从 "禁忌症 "到 "一线治疗"--当前超越典型β受体信号转导的机理认识

IF 4 3区 医学 Q1 PHARMACOLOGY & PHARMACY
Theresa Brand , Ann-Kathrin Lukannek , Valérie Jahns , Roland Jahns , Kristina Lorenz
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引用次数: 0

摘要

β 受体阻滞剂是治疗心血管疾病的坚实支柱。然而,它们在某些适应症的疗效和副作用方面却备受争议。尽管有多达 20 种获得许可的化合物,但只有 4 种用于心力衰竭(HF)治疗。在受体层面,有几个关键特征似乎会影响临床结果:亚型选择性、拮抗与(反向/偏向)激动特性,尤其是辅助能力。在分子水平上,不同的新型信号传导模式正在被确定,对炎症、新陈代谢和氧化应激等心脏外影响也得到了强调。本综述讨论了在高血压治疗和并发症方面需要考虑的各种众所周知的和新发现的特性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
From “contraindicated” to “first line” – Current mechanistic insights beyond canonical β-receptor signaling

β-blockers are a solid pillar in the treatment of cardiovascular diseases. However, they are highly discussed regarding effectiveness for certain indications and side-effects. Even though there are up to 20 licensed compounds, only four are used for heart failure (HF) therapy. On the receptor level several key characteristics seem to influence the clinical outcome: subtype selectivity, antagonistic vs (inverse/biased) agonistic properties and -in particular- ancillary capacities. On a molecular level, divergent and novel signaling patterns are being identified and extra-cardiac effects on e.g. inflammation, metabolism and oxidative stress are highlighted. This review discusses different well-known and newly discovered characteristics that need to be considered for HF therapy and in the context of co-morbidities.

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来源期刊
CiteScore
8.80
自引率
2.50%
发文量
131
审稿时长
4-8 weeks
期刊介绍: Current Opinion in Pharmacology (COPHAR) publishes authoritative, comprehensive, and systematic reviews. COPHAR helps specialists keep up to date with a clear and readable synthesis on current advances in pharmacology and drug discovery. Expert authors annotate the most interesting papers from the expanding volume of information published today, saving valuable time and giving the reader insight on areas of importance.
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