Document Detail

[11C]RN5: a new agent for the in vivo imaging of myocardial alpha1-adrenoceptors.
MedLine Citation:
PMID:  12398909     Owner:  NLM     Status:  MEDLINE    
The radiolabelling with the positron-emitter Carbon-11 and the biological evaluation in rats of 3-[2-[4-(2-[11C]methoxyphenyl)piperazin-1-yl]ethyl]pyrimido[5,4-b]indole-2,4-dione ([11C]RN5), alpha1-adrenoceptor antagonist (K(i)=0.21 nM), as a putative radioligand for the non-invasive assessment of alpha1-adrenoceptors with positron emission tomography (PET) is reported. The radiosynthesis procedure consisted of O-methylation of des-methyl precursor with [11C]methyl iodide in the presence of potassium hydroxide in dimethylformamide (DMF) at 80 degrees C. [11C]RN5 was obtained in >99% radiochemical purity in 25 min with a radiochemical yield in the 20-30% range, end of synthesis (EOS) (non-decay corrected) and a specific radioactivity of 92.5+/-18.5 GBq/micromol. Pre-clinical studies in rats showed a high uptake of [11C]RN5 in heart, spleen, adrenal gland, lung and kidney but not in the brain. Inhibition studies with high doses of different adrenergic antagonists indicate that more than 70% of myocardial uptake of [11C]RN5 is due to specific binding to alpha1-adrenoceptors. Our results indicate that [11C]RN5 is suitable to be further developed as a potential radioligand for the in vivo PET imaging of myocardial alpha1-adrenoceptors in humans.
Mario Matarrese; Rosa M Moresco; Giuseppe Romeo; Elia A Turolla; Pasquale Simonelli; Sergio Todde; Sara Belloli; Assunta Carpinelli; Fulvio Magni; Filippo Russo; Marzia Galli Kienle; Ferruccio Fazio
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  European journal of pharmacology     Volume:  453     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  2002 Oct 
Date Detail:
Created Date:  2002-10-25     Completed Date:  2003-07-08     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  231-8     Citation Subset:  IM    
Institute of Molecular Bioimaging and Physiology-CNR, University of Milano/Bicocca, Institute San Raffaele, Via Olgettina 60, 20132, Milan, Italy.
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MeSH Terms
Adrenergic alpha-Antagonists / pharmacokinetics*
Binding Sites
Carbon Radioisotopes
Indoles / pharmacokinetics*
Isotope Labeling
Myocardium / metabolism*
Pyrimidines / pharmacokinetics*
Radiopharmaceuticals / pharmacokinetics*
Rats, Inbred Strains
Receptors, Adrenergic, alpha-1 / metabolism*
Tissue Distribution
Tomography, Emission-Computed
Reg. No./Substance:
0/3-(2-(4-(2-(11C)methoxyphenyl)piperazin-1-yl)ethyl)pyrimido(5,4-b)indole-2,4-dione; 0/Adrenergic alpha-Antagonists; 0/Carbon Radioisotopes; 0/Indoles; 0/Ligands; 0/Pyrimidines; 0/Radiopharmaceuticals; 0/Receptors, Adrenergic, alpha-1

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