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腺苷 A1“偏倚”受体是否是肺动脉高压治疗的有价值靶点?

Is the adenosine A 'biased' receptor a valuable target for the treatment of pulmonary arterial hypertension?

机构信息

Laboratório de Farmacologia e Neurobiologia, Centro de Investigação Farmacológica e Inovação Medicamentosa (MedInUP), Instituto de Ciências Biomédicas Abel Salazar, Universidade do Porto (ICBAS-UP), Porto, Portugal.

Laboratório de Farmacologia e Neurobiologia, Centro de Investigação Farmacológica e Inovação Medicamentosa (MedInUP), Instituto de Ciências Biomédicas Abel Salazar, Universidade do Porto (ICBAS-UP), Porto, Portugal.

出版信息

Drug Discov Today. 2018 Jun;23(6):1285-1292. doi: 10.1016/j.drudis.2018.05.005. Epub 2018 May 7.

DOI:10.1016/j.drudis.2018.05.005
PMID:29747005
Abstract

Pulmonary arterial hypertension (PAH) is a maladaptive disorder characterized by increased pulmonary vascular resistance leading to right ventricular failure and death. Adenosine released by injured tissues, such as the lung and heart, influences tissue remodeling through the activation of adenosine receptors. Evidence regarding activation of the low-affinity AAR by adenosine points towards pivotal roles of this receptor in processes associated with both acute and chronic lung diseases. Conflicting results exist concerning the beneficial or detrimental roles of the A 'biased' receptor in right ventricular failure secondary to PAH. In this review, we discuss the pros and cons of manipulating AARs as a putative therapeutic target in PAH.

摘要

肺动脉高压(PAH)是一种适应性失调疾病,其特征是肺血管阻力增加,导致右心室衰竭和死亡。受损组织(如肺和心脏)释放的腺苷通过激活腺苷受体影响组织重塑。关于腺苷激活低亲和力 AAR 的证据表明,该受体在与急性和慢性肺部疾病相关的过程中起着关键作用。关于 A '偏向'受体在 PAH 继发右心室衰竭中的有益或有害作用存在相互矛盾的结果。在这篇综述中,我们讨论了操纵 AAR 作为 PAH 潜在治疗靶点的利弊。

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