Journal of Nuclear Cardiology

, Volume 14, Issue 4, pp 514–520 | Cite as

Regadenoson, a selective A2A adenosine receptor agonist, causes dose-dependent increases in coronary blood flow velocity in humans

  • Hsiao D. Lieu
  • John C. Shryock
  • Gregory O. von Mering
  • Toufigh Gordi
  • Brent Blackburn
  • Ann W. Olmsted
  • Luiz Belardinelli
  • Richard A. Kerensky
Original Articles



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 (10–500μg, 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 μg of regadenoson was 2.3 to 2.4 minutes. Regadenoson (400–500 μg) 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 μg of regadenoson.


The results of this study demonstrate the utility of regadenoson as a coronary vasodilator for myocardial perfusion imaging.

Key Words

Regadenoson coronary flow velocity myocardial perfusion imaging A2A adenosine Doppler pharmacologic stress agent 


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  1. 1.
    Nuclear cardiac imaging. Principles and applications, 3rd ed. New York: Oxford University Press; 2003.Google Scholar
  2. 2.
    Verani MS. Pharmacologic stress testing and other alternative techniques in the diagnosis of coronary artery disease. In: Iskandrian AE, Verani MS, editors. Nuclear cardiac imaging. Principles and applications. 3rd ed. New York: Oxford University Press; 2003, p. 164–89.Google Scholar
  3. 3.
    Gao Z, Li Z, Baker SP, Lasley RD, Meyer S, Elzein E, et al. Novel short-acting A2A adenosine receptor agonists for coronary vasodilation: inverse relationship between affinity and duration of action of A2A agonists. J Pharmacol Exp Ther 2001;298:209–18.PubMedGoogle Scholar
  4. 4.
    Cerqueira MD. The future of pharmacologic stress: selective A2A adenosine receptor agonists. Am J Cardiol 2004;94(Suppl):33D-42D.PubMedCrossRefGoogle Scholar
  5. 5.
    Hendel RC, Bateman TM, Cerqueira MD, Iskandrian AE, Leppo JA, Blackburn B, et al. Initial clinical experience with regadenoson, a novel selective A2A agonist for pharmacologic stress single-photon emission computed tomography myocardial perfusion imaging. J Am Coll Cardiol 2005;46:2069–75.PubMedCrossRefGoogle Scholar
  6. 6.
    Trochu J-N, Zhao G, Post H, Xu X, Belardinelli L, Belloni FL, et al. Selective A2A adenosine receptor agonist as a coronary vasodilator in conscious dogs: potential for use in myocardial perfusion imaging. J Cardiovasc Pharmacol 2003;41:132–9.PubMedCrossRefGoogle Scholar
  7. 7.
    Skillings JH, Wolfe DA. Distribution-free tests for ordered alternatives in a randomized block design. J Am Stat Assoc 1978;73:427–31.CrossRefGoogle Scholar
  8. 8.
    Dhalla AK, Wong MY, Wang WQ, Biaggioni I, Belardinelli L. Tachycardia caused by A2A adenosine receptor agonists is mediated by direct sympathoexcitation in awake rats. J Pharmacol Exp Ther 2006;316:695–702.PubMedCrossRefGoogle Scholar
  9. 9.
    Crea F, Gaspardone A, Araujo L, DaSilva R, Kaski JC, Davies G. et al. Effects of aminophylline on cardiac function and regional myocardial perfusion: implications regarding its antiischemic action. Am Heart J 1994;127:817–24.PubMedCrossRefGoogle Scholar
  10. 10.
    Wesley RC, Lerman BB, DiMarco JP, Berne RM, Belardinelli L. Mechanism of atropine-resistant atrioventricular block during inferior myocardial infarction: possible role of adenosine. J Am Coll Cardiol 1986;8:1232–4.PubMedCrossRefGoogle Scholar
  11. 11.
    Lee J, Heo J, Ogilby JD, Cave V, Iskandrian B, Iskandrian AS. Atrioventricular block during adenosine thallium imaging. Am Heart J 1992;123:1569–74.PubMedCrossRefGoogle Scholar
  12. 12.
    Belardinelli L, Fenton RA, West A, Linden J, Althaus JS, Berne RM. Extracellular action of adenosine and the antagonism by aminophylline on the atrioventricular conduction of isolated perfused guinea pig and rat hearts Circ Res 1982;51:569–79.PubMedGoogle Scholar

Copyright information

© American Society of Nuclear Cardiology 2007

Authors and Affiliations

  • Hsiao D. Lieu
    • 1
  • John C. Shryock
    • 2
  • Gregory O. von Mering
    • 3
  • Toufigh Gordi
    • 4
  • Brent Blackburn
    • 2
  • Ann W. Olmsted
    • 2
  • Luiz Belardinelli
    • 2
  • Richard A. Kerensky
    • 5
  1. 1.Portola PharmaceuticalsSouth San Francisco
  2. 2.CV TherapeuticsPalo Alto
  3. 3.Division of Cardiology, College of MedicineUniversity of FloridaGainesville
  4. 4.DepomedMenlo Park
  5. 5.Archbold Medical CenterThomasville

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