生物活性

• 描述Regadenoson is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor^[3]. Regadenoson binds to the A 2A receptor and stimulates adenylate cyclase, resulting in increased cAMP, which phosphorylates protein kinase A thereby opening the ATP-dependant potassium channels leading to hyperpolarization in the coronary vascular smooth muscle. After a single bolus dose of regadenoson 400 μg, a peak plasma concentration (C max) of 13.6 ng/mL is attained in 1-4 min, with a terminal half-life of 2 h. It has a quick onset, short duration sufficient enough for hyperemic response, with comparable efficacy to adenosine, but with fewer side-effects^[4]. Infusion of regadenoson achieves maximum coronary hyperemia that is equivalent to adenosine. Regadenoson selectively causes vasodilation of the coronary circulation, whereas effects on systemic blood pressure are only mild^[5].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT03338504	-	-	Recruiting	November 1, 2020	United Kingdom ... more >> Centre for Cardiovascular Science Recruiting Edinburgh, United Kingdom, EH16 4SB Contact: Andrew R Chapman, MBChB    01313153987    a.r.chapman@ed.ac.uk    Principal Investigator: Andrew R Chapman, MD          Sub-Investigator: Nicholas L MIlls, MD PhD          Sub-Investigator: David E Newby, MD PhD Collapse <<
  NCT03354273	Coronary Artery Disease (CAD)	Phase 3	Recruiting	August 2020	United States, California ... more >> Keck Hospital of USC Recruiting Los Angeles, California, United States, 90033 VA Greater Los Angeles Health Care System Recruiting Los Angeles, California, United States, 90073 United States, Delaware Alfieri Cardiology Recruiting Newark, Delaware, United States, 19713 Cardiology Physicians PA/Red Clay Research LLC Recruiting Newark, Delaware, United States, 19713 United States, Missouri Saint Luke's Hospital of Kansas City Recruiting Kansas City, Missouri, United States, 64111 United States, Ohio University of Cincinnati Medical Center Recruiting Cincinnati, Ohio, United States, 45219 United States, Pennsylvania Berks Cardiologists, LTD Recruiting Wyomissing, Pennsylvania, United States, 19610 United States, Tennessee Wellmont CVA Heart Institute Recruiting Kingsport, Tennessee, United States, 37660 University of Tennessee Medical Center Recruiting Knoxville, Tennessee, United States, 37920 Vanderbilt University Medical Center Recruiting Nashville, Tennessee, United States, 37232 United States, Texas West Houston Area Clinical Trial Consultants, LLC Recruiting Katy, Texas, United States, 77493 Northwest Houston Clinical Research, PLLC Recruiting Tomball, Texas, United States, 77375 United States, West Virginia West Virginia University Hospital Recruiting Morgantown, West Virginia, United States, 26506 Finland Turku University Hospital Recruiting Turku, Finland, FI-20520 Collapse <<
  NCT01370265	Coronary Artery Disease	Not Applicable	Completed	-	United States, Minnesota ... more >> Mayo Clinic Rochester, Minnesota, United States, 55905 Collapse <<

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• 参考文献

• [1] Pape M, Zacho HD, et al. Safety and tolerability of regadenoson for myocardial perfusion imaging - first Danish experience. Scand Cardiovasc J. 2016 Jun;50(3):180-6.

  [2] Zhao G, Messina E, et al. Caffeine attenuates the duration of coronary vasodilation and changes in hemodynamics induced by regadenoson (CVT-3146), a novel adenosine A2A receptor agonist. J Cardiovasc Pharmacol. 2007 Jun;49(6):369-75.

  [3] Golzar Y, Doukky R. Regadenoson use in patients with chronic obstructive pulmonary disease: the state of current knowledge. Int J Chron Obstruct Pulmon Dis. 2014 Jan 22;9:129-37

  [4] Bengalorkar GM, Bhuvana K, Sarala N, Kumar TN. Regadenoson. J Postgrad Med. 2012 Apr-Jun;58(2):140-6

  [5] Buhr C, Gössl M, Erbel R, Eggebrecht H. Regadenoson in the detection of coronary artery disease. Vasc Health Risk Manag. 2008;4(2):337-40

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