PMID: 11323238Apr 27, 2001Paper

Synthesis and preliminary evaluation of a carbon-11-labeled adenosine transporter blocker [(11)C]KF21562

Nuclear Medicine and Biology
K IshiwataM Senda

Abstract

We prepared an (11)C-labeled adenosine transporter blocker, [1-methyl-(11)C]-3-[1-(6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]-1,6-dimethyl-2,4(1H, 3H)-quinazolinedione ([(11)C]KF21652) and examined its potential as a positron emission tomography (PET) ligand for mapping adenosine transporters in the brain and peripheral organs. The log P(7.4) value of KF21652 was 3.14, and the K(i) value was 13 nM for adenosine transporters using [(3)H]nitrobenzylthioinosine as a radioligand. In mice, the highest initial uptake was found in the liver, followed by the kidney and small intestine. The brain uptake was very low. The radioactivity level slightly increased with time in the liver and small intestine, but decreased in the other organs. Coinjection of carrier KF21652 slightly decreased the uptake of [(11)C]KF21562 only in the liver, but not in any other organs. Ex vivo autoradiography of the rat brain showed that [(11)C]KF21652 was scarcely incorporated into the brain. On the other hand, in vitro autoradiography showed the binding of [(11)C]KF21562 to adenosine transporters with high nonspecific binding. These results show that the compound is not a suitable PET ligand for mapping adenosine transporters.

References

Oct 11, 1988·Biochimica Et Biophysica Acta·P G PlagemannC Woffendin
Jan 21, 1985·Life Sciences·A Verma, P J Marangos
May 1, 1992·Trends in Cardiovascular Medicine·B T Liang

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Citations

Jun 18, 2002·European Journal of Pharmacology·Tomas de PaulisPeter R Martin
Jul 16, 2010·Geriatrics & Gerontology International·Kiichi IshiwataJun Toyohara
Apr 20, 2004·Nuclear Medicine and Biology·Kiichi IshiwataKazuhiko Yanai

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