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Evaluation of Cardiac ß-Adrenoreceptors in the Isolated Perfused Rat Heart Using (S)-11C-CGP12388

Mitsuru Momose, MD1, Sybille Reder, MT1, David M. Raffel, PhD2, Petra Watzlowik, PhD1, Hans-Jürgen Wester, PhD1, Ngoc Nguyen, MT1, Philip H. Elsinga, PhD3, Frank M. Bengel, MD1, Joerg Remien, MD4 and Markus Schwaiger, MD1

1 Nuklearmedizinische Klinik und Poliklinik der Technischen Universität München, Munich, Germany
2 Department of Radiology, University of Michigan, Ann Arbor, Michigan
3 PET Center, Groningen University Hospital, Groningen, The Netherlands
4 Walther Straub für Pharmakologie und Toxikologie, Ludwig-Maximilians-Universität München, Munich, Germany



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  		FIGURE 1. Compartmental model describing the kinetics of a receptor-binding radioligand administered as a bolus injection into the perfused rat heart.

 


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  		FIGURE 2. In vitro binding of 3H-CGP12177 to ß-adrenoreceptors in membrane preparations: representative saturation binding assay curve for a heart from the group perfused at 6 mL/min (A), Scatchard plot using data from the same heart (B), and saturation binding assay curve for a heart from the propranolol-blocking group (C). No specific binding can be detected in this study.

 


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  		FIGURE 3. Representative time–activity curves for each group: high-flow study (A), low-flow study (B), and ß-blocker study (C). In each group, a second injection with lower specific activity was performed 25 min after the first injection. inj = injection.

 


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  		FIGURE 4. (A) Relationship between Bmax measured in the isolated perfused heart and in vitro. (B) Relationship between KD measured in isolated hearts and in vitro.

 




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