Myocardial beta-adrenoceptor downregulation in idiopathic dilated cardiomyopathy measured in vivo with PET using the new radioligand (S)-[11C]CGP12388

Eur J Nucl Med Mol Imaging. 2005 Apr;32(4):443-7. doi: 10.1007/s00259-004-1701-z. Epub 2004 Dec 11.

Abstract

Purpose: The beta-adrenoceptor (beta-AR) plays an important role in heart failure. Recently, the new tracer (S)-[11C]CGP12388 has been developed. It displays excellent properties for investigation of the cardiac beta-ARs in vivo with positron emission tomography (PET). Furthermore, the simple production method allows its use in a routine clinical setting. The aim of this study was to investigate whether decreased myocardial beta-AR density in patients with idiopathic dilated cardiomyopathy (IDC) can be estimated using (S)-[11C]CGP12388 PET.

Methods: Myocardial beta-AR density was investigated in six patients with IDC and six age-matched healthy controls, using (S)-[11C]CGP12388 PET.

Results: Beta-AR densities of 5.4+/-1.3 pmol/g (mean +/- SD) were observed in patients; these values were significantly lower than those observed in healthy controls (8.4+/-1.5 pmol/g, p<0.005).

Conclusion: This study indicates that PET with (S)-[11C]CGP12388 is applicable for the measurement of myocardial beta-AR density in patients. A highly significant reduction in beta-AR density was found in patients with IDC compared with healthy controls.

Publication types

  • Clinical Trial
  • Controlled Clinical Trial

MeSH terms

  • Adult
  • Aged
  • Benzimidazoles / pharmacokinetics*
  • Carbon Radioisotopes / pharmacokinetics
  • Cardiomyopathy, Dilated / diagnostic imaging*
  • Cardiomyopathy, Dilated / metabolism*
  • Down-Regulation
  • Female
  • Heart / diagnostic imaging
  • Humans
  • Ligands
  • Male
  • Middle Aged
  • Myocardium / metabolism*
  • Positron-Emission Tomography / methods*
  • Radiopharmaceuticals / pharmacokinetics
  • Receptors, Adrenergic, beta / metabolism*
  • Tissue Distribution

Substances

  • Benzimidazoles
  • Carbon Radioisotopes
  • Ligands
  • Radiopharmaceuticals
  • Receptors, Adrenergic, beta
  • CGP 12388