Abstract：
:We report positron emission tomography studies of beta-adrenoceptors in the human thorax with (S)-[(11)C]CGP12388 (4-(3-(2'-[(11)C]-isopropylamino)-2-hydroxypropoxy)-2H-benzimidazol-2-one). Beta-adrenoceptors have previously been quantified using (S)-[(11)C]CGP12177 (4-(3-tert-butylamino-2-hydroxypropoxy)-2H-benzimidazol-2[(11)C]-one), but (S)-[(11)C]CGP12388 is more easily prepared and therefore more suitable in a clinical setting. (S)-[(11)C]CGP12388 was administered to five healthy volunteers on two separate days (control and pindolol block study). Arterial plasma samples were used to determine clearance, metabolites, and protein binding of the radioligand. Heart, lung and spleen showed high uptake of radioactivity, which was strongly suppressed (68-77%) by pindolol. Plasma clearance of (S)-[(11)C]CGP12388 was rapid, binding to plasma proteins was low (53+/-4%), and the radioligand was slowly metabolized. (S)-[(11)C]CGP12388 produces high-quality images of the human thorax. Uptake of (S)-[(11)C]CGP12388 in heart, lung and spleen represents binding to beta-adrenoceptors. (S)-[(11)C]-CGP12388 seems useful for imaging of beta-adrenoceptors in a clinical setting.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Elsinga PH,Doze P,van Waarde A,Pieterman RM,Blanksma PK,Willemsen AT,Vaalburg Wdoi
10.1016/s0014-2999(01)01499-6keywords:
subject
Has Abstractpub_date
2001-12-21 00:00:00pages
173-6issue
2-3eissn
0014-2999issn
1879-0712pii
S0014299901014996journal_volume
433pub_type
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