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(Circulation. 2000;102:438.)
© 2000 American Heart Association, Inc.

Basic Science Reports

Myocardial Blood Flow and Myocardial Uptake of ²⁰¹Tl and ^99mTc-Sestamibi During Coronary Vasodilation Induced by CGS-21680, a Selective Adenosine A_2A Receptor Agonist

Zuo-Xiang He, MD; Eduardo Cwajg, MD; Wayne Hwang, MD; Craig J. Hartley, PhD; Etai Funk, BS; Lloyd H. Michael, PhD; Mario S. Verani, MD

From the Section of Cardiology, Baylor College of Medicine/Methodist Hospital, Houston, Tex. Dr He’s current address is Fu Wai Hospital, Dept of Nuclear Medicine, Beijing, China.

Correspondence to Mario S. Verani, MD, Professor of Medicine, Baylor College of Medicine, 6550 Fannin, SM 677, Houston, TX 77030. E-mail mverani{at}bcm.tmc.edu

Background—We investigated the hemodynamic and coronary vasodilatory effects of CGS-21680, a potent selective adenosine A_2A agonist, as well as its potential use as a new stress modality in combination with perfusion scintigraphy.

Methods and Results—A stenosis of the left anterior descending coronary artery (LAD) was produced in dogs to reduce the reactive hyperemic response to <20%. Adenosine and CGS-21680 were then separately infused to maximize left circumflex coronary artery (LCx) flow velocity. ²⁰¹Tl (0.5 mCi) and ^99mTc-sestamibi (5 mCi) were injected at the maximal dose of CGS-21680. Heart rate decreased with adenosine but increased during CGS-21680 infusion (P<0.005). The decrease in systolic blood pressure was more prominent with adenosine than with CGS-21680 (P<0.005). In the control LCx zone, maximal myocardial blood flow (MBF) (measured by radioactive microspheres) increased 3.1-fold during adenosine infusion (P<0.005) and 3.8-fold during CGS-21680 infusion (P<0.005). In the stenotic LAD zone, MBF did not change significantly. During adenosine and CGS-21680 infusion, stenosis/control zone MBF ratios were comparable (0.32±0.11 versus 0.27±0.10, P=NS), and transmural ²⁰¹Tl and ^99mTc-sestamibi count-activity ratios (0.48±0.11 and 0.51±0.09, respectively) were also comparable (P=NS). Myocardial scintigraphy uncovered perfusion defects in all dogs.

Conclusions—CGS-21680 elicits coronary vasodilation comparable to that of adenosine and produces profound heterogeneity of MBF and of ²⁰¹Tl and ^99mTc-sestamibi myocardial uptake, rendering it a promising agent for pharmacological myocardial perfusion imaging.

Key Words: adenosine • receptors • CGS-21680 • radioisotopes • imaging • coronary disease

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