高浓度的普萘洛尔可抑制离体猪冠状动脉的收缩。

Contraction of isolated porcine coronary arteries is inhibited by high concentrations of propranolol.

作者信息

Carey E L, Robertson D, Wells J N, Robertson R M

机构信息

Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, USA.

出版信息

Angiology. 1995 Jun;46(6):453-60. doi: 10.1177/000331979504600601.

DOI:10.1177/000331979504600601

PMID:7785786

Abstract

Isometric tension responses of isolated porcine coronary artery rings were studied in the presence of concentrations of propranolol higher than those necessary to block effects mediated by beta-adrenergic receptors. Propranolol (50-300 microM) inhibited contractions induced by 30 mM KCl and by histamine, norepinephrine, and acetylcholine in a concentration-dependent, noncompetitive fashion. The (+) propranolol isomer and the racemic mixture were equipotent inhibitors of contraction. Propranolol inhibition was partly reversed by increased extracellular Ca++. These effects of propranolol thus appeared to be independent of beta-blockade and could be relevant to some of the drug's observed but still unexplained in vivo actions.

摘要

在高于阻断β-肾上腺素能受体介导作用所需浓度的普萘洛尔存在下，研究了离体猪冠状动脉环的等长张力反应。普萘洛尔（50 - 300微摩尔）以浓度依赖性、非竞争性方式抑制由30毫摩尔氯化钾以及组胺、去甲肾上腺素和乙酰胆碱诱导的收缩。（+）普萘洛尔异构体和外消旋混合物是等效的收缩抑制剂。增加细胞外钙离子浓度可部分逆转普萘洛尔的抑制作用。因此，普萘洛尔的这些作用似乎与β受体阻断无关，可能与该药物一些已观察到但仍无法解释的体内作用有关。