Document Detail

Regadenoson, a selective A2A adenosine receptor agonist, causes dose-dependent increases in coronary blood flow velocity in humans.
MedLine Citation:
PMID:  17679059     Owner:  NLM     Status:  MEDLINE    
BACKGROUND: Regadenoson is a selective A2A adenosine receptor agonist and vasodilator used to increase the heterogeneity of distribution of coronary blood flow during myocardial perfusion imaging. This study characterized the dose dependence of regadenoson-induced coronary hyperemia. METHODS AND RESULTS: An open-label, dose-escalation study of regadenoson (10-500 microg, rapid intravenous bolus) was performed in 34 subjects; in 4 additional subjects, the effect of aminophylline to reverse the response to regadenoson was determined. Intracoronary peak blood flow velocity in either the left anterior descending or left circumflex artery was measured by continuous Doppler signal recording, heart rate, central aortic blood pressure, and adverse effects were recorded. Regadenoson increased peak blood flow velocity by up to 3.4-fold in a dose-dependent manner. The mean duration of the increase in flow velocity of 2.5-fold or greater caused by 400 to 500 microg of regadenoson was 2.3 to 2.4 minutes. Regadenoson (400-500 microg) increased heart rate by up to 21 +/- 6 beats/min and decreased systolic blood pressure (-5 +/- 8 mm Hg to -24 +/- 16 mm Hg) and diastolic blood pressure (-8 +/- 4 mm Hg to -15 +/- 14 mm Hg). Aminophylline (100 mg) attenuated the increase in peak flow velocity but not tachycardia caused by 400 microg of regadenoson. CONCLUSION: The results of this study demonstrate the utility of regadenoson as a coronary vasodilator for myocardial perfusion imaging.
Hsiao D Lieu; John C Shryock; Gregory O von Mering; Toufigh Gordi; Brent Blackburn; Ann W Olmsted; Luiz Belardinelli; Richard A Kerensky
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Publication Detail:
Type:  Clinical Trial; Clinical Trial, Phase II; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of nuclear cardiology : official publication of the American Society of Nuclear Cardiology     Volume:  14     ISSN:  1532-6551     ISO Abbreviation:  J Nucl Cardiol     Publication Date:  2007 Jul 
Date Detail:
Created Date:  2007-08-06     Completed Date:  2007-08-30     Revised Date:  2010-04-12    
Medline Journal Info:
Nlm Unique ID:  9423534     Medline TA:  J Nucl Cardiol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  514-20     Citation Subset:  IM    
Portola Pharmaceuticals, South San Francisco, Calif, USA.
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MeSH Terms
Aminophylline / pharmacology
Blood Flow Velocity / drug effects*
Coronary Circulation / drug effects*
Dose-Response Relationship, Drug
Middle Aged
Purines / pharmacology*
Pyrazoles / pharmacology*
Receptor, Adenosine A2A / agonists*
Tomography, Emission-Computed, Single-Photon / methods
Ultrasonography, Doppler
Vasodilator Agents / pharmacology
Reg. No./Substance:
0/Purines; 0/Pyrazoles; 0/Receptor, Adenosine A2A; 0/Vasodilator Agents; 0/regadenoson; 317-34-0/Aminophylline

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