β2- and β3-Adrenoreceptor agonists: Human myometrial selectivity and effects on umbilical artery tone

Dennedy, Michael Conall; Houlihan, Diarmaid D.; McMillan, Helen; Morrison, John J.

doi:10.1067/mob.2002.125277

Cited by 49 publications

(35 citation statements)

References 16 publications

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“…This effect is at least in part due to smooth muscle relaxation in the arterial wall and is in line with the in vitro observation on the umbilical artery by Dennedy et al. [34] The large effect on the less muscular CCA is somewhat surprising and is correlated with the strong vasodilation, although an ancillary acute mechanism cannot fully be excluded.In contrast, stiffness of the more elastic aorta, measured by pulse wave velocity, did not change with ritodrine. However, a small direct effect hidden by the indirect effects of changes in blood pressure and heart rate could not be expelled.…”

Section: Discussionsupporting

confidence: 69%

The influence of tocolytic drugs on cardiac function, large arteries, and resistance vessels

Fabry

Paepe

Kips

et al. 2011

Eur J Clin Pharmacol

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Section: Discussionsupporting

confidence: 69%

The influence of tocolytic drugs on cardiac function, large arteries, and resistance vessels

Fabry

Paepe

Kips

et al. 2011

Eur J Clin Pharmacol

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“…Rouget et al (2005) provided the first evidence that not only are β 3 -receptors present, but that they are also the predominant subtype compared to β 2 -receptors, both in human non-pregnant and pregnant myometrium. More recently, Dennedy et al (2002) showed that BRL 37344 induced relaxation of human myometrial strips from biopsies obtained from caesarean sections with a similar potency to ritodrine. Pędzińska-Bietuk et al 2008, using another agonist (CL 316243), also confirmed the participation of β 3 -adrenoceptors in the inhibition of spontaneous contractile activity of human non-pregnant myometrium.…”

Section: Discussionmentioning

confidence: 99%

Influence of β2- and β3-adrenoceptor agonists on contractile activity of the porcine myometrium in the luteal phase and the first days of pregnancy

Markiewicz

Jaroszewski

2017

Polish Journal of Veterinary Sciences

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This study analysed the relaxant properties of salbutamol (β 2 -adrenoceptors agonist) and BRL 37344 (β 3 -adrenoceptors agonist) regarding the contractility of porcine myometrium on days 10-14 of the oestrous cycle (cyclic group; n = 10) and on days 3-5 of pregnancy (early pregnant group; n = 6). The activity of myometrial strips (tension, frequency and amplitude) was recorded under isometric conditions using force transducers. The contractility was assessed further following the administration of increasing concentrations of the agonists (10 -9 -10 -4 M), both with and without β-adrenoceptorantagonists (butaxamine -a selective β 2 -adrenoceptor antagonist, propranolol-a non-selective β 1 -and β 2 -adrenoceptor antagonist and bupranolol -a non-selective β 1 -, β 2 -and β 3 -adrenoceptor antagonist) at a concentration of 10 -4 M. Although neither salbutamol nor BRL 37344 caused changes in the tension, at the highest concentrations they decreased the frequency and amplitude of contractions. These changes were more evident after salbutamol treatment and in the early pregnant group. Antagonists given alone did not cause changes in the parameters examined but changed some activity of the agonists. Butoxamine reduced the decrease in frequency and amplitude induced by salbutamol and produced a decrease in the tension after BRL 37344 treatment in the early pregnant group. Propranolol reduced the decrease in frequency and amplitude induced by salbutamol in both examined groups and did not cause significant changes in BRL 37344 activity. The administration of bupranolol before salbutamol treatment caused an increase in the tension and reduced the decrease in the frequency in the cyclic group. Moreover, bupranolol eliminated a decrease in frequency and induced an increase in amplitude caused by BRL 37344 in both groups and these changes were more evident in the early pregnant group. The data indicates that both β 2 -and β 3 -adenoreceptors are involved in the regulation of the contractility in both groups, but the changes after agonists and antagonists treatment are more evident in the early pregnant myometrium.

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“…However, there is emerging literature which suggests that the β 3 -adrenoceptor may also play a role in uterine quiescence and actually be up-regulated near term in humans and rats [7,8,9,16,20]. SR 59119A has been reported to be a selective β 3 -adrenoceptor agonist [21], and has been inhibited of near term human myometrial contraction by SR 59119A [7].…”

Section: Discussionmentioning

confidence: 99%

Effects and Selectivity of CL 316243, Beta-3-Adrenoceptor Agonist, in Term-Pregnant Rat Myometrium

Kaya

Karadaş

Altun

et al. 2011

Gynecol Obstet Invest

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Background/Aims: Recent evidence supports a predominant role of β₃-adrenoceptors at the end of pregnancy in myometrium. This study was designed to characterize the pharmacology of the selective β₃-adrenoceptor agonist CL 316243 on oxytocin-induced myometrial contractions and the levels of cAMP and cGMP of myometrial strips isolated from term-pregnant rats. Methods: Myometrial strips were obtained from term-pregnant Wistar albino rats (n = 10), mounted in organ baths and tested for changes in isometric tension in response to CL 316243 (10^–10–10^–5M) on oxytocin-induced myometrial contractions. Effects of CL 316243 on cAMP and cGMP levels in isolated myometrial strips (n = 8) were evaluated by radioimmunoassay kits. We evaluated the effect of increasing concentrations of CL 316243 on myometrial contractions and on contractions of myometrial smooth muscle pretreated with metoprolol, ICI 118.551 and SR 59230A (β₁-, β₂-, β₃-adrenoceptor antagonists, respectively, 10^–6M). Results: The inhibition of the amplitude of oxytocin-induced contractions by CL 316243 were antagonized with SR 59230A (10^–6M), but they were not changed by metoprolol (10^–6M) or ICI 118.551 (10^–6M). CL 316243 increased cAMP levels compared to the control group. CL 316243 increased cGMP levels, in the CL 316243 group more than in the control group, but this increase is less significant than cAMP levels. Conclusion: These results demonstrate that the inhibition of rat myometrial contractions with CL 316243 is mediated by β₃-adrenoceptor subtype and increased cAMP and cGMP levels.

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β2- and β3-Adrenoreceptor agonists: Human myometrial selectivity and effects on umbilical artery tone

Cited by 49 publications

References 16 publications

The influence of tocolytic drugs on cardiac function, large arteries, and resistance vessels

The influence of tocolytic drugs on cardiac function, large arteries, and resistance vessels

Influence of β2- and β3-adrenoceptor agonists on contractile activity of the porcine myometrium in the luteal phase and the first days of pregnancy

Effects and Selectivity of CL 316243, Beta-3-Adrenoceptor Agonist, in Term-Pregnant Rat Myometrium

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