[18F]Altanserin; 5HT2 Receptors; Rat; Brain; Autoradiography; PET
Abstract :
[en] To further validate its use in positron emission tomography (PET), we studied the binding of [18F]altanserin, a specific 5HT2 radioligand, in the rat brain using in vivo autoradiography. Distribution of [18F]altanserin binding was comparable to the in vitro mapping of 5HT2 receptors reported in the literature. Selective displacers were used to test the reversibility and the selectivity of this radioligand. Specific binding of [18F]altanserin in the rat frontal cortex was quantified by direct counting with an electronic imaging system and by quantification on digitalized autoradiograms. Close results of about 30 pmol/g were obtained with both methods. Our data confirmed that [18F]altanserin is a valid tracer for 5HT2 receptors binding studies.
Disciplines :
Laboratory medicine & medical technology
Author, co-author :
Biver, Françoise
Lotstra, Françoise
Monclus, M.
Dethy, S.
Damhaut, P.
Wikler, D.
Luxen, André ; Université de Liège - ULiège > Département de chimie (sciences) > Chimie organique de synthèse - Centre de recherches du cyclotron
Goldman, Serge
Language :
English
Title :
In vivo binding of [F-18]altanserin to rat brain 5HT(2) receptors: A film and electronic autoradiographic study
Publication date :
1997
Journal title :
Nuclear Medicine and Biology
ISSN :
0969-8051
Publisher :
Elsevier Science Inc, New York, United States - New York
Appel N. M., Mitchell W. M., Garlick R. K., Glennon R. A., Teitler M. and De Souza E. B. (1990) Autoradiographic characterization of (±)-1-(2,5-dimethoxy-4-[125I]iodophenyl0-2-amino-propane ([125I]DOIO binding to 5-HT2 and 5-HT1C receptors in rat brain. J. Pharmacol. Exp. Ther. 255, 843-857.
Biver F., Goldman S., Luxen A., Monclus M., Forestini M., Mendlewicz J. and Lotstra F. (1994) Multi-compartmental study of [18F]altanserin binding to brain 5HT2 receptors in human using positron emission tomography. Eur. J. Nucl. Med. 21, 937-946.
Johnson E. W., Sybirska E., Al-Tikriti M. and Innis R. B. (1991) Calibration of [123I]Iodine-labeled tissue standards for autoradiographic studies. Appl. Radiat. Isot. 42, 1199-1201.
Lemaire C., Cantineau R., Guillaume M., Plenevaux A. and Christiaens L. (1991) Fluorine-18-altanserin: a radioligand for the study of serotonin receptors with PET: radiolabeling and in vivo biologic behavior in rats. J. Nucl. Med. 32, 2266-72.
Leysen J. E. (1992) 5HT2-receptors: location, pharmacological, pathological and physiological role. In: Serotonin receptor subtypes: pharmacological significance and clinical implications (Edited by Langer S. Z., Brunello N., Racagni G. and Mendlewicz J.) pp 31-43. Karger, Basel.
Malgouris C., Flamand F. and Doble A. (1993) Autoradiographic studies of RP62203, a potent 5-HT2 receptor antagonist. In vitro and ex vivo selectivity profile. Eur. J. Pharmacol. 233, 29-35.
Mengod G., Pompeiano M., Martinez-Mir I. and Palacios J. M. (1990) Localization of the mRNA for the 5-HT2 receptor by in situ hybridization histochemistry. Correlation with the distribution of receptors sites. Brain Res. 524, 139-143.
Monclus M., Masson C., Luypaert P. J., Van Naemen J., Ledent E. and Luxen A. (1993) Nucleophilic [18F] radiofluorination using microwave cavity: application to [18F]FDG and [18F]altanserin synthesis. Eur. J. Nucl. Med. 20, 1000.
Pazos A., Probst A. and Palacios J. M. (1987) Serotonin receptors in the human brain. IV. Autoradiographic mapping of serotonin-2 receptors. Neuroscience 21, 123-139.
