Newer beta blockers and the treatment of hypertension

McAreavey, Dorothea; Vermeulen, Royce; Robertson, James I.

doi:10.1007/bf03029727

Cited by 10 publications

(3 citation statements)

References 115 publications

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“…Previous reports [1,2] showed that betaxolol, in contrast with other beta-blockers, has no adverse effect on lipid metabolism and carbohydrate metabolism. McAreavy et al [3] reviewed the new beta-blockers and the treatment of hypertension, and they reported that betaxolol decreases LDL cholesterol levels. McAreavy et al [3] reviewed the new beta-blockers and the treatment of hypertension, and they reported that betaxolol decreases LDL cholesterol levels.…”

Section: Discussionmentioning

confidence: 99%

Effects of beta-blockers on HMG CoA reductase and LDL receptor activity in cultured human skin fibroblasts

Yoshida

Suzukawa

Ishikawa

et al. 1996

Cardiovasc Drug Ther

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Previous reports, based on clinical trials and animal experiments, suggest that beta-blockers may be useful in the prevention of atherosclerosis. Betaxolol, a new beta1-selective blocker, was shown to decrease plasma total and LDL cholesterol levels or to have no adverse effect on those [1-4]. While many reports deal with metabolism of triglyceride and high density lipoprotein, fewer publications about cholesterol metabolism are currently available. To clarify the mechanism by which beta-blockers affect lipid metabolism, we examined the effects of beta-blockers on HMG CoA reductase and LDL receptor activity in cultured human skin fibroblasts. L-propranolol, a nonselective beta-blocker, increased HMG CoA reductase activity and decreased LDL receptor activity. However, d-propranolol had no major effects on HMG CoA reductase activity. These results suggest that beta-blockers act on HMG CoA reductase through the beta receptors. Beta1-blocking action should decrease HMG CoA reductase activity and increase LDL receptor activity. In fact, betaxolol, a beta1-selective blocker, decreased HMG CoA reductase activity and increased LDL receptor activity, but metoprolol had no major effect. We speculate that the discrepancy between betaxolol and metoprolol in the effect on HMG CoA reductase and the LDL receptor might be due to the difference of the extent of beta1-selectivity. We conclude that beta1-selective blockers are antihypertensive agents potentially valuable in the prevention of atherosclerosis.

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Section: Discussionmentioning

confidence: 99%

Effects of beta-blockers on HMG CoA reductase and LDL receptor activity in cultured human skin fibroblasts

Yoshida

Suzukawa

Ishikawa

et al. 1996

Cardiovasc Drug Ther

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“…A more rational approach would be to lower blood pressure by correcting the damaged hemodynamic mechanism, i.e., by vasodilation [Zanchetti, 1987]. A new generation of β-blockers with a variety of additional characteristics is now emerging; the most interesting of these are β-blockers with vasodilating activity [Hampton, 1994;McAreavey et al, 1991;Prichard, 1991], achieved by a variety of mechanisms including α-receptor blockade, β 2 -agonism, and a dilator action independent of the α-and β-receptors. Such β-blockers reduce total peripheral resistance and bring about less suppression of cardiac output in exercise [Lund-Johansen, 1992].…”

Section: Introductionmentioning

confidence: 98%

Eugenolol: An eugenol-derived ?-adrenoceptor blocker with partial ?2-agonist and calcium mobilization inhibition associated vasorelaxant activities

Chen

Huang

et al. 1997

Drug Dev. Res.

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“…adrenoceptors, intrinsic sympathomi metic activity (ISA), membrane-stabilizing ac tivity, and lipid versus water solubility [4,5], A new generation of p blockers with a vari ety of additional characteristics are now emerging. The most interesting of these are (3 blockers with vasodilating activity, achieved by a variety of mechanisms including a-adrenoceptor blockade, P-adrenoceptor agonism, and a dilator action independent of the a and p receptors [6][7][8], Such p blockers reduce total peripheral resistance and bring about less sup pression of cardiac output in exercise [9], For example, celiprolol is a p blocker character ized by selective blockade of Pi receptors and partial agonist activity on P2 receptor [ 10], Carvcdilol and labetalol are P-adrenoceptor antagonists which cause peripheral vasodila tion primarily via aj adrenergic blockade [ 10,11 ]. Regarding ISA, a nonselective p-adrenoceptor blocker such as vanidilol with partial p2-agonist activity has never been described.…”

Section: Introductionmentioning

confidence: 99%

Vanidilol: A Vanilloid-Type Vasorelaxant and Ocular Hypotensive Beta-Adrenoceptor Blocker with Partial Beta-2-Agonist Activity

Sheu

Wu²,

Ho³

et al. 1997

Pharmacology

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Vanidilol, [4’-(2-hydroxy-3-(tert-butylamino)propoxy)-3’-methoxyphenyl]-benzaldehyde, newly synthesized from vanillin, is a vanilloid-type β-adrenoceptor blocker. The β-adrenoceptor-blocking properties of vanidilol were studied both in vivo and in vitro. Intravenous injection of vanidilol (1.0, 3.0, 5.0 mg/kg) in anesthetized Wistar rats produced a decrease in blood pressure and a dose-dependent bradycardia response. Vanidilol inhibited the tachycardia effects induced by (-)isoproterenol, but had no blocking effect on the arterial pressor responses induced by phenylephrine. In isolated guinea-pig tissues, vanidilol attenuated the (–)isoproterenol-induced positive chronotropic and inotropic effects of the atria and trachea relaxation responses in a concentration-dependent manner. The parallel shift to the right of the concentration-response curve of (–)isoproterenol suggested that the agent was a β-adrenoceptor competitive antagonist. The apparent pA2 values for vanidilol on the right atria, left atria and trachea were 7.67 ± 0.03, 7.89 ± 1.02 and 7.66 ± 0.15, respectively, denoting that vanidilol was a nonselective β-blocker. The intrinsic sympathomimetic activity of vanidilol and propranolol was determined on isolated atria and trachea from reserpinized guinea pigs. Propranolol caused significantly negative inotropic and chronotropic effects at 10^–6 mol/l or above, whereas vanidilol possessed less cardiodepressant activities than propranolol. In reserpinized tracheal strips, vanidilol produced dose-dependent relaxant responses, but propranolol was ineffective. Preincubating the preparations with ICI 118,551 (0.1–10 nmol/l), a β₂-adrenoceptor antagonist, significantly shifted the concentration-relaxation curves of vanidilol to a region of higher concentrations. In isolated guinea-pig thoracic aorta, vanidilol (0.1–10 µmol/l) inhibited the phenylephrine (10^–5 mol/l)-induced tonic contraction in vascular smooth muscle which was related to the block of calcium influx. In 20% saline-perfused rabbits, vanidilol showed a marked delay in intraocular pressure recovery, demonstrating an ocular hypotensive action. Binding characteristics of vanidilol and propranolol were evaluated in [³H]dihydroalprenolol binding to porcine ventricular membranes. Vanidilol was less potent than propranolol in competing for the β-adrenoceptor-binding sites. On the other hand, vanidilol had a high hydrophilicity in comparison with propranolol. In conclusion, vanidilol exhibited nonselective β-adrenoceptor blocking, vasorelaxant and ocular hypotensive activities, but was devoid of α-adrenoceptor blocking and β₁-agonist activity. Partial β₂-adrenoceptor agonist activity and inhibitory activity on calcium influx may share in the vasorelaxant activity.

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Newer beta blockers and the treatment of hypertension

Cited by 10 publications

References 115 publications

Effects of beta-blockers on HMG CoA reductase and LDL receptor activity in cultured human skin fibroblasts

Effects of beta-blockers on HMG CoA reductase and LDL receptor activity in cultured human skin fibroblasts

Eugenolol: An eugenol-derived ?-adrenoceptor blocker with partial ?2-agonist and calcium mobilization inhibition associated vasorelaxant activities

Vanidilol: A Vanilloid-Type Vasorelaxant and Ocular Hypotensive Beta-Adrenoceptor Blocker with Partial Beta-2-Agonist Activity

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