Synthesis and biodistribution of [5-131I]iodotropapride: a potential D2 dopamine receptor imaging agent.

Animals; Brain/metabolism; Cerebellum/metabolism; Frontal Lobe/metabolism; Iodine Radioisotopes/diagnostic use; Male; Nortropanes/metabolism/pharmacokinetics; Octanols; Protein Binding; Radiopharmaceuticals/metabolism/pharmacokinetics; Rats; Rats, Wistar; Receptors, Dopamine D2/metabolism; Tissue Distribution/physiology; Water

Abstract :

[en] [5-131I]Iodotropapride is a benzamidic compound which displays high affinity and selectivity for dopaminergic receptors. It was prepared from the corresponding brominated compound by a nucleophilic substitution with [131I]iodine (t1/2 = 8.02 days, E gamma = 364 keV) based on the use of Cu(I) as catalyst and high specific activity of [131I]NaI. After i.v. injection in rats the tracer crosses the blood-brain barrier (0.42 +/- 0.06% of injected dose in the total brain) and demonstrates a high affinity binding to the striatum. The striatum-to-cerebellum ratio increases with time and reaches values of 9 and 22 at 30 and 120 min after injection, respectively. This specific uptake in the striatum is saturable and can be blocked by pretreatment with different D2 antagonists. When labeled with 123I (t1/2 = 13 h, E1 = 159 keV), the corresponding [123I]iodotropapride may be useful for the investigation of the D2 dopamine receptors in humans with single photon emission computer tomography (SPECT).

Research Center/Unit :

GIGA CRC (Cyclotron Research Center) In vivo Imaging-Aging & Memory - ULiège

Disciplines :

Chemistry

Author, co-author :

Cantineau, Robert

Guillaume, Marcel

Damhaut, Philippe; Université de Liège - ULiège > Centre de recherches du cyclotron

Lemaire, Christian ; Université de Liège - ULiège > Centre de recherches du cyclotron

Plenevaux, Alain

Gauthier, Françoise

Pourrias, Bernard

Christiaens, Léon

Language :

English

Title :

Synthesis and biodistribution of [5-131I]iodotropapride: a potential D2 dopamine receptor imaging agent.

Publication date :

1994

Journal title :

Nuclear Medicine and Biology

ISSN :

0969-8051

Publisher :

Pergamon Press, Oxford, United Kingdom

Volume :

Issue :

Pages :

255-62

Peer reviewed :

Peer Reviewed verified by ORBi

Funders :

F.R.S.-FNRS - Fonds de la Recherche Scientifique

Available on ORBi :

since 02 February 2009

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