Evaluation of cardiac β-adrenoreceptors in the isolated perfused rat heart using (S)-11C-CGP12388

Mitsuru Momose, Sybille Reder, David M. Raffel, Petra Watzlowik, Hans Jürgen Wester, Ngoc Nguyen, Philip H. Elsinga, Frank M. Bengel, Joerg Remien, Markus Schwaiger

Research output: Contribution to journalArticlepeer-review

21 Scopus citations


(S)-11C-CGP12388 (11C-CGP12388) was recently developed as an in vivo PET tracer for the evaluation of cardiac β-adrenergic receptors. The purpose of this study was to evaluate the myocardial kinetics of 11C-CGP12388 using the perfused rat heart model. Methods: Normal rat hearts were cannulated for retrograde perfusion according to the Langendorff method. Studies were performed using constant coronary flow rates of 12 mL/min (high flow: n = 6) and 6 mL/min (low flow: n = 6). β-Adrenergic-blocking studies were also done using propranolol (blocking: n = 6). Two bolus injections of 11C-CGP12388 were administered at a 25-min interval, and time-activity curves were measured using bismuth germanate detectors. The β-adrenergic receptor density (B max) and total distribution volume (DVtot) were estimated using compartmental modeling. After the experiment, Bmax in vitro was measured for all hearts using 3H-CGP12177, and the values were compared with the Bmax estimated in isolated hearts. Results: DV tot was significantly lower in the blocking group than in the high-flow group (P < 0.01), and there was no significant difference in DVtot between the high-and the low-flow groups. Bmax values estimated from 11C-CGP12388 kinetics were 5.05 ± 0.90 pmol/g under the high-flow model and 5.20 ± 0.63 pmol/g under the low-flow model. The Bmax results in isolated hearts correlated significantly with the measured in vitro Bmax values (r2 = 0.69; P < 0.001). Conclusion: β-Adrenoreceptor density in the isolated rat heart can be quantified using 11C-CGP12388 and a 2-injection protocol. The binding of the tracer was flow independent, with low nonspecific binding. These results suggest that 11C-CGP12388 is a promising PET tracer that may be applicable to human studies.

Original languageEnglish (US)
Pages (from-to)471-477
Number of pages7
JournalJournal of Nuclear Medicine
Issue number3
StatePublished - Mar 1 2004
Externally publishedYes


  • C-CGP12388
  • Isolated rat heart
  • Langendorff
  • PET
  • β-adrenoreceptor density

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging


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