-adrenergic Receptors

Hauzer¹,

Bujok²,

Czerski³

et al. 2014

folia biol (krakow)

View full text Add to dashboard Cite

â-adrenergic antagonists influence abdominal aorta contractility by mechanisms not involving â-adrenergic receptors. Folia Biologica (Kraków) 62: 243-250. â-adrenergic receptors (â-AR) are widely distributed in the cardiovascular system, where they considerably contribute to the control of its functions. â-blockers are commonly used in the treatment of disorders of the circulatory system. They act primarily by inhibiting cardiac â-receptors. However, there are also reports of pleiotropic action of â-blockers as well as of new compounds created to study â 3 adrenergic receptors. The study aimed to investigate additional mechanisms of action of â-AR inhibitors in the rabbit abdominal aorta with emphasis on their action on á-adrenergic receptors and calcium influx. Responses to propranolol, betaxolol, metoprolol and SR59230A were evaluated in phenylephrine and PGF 2alpha precontracted aortic rings. The effect of propranolol on the phenylephrine concentration-contraction curve was examined. Propranolol ($10 FM) and SR59230A ($0.1 FM) induced relaxations in phenylephrine-precontracted rings, while betaxolol and metoprolol had little effect. The â-AR inhibitors produced further contraction of tissues preincubated with PGF 2alpha , excluding SR59230A, which after initial contraction, elicited marked relaxation at a concentration above 1 ìM. 100 FM of propranolol caused a significant rightward shift of the concentration-contraction curve to phenylephrine with no reduction in the maximum response. Incubation of aortic rings in phentolamine reduced the maximal contraction to propranolol; verapamil pretreatment by contrast enhanced contractile response. In conclusion, SR59230A and propranolol most probably act as á 1-AR competitive antagonists in the presence of phenylephrine in rabbit abdominal aortic rings. After á-ARs blockade, propranolol exerts a weak relaxing activity connected with Ca 2+ channel inactivation. SR59230A at a high concentration acts on the rabbit aorta by an additional mechanism needing further investigation.

show abstract

Section: Discussionmentioning

confidence: 97%

β-adrenergic Antagonists Influence Abdominal Aorta Contractility by Mechanisms not Involving β-adrenergic Receptors

Hauzer¹,

Bujok²,

Czerski³

et al. 2014

folia biol (krakow)

View full text Add to dashboard Cite

show abstract

“…higher concentrations of propranolol were used. Other possible mechanisms of propranolol action may involve membrane stabilizing activity, effect on calcium channels, inhibition of thromboxane A 2 production, and antagonistic activity at 5-HT 1 receptors (MARANO et al 2002;SAKANASHI & TAKEO 1983;ORIJI & SCHANZ 2001;SAXENA & VILLALÓN 1990;CEKIC et al 2013). Propranolol and betaxolol were also equipotent in relaxing the bovine retinal microartery via a Ca 2+ channel blockade.…”

Section: Discussionmentioning

confidence: 97%

Nonspecific Effects of Ligands on the β-Adrenergic Receptors in Rabbit Abdominal Aorta in vitro

Gnus¹,

Czerski²,

Bujok³

et al. 2013

folia biol (krakow)

View full text Add to dashboard Cite

The study was conducted on 30 New Zealand rabbits weighing 3-4 kg from which sample strips of the abdominal aorta were collected. The study investigated the in vitro reaction of rabbit aorta smooth muscle to ligands binding to beta-adrenergic receptors. The response of aortic strips to beta-adrenergic receptor agonists (dobutamine, isoproterenol, salbutamol) and the influence of beta-adrenergic receptor antagonists (propranolol, betaxolol) on contractile activity was determined. All tested agonists induced contraction of the rabbit abdominal aorta muscle in a concentration-dependent manner (dobutamine >> isoproterenol > salbutamol). Enhanced reaction to low concentrations of agonists (dobutamine, isoproterenol) after administration of propranolol and inhibition of contractility in the presence of high concentrations thereof (dobutamine, salbutamol) was observed. Maximal reaction to agonists decreased after betaxolol pretreatment. The results indicate that all the substances with beta-agonist activity also possess contracting properties (presumably by acting at alpha-adrenergic receptors), but are much weaker in the case of isoproterenol and salbutamol than for dobutamine. Propranolol and betaxolol reduce the contractile response of smooth muscle using probably other mechanisms than those associated with adrenergic receptors.

show abstract

“…Priviero et al showed that propranolol-induced relaxation in rat aorta and mesenteric artery may occur, independent of beta-adrenoceptor blockade, via inhibition of calcium influx [ 49 ]. Similarly, Cekic et al suggested, that nonspecific beta-blocker propranolol exhibited calcium antagonist activity in rat basilar arteries [ 50 ].…”

Section: Discussionmentioning

confidence: 99%

The Beta-1-Receptor Blocker Nebivolol Elicits Dilation of Cerebral Arteries by Reducing Smooth Muscle [Ca2+]i

et al. 2016

View full text Add to dashboard Cite

RationaleNebivolol is known to have beta-1 blocker activity, but it was also suggested that it elicits relaxation of the peripheral arteries in part via release of nitric oxide (NO). However, the effect of nebivolol on the vasomotor tone of cerebral arteries is still unclear.ObjectiveTo assess the effects of nebivolol on the diameter of isolated rat basilar arteries (BA) in control, in the presence of inhibitors of vasomotor signaling pathways of know action and hemolysed blood.Methods and ResultsVasomotor responses were measured by videomicroscopy and the intracellular Ca2+ by the Fura-2 AM ratiometric method. Under control conditions, nebivolol elicited a substantial dilation of the BA (from 216±22 to 394±20 μm; p<0.05) in a concentration-dependent manner (10−7 to 10−4 M). The dilatation was significantly reduced by endothelium denudation or by L-NAME (inhibitor of NO synthase) or by SQ22536 (adenylyl cyclase blocker). Dilatation of BA was also affected by beta-2 receptor blockade with butoxamine, but not by the guanylate cyclase blocker ODQ. Interestingly, beta-1 blockade by atenolol inhibited nebivolol-induced dilation. Also, the BKCa channel blocker iberiotoxin and KCa channel inhibitor TEA significantly reduced nebivolol-induced dilation. Nebivolol significantly reduced smooth muscle Ca2+ level, which correlated with the increases in diameters and moreover it reversed the hemolysed blood-induced constriction of BA.ConclusionsNebivolol seems to have an important dilator effect in cerebral arteries, which is mediated via several vasomotor mechanisms, converging on the reduction of smooth muscle Ca2+ levels. As such, nebivolol may be effective to improve cerebral circulation in various diseased conditions, such as hemorrhage.

show abstract

Propranolol-induced relaxation in the rat basilar artery

Cited by 10 publications

References 23 publications

β-adrenergic Antagonists Influence Abdominal Aorta Contractility by Mechanisms not Involving β-adrenergic Receptors

β-adrenergic Antagonists Influence Abdominal Aorta Contractility by Mechanisms not Involving β-adrenergic Receptors

Nonspecific Effects of Ligands on the β-Adrenergic Receptors in Rabbit Abdominal Aorta in vitro

The Beta-1-Receptor Blocker Nebivolol Elicits Dilation of Cerebral Arteries by Reducing Smooth Muscle [Ca2+]i

Contact Info

Product

Resources

About