Effects of the β-Receptor Antagonists Propranolol, Oxprenolol and Labetalol on Human Vascular Smooth-Muscle Contraction

1978 ◽  
Vol 55 (3) ◽  
pp. 235-240
Author(s):  
R. F. W. Moulds ◽  
R. A. Jauernig ◽  
J. D. Hobson ◽  
J. Shaw

1. Spiral strips of human digital arteries have been studied in vitro to investigate whether dl-propranolol, d-propranolol, oxprenolol and labetalol have peripheral vascular effects in man. 2. Labetalol was a potent inhibitor of contractile responses to noradrenaline, but had less effect on responses to 5-hydroxytryptamine and barium chloride. 3. dl-and d-propranolol were equally effective inhibitors of responses to barium chloride. They were only weak antagonists of noradrenaline responses, but stronger, non-competitive antagonists of 5-hydroxytryptamine responses. 4. Oxprenolol was only a weak inhibitor of the responses to both noradrenaline and 5-hydroxytryptamine and had little effect on responses to barium chloride. 5. It is concluded that labetalol has specific α-adrenoreceptor-blocking properties, which are probably relevant to its therapeutic action in man. Propranolol has non-specific inhibitory effects on vascular smooth muscle, which might contribute to its hypotensive activity at high concentrations, but oxprenolol has only slight peripheral effects that are probably therapeutically insignificant.

1975 ◽  
Vol 229 (1) ◽  
pp. 8-12 ◽  
Author(s):  
HS Solomon ◽  
NK Hollenberg

The mechanism by which mercuric ion (HgCl2) induces contraction of vascular smooth muscle was defined in the kidney of anesthetized dogs and in rabbit aortic strips. In vivo, HgCl2 injected into the renal artery induced a dose-related reduction in renal blood flow (electromagnetic flowmeter) and glomerular filtration rate (creatinine clearance). An intra-arterial infusion of phenoxybenzamine (POB) significantly reduced the vascular response to HgCl2 (P less than 0.001). In vitro, alpha-adrenergic blockade with phentolamine and POB prevented mercury-induced contraction, whereas agents that block serotonin, histamine, acetylcholine, and angiotensin did not do so. Norepinephrine receptor "protection" from phenoxybenzamine blockade sustained the response to HgCl2. Reserpine pretreatment produced a parallel reduction in the response of the aorta to tyramine and mercury. The results are consistent with an indirect action of mercuric ion via release of endogenous catecholamines.


1983 ◽  
Vol 3 (3) ◽  
pp. 395-398 ◽  
Author(s):  
Lennart Brandt ◽  
Karl-Erik Andersson ◽  
Bengt Hindfelt ◽  
Bengt Ljunggren ◽  
John D. Pickard

In vitro, the Nalonee® preparation of naloxone caused a concentration-dependent relaxation of human pial cortical arteries contracted by potassium, noradrenaline, serotonin, prostaglandin F2α (PGF2α), and haemorrhagic cerebrospinal fluid, or inhibited contractions elicited by these agents. However, the preservatives in the Nalonee preparation, methyl- and propylparaben, had similar effects. Pure naloxone alone had no effect on potassium or PGF2α-induced contractions. It is suggested that the relaxant effects on vascular smooth muscle of Nalonee can be attributed to the alkylparabens rather than to naloxone. The pronounced relaxations induced by the alkylparabens had a rapid onset, and they were stable and could easily be cleared after rinsing.


2009 ◽  
Vol 60-61 ◽  
pp. 125-129
Author(s):  
Su Su Zhao ◽  
Qin Lu ◽  
Dong Sheng Zhang

Proliferation and migration of vascular smooth muscle cells(VSMCs) into the sub-intimal space play an important role in intimal thickening in atherosclerosis and in-stent restenosis. Arsenic compounds are natural substances that have been used in the treatment of patients with acute promyelocytic leukemia (APL).And Arsenic trioxide (As2O3) is known to be a potent inhibitor of cell proliferation.The aim of this study was to prepare arsenic trioxide (As2O3) -loaded PLGA nanoparticles(As2O3-PLGA-NP) and investigate its general properties, preservation of As2O3 bioactivity and their inhibitory effects on Rabbit Vascular Smooth Muscle Cells(RVSMCs) in vitro. With PLGA as carrier,As2O3 drug delivery nanoparticles were prepared by w /o /w double-emulsion evaporation technique,and their inhibitory effects on Rabbit Vascular Smooth Muscle Cells(VSMCs) in vitro was investigated.The results of the experiment show the self-prepared As2O3-PLGA-NP were approximately spherical,with the mean diameter of 90±25.03 nm, and the average drug loading was 1.72% .The As2O3-PLGA-NP has drug sustained-release character and can prolong the phase of the inhibitory effect of As2O3 against RVSMCs.The As2O3-PLGA-NP do not reduce the biological activity of As2O3.


2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Hak Rim Kim ◽  
Cynthia Gallant ◽  
Kathleen G. Morgan

Protein kinase C (PKC) is a key enzyme involved in agonist-induced smooth muscle contraction. In some cases, regulatory phosphorylation of PKC is required for full activation of the enzyme. However, this issue has largely been ignored with respect to PKC-dependent regulation of contractile vascular smooth muscle (VSM) contractility. The first event in PKC regulation is a transphosphorylation by PDK at a conserved threonine in the activation loop of PKC, followed by the subsequent autophosphorylation at the turn motif and hydrophobic motif sites. In the present study, we determined whether phosphorylation of PKC is a regulated process in VSM and also investigated a potential role of calponin in the regulation of PKC. We found that calponin increases the level of in vitro PKCαphosphorylation at the PDK and hydrophobic sites, but not the turn motif site. In vascular tissues, phosphorylation of the PKC hydrophobic site, but not turn motif site, as well as phosphorylation of PDK at S241 increased in response to phenylephrine. Calponin knockdown inhibits autophosphorylation of cellular PKC in response to phenylephrine, confirming results with recombinant PKC. Thus these results show that autophosphorylation of PKC is regulated in dVSM and calponin is necessary for autophosphorylation of PKC in VSM.


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