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Synthesis of [123I]-3-(4-iodobenzyl)-1,2,3,4-tetrahydro-8-hydroxychromeno[3,4-c]pyridin-5-one, a potential dopamine D4 ligand for SPECT studies

✍ Scribed by L. Staelens; R. Oltenfreiter; B. Cornelissen; P. Blanckaert; F. De Vos; D. Deforce; R.A. Dierckx; G. Slegers

Publisher
John Wiley and Sons
Year
2005
Tongue
French
Weight
108 KB
Volume
48
Category
Article
ISSN
0022-2135

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✦ Synopsis

Schizophrenia is a devastating mental disorder characterized by relapsing psychotic episodes accompanied with emotional, professional and social decline. The classical dopamine hypothesis of schizophrenia postulates that hyperactivity of dopaminergic neurotransmission is responsible for the positive symptoms of the disorder, more exactly hyperactivity of the dopamine D 2 -like receptors. One of these receptors is the D 4 receptor which is thought to be involved in the motor side-effects caused antipsychotics. However, research into the specific role of this receptor has been hampered by the lack of specific ligands. Therefore, a new 123 I-labelled compound was developed which may allow in vivo visualization of the D 4 receptor by SPECT. 2,3,4-tetrahydro-8-hydroxychromeno[3,4-c]pyridin-5-one was prepared by electrophillic aromatic substitution of the tributylstannyl derivative. The radiochemical yield was 68 AE 3% (n=5) and the specific activity was >2.96 Ci/ mmol.

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