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Characterization of Pulmonary and Myocardial Beta-Adrenoceptors with S-1'-[Fluorine-18]Fluorocarazolol

Positron Emission Tomography Center and Department of Pulmonary Diseases, University Hospital, Groningen
Department of Analytical Chemistry and Toxicology, University Center for Pharmacy, Groningen, The Netherlands

Correspondence: For correspondence or reprints contact: Aren van Waarde, PET Center, University Hospital, P.O. Box 30001, 9700 RB Groningen, The Netherlands.

ABSTRACT

S-1'-[¹⁸F]fluorocarazolol was administered to healthy volunteers to assess its potential for noninvasive measurement of regional pulmonary and myocardial beta-adrenoceptor densities. Methods: High specific activity fluorocarazolol was intravenously injected on two separate occasions within a 1-wk interval. The initial injection was without pretreatment, but before the second injection, the volunteers either inhaled salbutamol (2 x 200 µg aerosol) or they ingested pindolol (3 x 5 mg during a 12-hr interval). Twenty-eight PET time frames of 31 planes were acquired over a period of 60 min after each injection. BlOOd samples were drawn and analyzed for the presence of fluorocarazolol and radioactive metabolites. Results: Uptake of fluorocarazolol in the target tissues was hardly affected by salbutamol but was strongly depressed by pindolol. Pulmonary and myocardial tissue-to-plasma concentration ratios of fluorocarazolol reached plateau values of 11.6 ± 0.6 lungs) and 18.1 ± 1.0 (heart) at 45–50 min postinjection. These values were reduced to 2.0 ± 0.4 and 2.0 ± 0.6 after treatment with pindolol. Conclusion: These data indicate that:

1. Pulmonary and myocardial uptake of radioactivity after intravenous administration of S-1'-[¹⁸F]fluorocarazolol represents radioligand binding to beta-adrenoceptors.

2. Pulmonary binding occurs mainly in alveoli rather than in airway smooth muscle under these conditions.

3. Binding kinetics do not preclude quantification of receptors with compartment models.

Key Words: beta-adrenoceptor density • fluorine-18-fluorocarazolol • PET

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