PMID: 9169564Jun 1, 1997Paper

In vitro and in vivo characterisation of nor-beta-CIT: a potential radioligand for visualisation of the serotonin transporter in the brain

European Journal of Nuclear Medicine
K A BergströmL Farde

Abstract

Radiolabelled 2beta-carbomethoxy-3beta-(4-iodophenyl)tropane (beta-CIT) has been used in clinical studies for the imaging of dopamine and serotonin transporters with single-photon emission tomography (SPET). 2beta-Carbomethoxy-3beta-(4-iodophenyl)nortropane (nor-beta-CIT) is a des-methyl analogue of beta-CIT, which in vitro has tenfold higher affinity (IC50=0.36 nM) to the serotonin transporter than beta-CIT (IC50=4.2 nM). Nor-beta-CIT may thus be a useful radioligand for imaging of the serotonin transporter. In the present study iodine-125 and carbon-11 labelled nor-beta-CIT were prepared for in vitro autoradiographic studies on post-mortem human brain cryosections and for in vivo positron emission tomography (PET) studies in Cynomolgus monkeys. Whole hemisphere autoradiography with [125I]nor-beta-CIT demonstrated high binding in the striatum, the thalamus and cortical regions of the human brain. Addition of a high concentration (1 microM) of citalopram inhibited binding in the thalamus and the neocortex, but not in the striatum. In PET studies with [11C]nor-beta-CIT there was rapid uptake of radioactivity in the monkey brain (6% of injected dose at 15 min) and high accumulation of radioactivity in the striatum, thalamus and n...Continue Reading

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Citations

Feb 2, 2013·World Journal of Nuclear Medicine·Kalevi Kairemo
Mar 30, 2004·CNS Spectrums·Susan E Kennedy, Jon-Kar Zubieta
Dec 18, 2008·Expert Review of Neurotherapeutics·Angelo Antonini, Ioannis U Isaias
Jun 16, 2011·Medicinal Research Reviews·Louise M PatersonGitte M Knudsen
Nov 13, 2004·European Archives of Psychiatry and Clinical Neuroscience·Eduard MaronJakov Shlik
Nov 29, 2013·Journal of Labelled Compounds & Radiopharmaceuticals·Jeffrey S Stehouwer, Mark M Goodman
Nov 20, 2002·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Yiyun HuangMarc Laruelle

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