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


CONCLUSIONS
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.
de Jong
Richard M
RM
Deparment of Cardiology, Groningen University Hospital, Groningen, The Netherlands.
Willemsen
Antoon T M
AT
Slart
Riemer H J A
RH
Blanksma
Paul K
PK
van Waarde
Aren
A
Cornel
Jan Hein
JH
Vaalburg
Willem
W
van Veldhuisen
Dirk J
DJ
Elsinga
Philip H
PH
D000328:Adult; D000368:Aged; D001562:Benzimidazoles / Q000493:pharmacokinetics*; D002250:Carbon Radioisotopes / Q000493:pharmacokinetics; D002311:Cardiomyopathy, Dilated / Q000000981:diagnostic imaging* / Q000378:metabolism*; D015536:Down-Regulation; D005260:Female; D006321:Heart / Q000000981:diagnostic imaging; D006801:Humans; D008024:Ligands; D008297:Male; D008875:Middle Aged; D009206:Myocardium / Q000378:metabolism*; D049268:Positron-Emission Tomography / Q000379:methods*; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D011943:Receptors, Adrenergic, beta / Q000378:metabolism*; D014018:Tissue Distribution
D001562:Benzimidazoles; D002250:Carbon Radioisotopes; D008024:Ligands; D019275:Radiopharmaceuticals; D011943:Receptors, Adrenergic, beta; C109239:CGP 12388