Departamento de Farmacología, Facultad de Farmacia, Universitat de València Valencia, Spain.
Autonomic Physiology Unit, School of Life Sciences, College of Medical, Veterinary and Life Sciences, University of Glasgow Glasgow, U.K.
Pharmacol Res Perspect. 2013 Oct;1(1):e00001. doi: 10.1002/prp2.1. Epub 2013 Aug 28.
The objective of this study was to determine whether the different time-course characteristics of α1-adrenoceptor-mediated contraction in arteries can be related to the subtypes involved. Contractile responses to noradrenaline (NA) were compared with inositol phosphate accumulation and extracellular signal-regulated kinase (ERK)1/2 phosphorylation after α1-agonist stimuli in the same vessels in the presence or absence of α1-antagonists in rat or in α1-subtype knockout (KO) mice. Aorta, where α1D-AR is the main functional subtype, had higher sensitivity to NA (in respect of inositol phosphate [IP], pERK1/2, and contractile response) than tail artery, where the α1A-adrenoceptor subtype is predominant. Furthermore, the contraction in aorta exhibited a slower decay after agonist removal and this was consistent in all strains harboring α1D-adrenoceptors (from rat, α1B-KO, and wild-type [WT] mice) but was not observed in the absence of the α1D-adrenoceptor signal (α1D-adrenoceptor blocked rat aorta or aorta from α1D-KO). IP formation paralleled α1-adrenoceptor-mediated contraction (agonist present or postagonist) in aorta and tail artery. High sensitivity to agonist and persistence of response after agonist removal is a property of α1D-adrenoceptors. Therefore, the preponderance of this subtype in noninnervated conductance arteries such as aorta allows responsiveness to circulating catecholamines and prevents abrupt changes in vessel caliber when the stimulus fluctuates. Conversely, in innervated distributing arteries, high local concentrations of NA are required to activate α1A-adrenoceptors for a response that is rapid but short lived allowing fine adjustment of the contractile tone by perivascular sympathetic nerves.
本研究旨在确定 α1-肾上腺素受体介导的动脉收缩的不同时程特征是否与涉及的亚型有关。在存在或不存在 α1-拮抗剂的情况下,比较了在大鼠或 α1 亚型敲除(KO)小鼠的相同血管中,去甲肾上腺素(NA)引起的收缩与肌醇磷酸盐积累和细胞外信号调节激酶(ERK)1/2 磷酸化。与尾动脉相比,主动脉中 α1D-AR 是主要的功能性亚型,对 NA(在肌醇磷酸盐[IP]、pERK1/2 和收缩反应方面)的敏感性更高,而尾动脉中 α1A-肾上腺素受体亚型占主导地位。此外,在激动剂去除后,主动脉的收缩衰减较慢,这在所有含有 α1D-肾上腺素受体的品系中是一致的(从大鼠、α1B-KO 和野生型[WT]小鼠),但在缺乏 α1D-肾上腺素受体信号的情况下没有观察到(α1D-肾上腺素受体阻断的大鼠主动脉或 α1D-KO 主动脉)。IP 的形成与主动脉和尾动脉中的 α1-肾上腺素受体介导的收缩(存在激动剂或激动剂后)平行。对激动剂的高敏感性和激动剂去除后反应的持续存在是 α1D-肾上腺素受体的特性。因此,这种亚型在非神经支配的传导性动脉(如主动脉)中的优势允许对循环儿茶酚胺的反应,并防止当刺激波动时血管口径的突然变化。相反,在有神经支配的分布性动脉中,需要高浓度的局部 NA 来激活 α1A-肾上腺素受体,以产生快速但短暂的反应,允许通过血管周围交感神经对收缩张力进行精细调节。