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药物负荷试验的未来:选择性A2A腺苷受体激动剂

The future of pharmacologic stress: selective A2A adenosine receptor agonists.

作者信息

Cerqueira Manuel D

机构信息

Division of Cardiology, Georgetown University Medical Center, Washington, DC 20007-2197, USA.

出版信息

Am J Cardiol. 2004 Jul 22;94(2A):33D-40D; discussion 40D-42D. doi: 10.1016/j.amjcard.2004.04.017.

Abstract

Adenosine and dipyridamole, the currently available vasodilators for myocardial perfusion imaging, produce hyperemic coronary flow by stimulating A(2A) adenosine receptors on arteriolar vascular smooth muscle cells. However, both vasodilators nonselectively activate A(1), A(2B), and A(3) adenosine receptors, which contributes to common undesirable effects. In the development of a novel pharmacologic stress agent, more selective agonism of the A(2A) receptor subtype would be desirable. Currently, 2 selective A(2A) adenosine receptor agonists are being evaluated in phase 3 studies as pharmacologic stress agents. The highly selective, potent, low-affinity A(2A) adenosine agonist regadenoson (also known as CVT-3146) holds significant potential as a pharmacologic stress agent, based on available results from experimental and clinical trials. Regadenoson produces maximal hyperemia quickly and maintains it for an optimal duration that is practical for radionuclide myocardial perfusion imaging. Regadenoson's simple rapid bolus administration and short duration of hyperemic effect point to an advantage of enhanced control for the clinician.

摘要

腺苷和双嘧达莫是目前用于心肌灌注成像的血管扩张剂,它们通过刺激小动脉血管平滑肌细胞上的A(2A)腺苷受体产生充血性冠状动脉血流。然而,这两种血管扩张剂都会非选择性地激活A(1)、A(2B)和A(3)腺苷受体,这会导致常见的不良影响。在开发新型药理应激剂时,更具选择性地激动A(2A)受体亚型是可取的。目前,有2种选择性A(2A)腺苷受体激动剂正在3期研究中作为药理应激剂进行评估。基于实验和临床试验的现有结果,高选择性、强效、低亲和力的A(2A)腺苷激动剂瑞加腺苷(也称为CVT-3146)作为药理应激剂具有巨大潜力。瑞加腺苷能迅速产生最大充血,并将其维持在对放射性核素心肌灌注成像实用的最佳持续时间。瑞加腺苷简单快速的推注给药方式和充血效应的短持续时间表明对临床医生而言具有增强控制的优势。

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