RegadenosonHighly selective and low affinity A2A adenosine agonist CAS# 313348-27-5 |
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| Cas No. | 313348-27-5 | SDF | Download SDF |
| PubChem ID | 219024 | Appearance | Powder |
| Formula | C15H18N8O5 | M.Wt | 390.35 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | CVT-3146 | ||
| Solubility | DMSO : 50 mg/mL (128.09 mM; Need ultrasonic) | ||
| Chemical Name | 1-[6-amino-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]purin-2-yl]-N-methylpyrazole-4-carboxamide | ||
| SMILES | CNC(=O)C1=CN(N=C1)C2=NC3=C(C(=N2)N)N=CN3C4C(C(C(O4)CO)O)O | ||
| Standard InChIKey | LZPZPHGJDAGEJZ-AKAIJSEGSA-N | ||
| Standard InChI | InChI=1S/C15H18N8O5/c1-17-13(27)6-2-19-23(3-6)15-20-11(16)8-12(21-15)22(5-18-8)14-10(26)9(25)7(4-24)28-14/h2-3,5,7,9-10,14,24-26H,4H2,1H3,(H,17,27)(H2,16,20,21)/t7-,9-,10-,14-/m1/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Regadenoson is an A2A adenosine receptor agonist that is a coronary vasodilator that is commonly used in pharmacologic stress testing.
Target: A2A adenosine receptor
Regadenoson produces hyperemia quickly and maintains it for a duration that is useful for radionuclide myocardial perfusion imaging. The selective nature of the drug makes it preferable to other stress agents such as adenosine, which are less selective and therefore cause more side-effects.Regadenoson has a 2 to 3 minute biological half-life.[1] References: | |||||
Regadenoson Dilution Calculator
Regadenoson Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.5618 mL | 12.809 mL | 25.618 mL | 51.2361 mL | 64.0451 mL |
| 5 mM | 0.5124 mL | 2.5618 mL | 5.1236 mL | 10.2472 mL | 12.809 mL |
| 10 mM | 0.2562 mL | 1.2809 mL | 2.5618 mL | 5.1236 mL | 6.4045 mL |
| 50 mM | 0.0512 mL | 0.2562 mL | 0.5124 mL | 1.0247 mL | 1.2809 mL |
| 100 mM | 0.0256 mL | 0.1281 mL | 0.2562 mL | 0.5124 mL | 0.6405 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Description:
Ki: 1095 nM for A2A receptor
The adenosine A2A receptor is a G-protein-coupled receptor that has been extensively studied during the past few decades because it offers numerous possibilities for therapeutic applications. Regadenoson (CVT-3146) is a highly selective, potent, low affinity A2A adenosine agonist.
In vitro: Regadenoson was selective for the A2A adenosine receptor versus the A1, A2B, and A3 receptors in binding and functional studies. Regadenoson was also found to be a full and potent agonist to cause coronary vasodilation, a response that has a very large A2A receptor reserve [1].
In vivo: In a study of 10 conscious dogs, authors compared intravenously injected regadenoson to that of adenosine. Regadenoson caused a dose-dependent increase of coronary blood flow (CBF), whereas adenosine was less potent but produced equivalent hyperemia. Thus, authors concluded that regadenoson is a potent coronary vasodilator with a short duration of action, minimal and transient systemic hemodynamic effects, and ease of administration [1].
Clinical trial: Previous study investigated the magnitude and duration of the effect of regadenoson on CBF velocity in humans. Results demonstrated that regadenoson produced a dose-dependent increase in duration of CBF velocity augmentation. At all dose levels, regadenoson caused a rapid increase in CBF velocity that was near peak within 30 seconds of the bolus delivery. Regadenoson was generally well tolerated, and side effects at all doses were infrequent, mild, and self-limited [1].
Reference:
[1] Cerqueira MD. The future of pharmacologic stress: selective A2A adenosine receptor agonists. Am J Cardiol. 2004 Jul 22;94(2A):33D-40D; discussion 40D-42D.
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The significance of post-stress decrease in left ventricular ejection fraction in patients undergoing regadenoson stress gated SPECT myocardial perfusion imaging.[Pubmed:28181156]
J Nucl Cardiol. 2018 Aug;25(4):1313-1323.
BACKGROUND: The significance of post-stress decrease in left ventricular ejection fraction (LVEF) with Regadenoson stress gated SPECT (GSPECT) myocardial perfusion imaging (MPI) has not been studied. METHODS AND RESULTS: Consecutive patients who underwent rest/Regadenoson stress GSPECT-MPI followed by coronary angiography within 6 months were analyzed. Change in LVEF by GSPECT-MPI was calculated as stress LVEF minus rest LVEF; a significant decrease was tested at 5% and 10% thresholds. In a diagnostic cohort of 793 subjects, LVEF change was not predictive of severe/extensive coronary artery disease (area under the curve, 0.50; 95% confidence interval, 0.44-0.57; P = 0.946). There was no significant difference in the rates of severe/extensive coronary artery disease in patients with or without a decrease in LVEF, irrespective of MPI findings. In an outcome cohort of the 929 subjects followed for 30 +/- 16 months, post-Regadenoson stress decrease in LVEF was not associated with increased risk of the composite endpoint of cardiac death or myocardial infarction or in the risk of coronary revascularization. CONCLUSIONS: In patients selected to undergo coronary angiography following Regadenoson stress GSPECT-MPI, a decrease in LVEF after Regadenoson stress is not predictive of severe/extensive CAD or adverse clinical outcomes, irrespective of MPI findings.
The EXERRT trial: "EXErcise to Regadenoson in Recovery Trial": A phase 3b, open-label, parallel group, randomized, multicenter study to assess regadenoson administration following an inadequate exercise stress test as compared to regadenoson without exercise for myocardial perfusion imaging using a SPECT protocol.[Pubmed:28224449]
J Nucl Cardiol. 2017 Jun;24(3):788-802.
BACKGROUND: This study assessed the non-inferiority and safety of Regadenoson administration during recovery from inadequate exercise compared with administration without exercise. METHODS: Patients unable to achieve adequate exercise stress were randomized to Regadenoson 0.4 mg either during recovery (Ex-Reg) or 1 hour after inadequate exercise (Regadenoson) (MPI1). All patients also underwent non-exercise Regadenoson MPI 1-14 days later (MPI2). The number of segments with reversible perfusion defects (RPDs) detected using single photon emission computerized tomography imaging was categorized. The primary analysis evaluated the majority agreement rate between Ex-Reg and Regadenoson groups. RESULTS: 1,147 patients were randomized. The lower bound of the 95% confidence interval of the difference in agreement rates (-6%) was above the -7.5% non-inferiority margin, demonstrating non-inferiority of Ex-Reg to Regadenoson. Adverse events were numerically less with Ex-Reg (MPI1). In the Ex-Reg group, one patient developed an acute coronary syndrome and another had a myocardial infarction following Regadenoson after exercise. Upon review, both had electrocardiographic changes consistent with ischemia prior to Regadenoson. CONCLUSIONS: Administering Regadenoson during recovery from inadequate exercise results in comparable categorization of segments with RPDs and with careful monitoring appears to be well tolerated in patients without signs/symptoms of ischemia during exercise and recovery.
The effect of regadenoson on the integrity of the human blood-brain barrier, a pilot study.[Pubmed:28315063]
J Neurooncol. 2017 May;132(3):513-519.
Regadenoson is an FDA approved adenosine receptor agonist which increases blood-brain barrier (BBB) permeability in rodents. Regadenoson is used clinically for pharmacologic cardiac stress testing using SPECT or CT imaging agents that do not cross an intact BBB. This study was conducted to determine if standard doses of Regadenoson transiently disrupt the human BBB allowing higher concentrations of systemically administered imaging agents to enter the brain. Patients without known intracranial disease undergoing clinically indicated pharmacologic cardiac stress tests were eligible for this study. They received Regadenoson (0.4 mg) followed by brain imaging with either (99m)Tc-sestamibi for SPECT or visipaque for CT imaging. Pre- and post-Regadenoson penetration of imaging agents into brain were quantified [SPECT: radioactive counts, CT: Hounsfield units (HU)] and compared using a matched-pairs t-test. Twelve patients (33% male, median 60 yo) were accrued: 7 SPECT and 5 CT. No significant differences were noted in pre- and post-Regadenoson values using mean radionuclide counts (726 vs. 757) or HU (29 vs. 30). While animal studies have demonstrated that Regadenoson transiently increases the permeability of the BBB to dextran and temozolomide, we were unable to document changes in the penetration of contrast agents in humans with intact BBB using the FDA approved doses of Regadenoson for cardiac evaluation. Further studies are needed exploring alternate Regadenoson dosing, schedules, and studies in patients with brain tumors; as transiently disrupting the BBB to improve drug entry into the brain is critical to improving the care of patients with CNS malignancies.
Common genetic polymorphisms of adenosine A2A receptor do not influence response to regadenoson.[Pubmed:28358597]
Pharmacogenomics. 2017 Apr;18(6):523-529.
AIM: Hemodynamic response to Regadenoson varies greatly, and underlying mechanisms for variability are poorly understood. We hypothesized that five common variants of adenosine A2A receptor (ADORA2A) are associated with altered response to Regadenoson. METHODS: Consecutive subjects (n = 357) undergoing resting Regadenoson nuclear stress imaging were enrolled. Genotyping was performed using Taqman-based assays for rs5751862, rs2298383, rs3761422, rs2267076 and rs5751876. RESULTS: There was no significant difference in heart rate or blood pressure between different genotypes following Regadenoson administration. There was also no significant difference in myocardial ischemia detected by nuclear perfusion imaging as defined by summed difference score, or in self-reported side effects among the genotypes tested. CONCLUSION: The common A2A variants studied are not associated with variability in hemodynamic response to Regadenoson or variability in detection of ischemia with nuclear perfusion stress imaging.
