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药物和疾病引起的人类心脏β1和β2肾上腺素能受体的变化。

Drug- and disease-induced changes of human cardiac beta 1- and beta 2-adrenoceptors.

作者信息

Brodde O E, Zerkowski H R, Borst H G, Maier W, Michel M C

机构信息

Biochem. Forschungslabor, Universität Essen, F.R.G.

出版信息

Eur Heart J. 1989 Jun;10 Suppl B:38-44. doi: 10.1093/eurheartj/10.suppl_b.38.

DOI:10.1093/eurheartj/10.suppl_b.38
PMID:2553410
Abstract

Cardiac beta-adrenoceptor density and subtype distribution has been determined in different kinds of heart failure. A decrease in cardiac beta-adrenoceptor function appears to be a general phenomenon in all kinds of heart failure. However, cardiac beta 1- and beta 2-adrenoceptors seem to be differentially affected in different kinds of heart failure: while in end-stage idiopathic dilated cardiomyopathy the diminished cardiac beta-adrenoceptor function is due to a selective loss in beta 1-adrenoceptors, in mitral valve disease, tetralogy of Fallot and end-stage ischaemic cardiomyopathy it is characterized by a concomitant reduction in beta 1- and beta 2-adrenoceptors. Chronic treatment of heart failure patients with beta-adrenoceptor antagonists leads to an up-regulation of cardiac beta-adrenoceptors, but in a subtype-selective fashion: beta 1-selective antagonists increase only cardiac beta 1-adrenoceptors, whereas non-selective antagonists increase both beta 1- and beta 2-adrenoceptors. Such a (subtype-selective) 'recovery' of cardiac beta-adrenoceptors may be one reason for the beneficial effects of low-dose beta-adrenoceptor antagonist treatment in patients with severe heart failure.

摘要

已对不同类型心力衰竭患者心脏β肾上腺素能受体的密度和亚型分布进行了测定。心脏β肾上腺素能受体功能下降似乎是各类心力衰竭的普遍现象。然而,心脏β1和β2肾上腺素能受体在不同类型心力衰竭中似乎受到不同影响:在终末期特发性扩张型心肌病中,心脏β肾上腺素能受体功能降低是由于β1肾上腺素能受体选择性丧失所致;而在二尖瓣疾病、法洛四联症和终末期缺血性心肌病中,其特征是β1和β2肾上腺素能受体同时减少。用β肾上腺素能受体拮抗剂对心力衰竭患者进行长期治疗可导致心脏β肾上腺素能受体上调,但具有亚型选择性:β1选择性拮抗剂仅增加心脏β1肾上腺素能受体,而非选择性拮抗剂则增加β1和β2肾上腺素能受体。心脏β肾上腺素能受体的这种(亚型选择性)“恢复”可能是低剂量β肾上腺素能受体拮抗剂治疗重症心力衰竭患者产生有益效果的原因之一。

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