Department of Pharmacology, Faculty of Pharmacy, Ankara University, Ankara, Turkey.
Department of Pharmacology, Johannes Gutenberg University, Mainz, Germany.
Br J Pharmacol. 2019 Jul;176(14):2482-2495. doi: 10.1111/bph.14635. Epub 2019 Apr 22.
As β -adrenoceptors were first demonstrated to be expressed in adipose tissue they have received much attention for their metabolic effects in obesity and diabetes. After the existence of this subtype had been suggested to be present in the heart, studies focused on its role in cardiac function. While the presence and functional role of β -adrenoceptors in the heart has not uniformly been detected, there is a broad consensus that they become up-regulated in pathological conditions associated with increased sympathetic activity such as heart failure and diabetes. When detected, the β -adrenceptor has been demonstrated to mediate negative inotropic effects in an inhibitory G protein-dependent manner through the NO-cGMP-PKG signalling pathway. Whether these negative inotropic effects provide protection from the adverse effects induced by overstimulation of β /β -adrenoceptors or in themselves are potentially harmful is controversial, but ongoing clinical studies in patients with congestive heart failure are testing the hypothesis that β -adrenceptor agonism has a beneficial effect. LINKED ARTICLES: This article is part of a themed section on Adrenoceptors-New Roles for Old Players. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v176.14/issuetoc.
β -肾上腺素受体最初在脂肪组织中被证实表达,因此它们在肥胖和糖尿病中的代谢作用受到了广泛关注。在该亚型存在于心脏中的假设被提出后,研究集中在其在心脏功能中的作用。虽然β -肾上腺素受体在心脏中的存在和功能作用尚未被一致检测到,但人们普遍认为,它们在与交感神经活动增加相关的病理状态下(如心力衰竭和糖尿病)会被上调。当被检测到时,β -肾上腺素受体已被证明通过 NO-cGMP-PKG 信号通路以抑制性 G 蛋白依赖的方式介导负性变力作用。这些负性变力作用是否提供了对β /β -肾上腺素受体过度刺激引起的不良反应的保护作用,或者本身是否具有潜在的危害性,这是有争议的,但正在进行的心力衰竭患者的临床研究正在检验β -肾上腺素受体激动剂具有有益作用的假设。相关文章:本文是关于肾上腺素能受体-旧角色的新角色的专题部分的一部分。要查看该部分中的其他文章,请访问 http://onlinelibrary.wiley.com/doi/10.1111/bph.v176.14/issuetoc/。