Myocardial Blood Flow and Myocardial Uptake of
 201
 Tl and
 99m
 Tc-Sestamibi During Coronary Vasodilation Induced by CGS-21680, a Selective Adenosine A
 2A
 Receptor Agonist

He, Zhaoyi; Cwajg, Eduardo; Hwang, Wayne S.; Hartley, Craig J.; Funk, Etai; Michael, Lloyd H.; Verani, Mario S.

doi:10.1161/01.cir.102.4.438

Cited by 18 publications

(9 citation statements)

References 30 publications

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“…The increase in normal-zone regional myocardial blood flow after a 1.0 g/kg bolus of ATL-146e was greater than the increase in normal-zone flow reported after either MRE-0470 or CGS-21680 infusions. 10,11 MAP fell only slightly after an ATL-146e bolus, such that it remained Ͼ90 mm Hg. This result is in marked contrast to adenosine bolus injections that caused MAP to fall precipitously by Ϸ50 mm Hg.…”

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confidence: 90%

“…) and CGS-21680 (0.5 to 4.0 g · kg Ϫ1 · min Ϫ1 ), 10,11 yet the former produced a nearly equivalent increase in CF. Thus, ATL-193 is more potent than both MRE-0470 and CGS-21680, and these findings are in agreement with what would be predicted on the basis of the in vitro radioligand binding assay data.…”

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confidence: 92%

“…Preliminary experimental studies have been promising. 10,11 Recently, a new class of selective adenosine A 2A receptor agonists has been synthesized at the University of Virginia. 9 Unlike adenosine, which has a half-life of seconds in human blood, 12 the new compounds are esters that are Ͼ50 times more potent than CGS-21680 at human A 2A receptors and have half-lives of several minutes in human blood.…”

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confidence: 99%

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Pharmacological Stress Myocardial Perfusion Imaging With the Potent and Selective A _2A Adenosine Receptor Agonists ATL193 and ATL146e Administered by Either Intravenous Infusion or Bolus Injection

Glover

Ruiz²,

Takehana³

et al. 2001

Circulation

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Background-Adenosine (Ado) and dipyridamole are alternatives to exercise stress for myocardial perfusion imaging.Though generally safe, side effects frequently occur that cause patient discomfort and sometimes lead to premature termination of the study or require aminophylline administration. Recently, a new class of A 2A Ado receptor agonists was synthesized. ATL193 and ATL146e are 2-propynylcyclohexyl-5Ј-N-ethylcarboxamido derivatives of Ado. The study goals were to evaluate the potency and selectivity of these new compounds on recombinant canine Ado receptors and to evaluate their hemodynamic properties in dogs to assess their usefulness as vasodilators for myocardial perfusion imaging. Methods and Results-In assays of recombinant canine Ado receptors, ATL-193 and ATL-146e were highly selective for the A 2A over the A 1 and A 3 receptors and were more potent than MRE-0470 and CGS-21680. In 16 anesthetized dogs, the agonists were administered by infusion (ATL-193; nϭ7 normal) or bolus injection (ATL-146e; nϭ9 critical left anterior descending coronary artery stenosis), and hemodynamic responses were compared with those of Ado. Both agonists produced dose-dependent coronary flow (CF) elevation without provoking the hypotension observed with Ado.After an ATL-146e bolus, the CF increase was sustained for several minutes, providing ample time for injection and myocardial uptake of 99m Tc-sestamibi, and CF returned to baseline within 20 minutes. The CF increase was completely blocked by the selective A 2A antagonist ZM241385 (3 g · kg Ϫ1 · min Ϫ1 ). Conclusions-ATL-193 and ATL-146e are highly potent and selective Ado A 2A receptor agonists with excellent potential for use as vasodilators for myocardial perfusion imaging. An important advantage of ATL-146e is the ability to administer it by bolus injection.

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confidence: 90%

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confidence: 92%

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confidence: 99%

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Pharmacological Stress Myocardial Perfusion Imaging With the Potent and Selective A _2A Adenosine Receptor Agonists ATL193 and ATL146e Administered by Either Intravenous Infusion or Bolus Injection

Glover

Ruiz²,

Takehana³

et al. 2001

Circulation

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“…In animal studies, vasodilators in the setting of severe coronary stenoses have been shown to create changes in the endocardial-epicardial flow ratio which could result in ischemic ECG changes in those with normal perfusion. 26 Recently, Sharma and colleagues demonstrated a very low incidence of hard events (CD or MI) in patients with normal MPI and adenosine-induced ischemic ECG changes. 15 Similar to the patient population in the study by Hage, Sharma et al also excluded patients with known CAD.…”

Section: Prognostic Significance Of Vasodilator Stress Ecg Changesmentioning

confidence: 99%

Electrocardiographic changes during vasodilator SPECT myocardial perfusion imaging: Does it affect diagnosis or prognosis?

Azemi

Rai

Parwani

et al. 2012

Journal of Nuclear Cardiology

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“…Apadenoson and CGS-21680 have been investigated in preclinical trials. To date, there are limited data published for binodenoson (25)(26)(27)(28)(29)(30) and even fewer for apadenoson and CGS-21680 (31,32).…”

Section: A 2a Receptor Agonistsmentioning

confidence: 99%

Advances in Pharmacologic Stress Agents: Focus on Regadenoson

Johnson¹,

Peters²

2010

Journal of Nuclear Medicine Technology

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Myocardial perfusion imaging using radionuclides is a wellestablished protocol for determining the diagnosis, prognosis, and management of coronary artery disease. Pharmacologic stress agents are used to induce cardiac hyperemia in patients unable to achieve the target workload by physical exercise alone. The vasodilators adenosine and dipyridamole are most commonly used, with dobutamine used only when these agents are contraindicated. However, because of frequent and intense side effects, as well as complex procedures both for patients and the nuclear medicine staff, there is room for improvement in these traditional stress agents. An ideal stress agent would be effective, safe, and well tolerated; have a simple protocol; be suitable for use in patients with reactive airway disease; and have few restrictions for the patient to adhere to before the procedure. Neither adenosine nor dipyridamole are receptorspecific, and act on A 1 , A 2A , A 2B , and A 3 adenosine receptors. As it is the A 2A receptor that mediates the desired coronary vasodilation, the A 1 , A 2B , and A 3 adenosine receptors are deemed responsible for most side effects associated with adenosine and dipyridamole. A 2A -selective pharmacologic stress agents should mediate the required hyperemic response while reducing the frequency of adverse events. The only selective A 2A adenosine receptor agonist currently approved for clinical use as a pharmacologic stress agent for myocardial perfusion imaging is regadenoson. Regadenoson has demonstrated non-inferiority to adenosine for detecting reversible myocardial perfusion defects in phase 3 trials, and patients were more comfortable during the regadenoson stress procedure than during an adenosine infusion. As regadenoson dosing is not dependent on patient weight or renal impairment and can be administered by rapid injection, it has the potential to simplify the stress procedure, reduce costs, and streamline the working day for the staff of the nuclear medicine department. In this review, the need to improve on older pharmacologic stress agents will be considered, along with an assessment of how A 2A receptor agonists fulfill that potential. Practical aspects of regadenoson are reviewed, and the impact that A 2A receptor agonist use may have on the nuclear medicine department is evaluated.

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Myocardial Blood Flow and Myocardial Uptake of ²⁰¹ Tl and ^99m Tc-Sestamibi During Coronary Vasodilation Induced by CGS-21680, a Selective Adenosine A _2A Receptor Agonist

Abstract: CGS-21680 elicits coronary vasodilation comparable to that of adenosine and produces profound heterogeneity of MBF and of (201)Tl and (99m)Tc-sestamibi myocardial uptake, rendering it a promising agent for pharmacological myocardial perfusion imaging.

Cited by 18 publications

References 30 publications

Pharmacological Stress Myocardial Perfusion Imaging With the Potent and Selective A _2A Adenosine Receptor Agonists ATL193 and ATL146e Administered by Either Intravenous Infusion or Bolus Injection

Pharmacological Stress Myocardial Perfusion Imaging With the Potent and Selective A _2A Adenosine Receptor Agonists ATL193 and ATL146e Administered by Either Intravenous Infusion or Bolus Injection

Electrocardiographic changes during vasodilator SPECT myocardial perfusion imaging: Does it affect diagnosis or prognosis?

Advances in Pharmacologic Stress Agents: Focus on Regadenoson

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Myocardial Blood Flow and Myocardial Uptake of 201 Tl and 99m Tc-Sestamibi During Coronary Vasodilation Induced by CGS-21680, a Selective Adenosine A 2A Receptor Agonist

Abstract: CGS-21680 elicits coronary vasodilation comparable to that of adenosine and produces profound heterogeneity of MBF and of (201)Tl and (99m)Tc-sestamibi myocardial uptake, rendering it a promising agent for pharmacological myocardial perfusion imaging.

Cited by 18 publications

References 30 publications

Pharmacological Stress Myocardial Perfusion Imaging With the Potent and Selective A 2A Adenosine Receptor Agonists ATL193 and ATL146e Administered by Either Intravenous Infusion or Bolus Injection

Pharmacological Stress Myocardial Perfusion Imaging With the Potent and Selective A 2A Adenosine Receptor Agonists ATL193 and ATL146e Administered by Either Intravenous Infusion or Bolus Injection

Electrocardiographic changes during vasodilator SPECT myocardial perfusion imaging: Does it affect diagnosis or prognosis?

Advances in Pharmacologic Stress Agents: Focus on Regadenoson

Contact Info

Product

Resources

About

Myocardial Blood Flow and Myocardial Uptake of ²⁰¹ Tl and ^99m Tc-Sestamibi During Coronary Vasodilation Induced by CGS-21680, a Selective Adenosine A _2A Receptor Agonist

Pharmacological Stress Myocardial Perfusion Imaging With the Potent and Selective A _2A Adenosine Receptor Agonists ATL193 and ATL146e Administered by Either Intravenous Infusion or Bolus Injection

Pharmacological Stress Myocardial Perfusion Imaging With the Potent and Selective A _2A Adenosine Receptor Agonists ATL193 and ATL146e Administered by Either Intravenous Infusion or Bolus Injection