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普瑞特罗治疗后年轻健康男性静息及运动状态下的血流动力学和腿部肌肉代谢

Hemodynamics and leg muscle metabolism at rest and during exercise in young healthy men after prenalterol.

作者信息

Dahlström U, Atterhög J H, Jorfeldt L

出版信息

Clin Pharmacol Ther. 1983 Jun;33(6):701-9. doi: 10.1038/clpt.1983.96.

Abstract

In eight young healthy men the effects of short-term treatment with prenalterol, a new beta-adrenergic agonist, on peripheral hemodynamics and leg muscle metabolism were studied at rest and during exercise at a moderate and a heavy workload. At rest prenalterol treatment significantly increased pulmonary oxygen uptake, heart rate, rate pressure product, and leg blood flow and decreased leg arteriovenous oxygen content difference. During exercise fewer hemodynamic effects of prenalterol were observed. At the moderate workload there was a slight increase in heart rate, but at the heavy workload heart rate fell. Prenalterol raised the arterial concentrations of free fatty acids and glycerol at rest by 70% and 40%, but during exercise these alterations were not present. The plasma levels of epinephrine and dopamine in subjects at rest decreased significantly during influence of prenalterol, but these differences were also abolished during exercise. The leg exchange of metabolites and the concentrations of endogenous muscle metabolites were not influenced by prenalterol, although the lactate concentrations in muscle tended to be lower at rest and during exercise. The results at rest demonstrate that prenalterol in this situation acts predominantly as a stimulator of beta 1-adrenoceptors. During heavy exercise, however, when the endogenous sympathetic tone is high, the beta-stimulating effects are no longer overt and instead reduced heart rate indicates a blocking effect on beta-adrenoceptors. The hemodynamic and metabolic results are concordant with the hypothesis that prenalterol acts as a partial beta-receptor agonist.

摘要

在八名年轻健康男性中,研究了新型β-肾上腺素能激动剂普瑞特罗短期治疗对静息状态以及中等和重度运动负荷下外周血流动力学和腿部肌肉代谢的影响。静息状态下,普瑞特罗治疗显著增加了肺摄氧量、心率、心率血压乘积和腿部血流量,并降低了腿部动静脉氧含量差。运动期间,观察到普瑞特罗的血流动力学效应较少。在中等运动负荷下,心率略有增加,但在重度运动负荷下心率下降。普瑞特罗使静息状态下的游离脂肪酸和甘油动脉浓度分别升高了70%和40%,但运动期间未出现这些变化。静息状态下受试者的肾上腺素和多巴胺血浆水平在普瑞特罗影响下显著降低,但运动期间这些差异也消失了。尽管肌肉中的乳酸浓度在静息和运动期间趋于降低,但腿部代谢物交换和内源性肌肉代谢物浓度不受普瑞特罗影响。静息状态下的结果表明,在这种情况下普瑞特罗主要作为β1-肾上腺素能受体的刺激剂起作用。然而,在重度运动期间,当内源性交感神经张力较高时,β刺激作用不再明显,相反,心率降低表明对β-肾上腺素能受体有阻断作用。血流动力学和代谢结果与普瑞特罗作为部分β受体激动剂的假说一致。

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