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Synthesis and radiolabelling of [123I]-4-iodo-N-(4-(4-(2-methoxyphenyl)-piperazin-1-yl)butyl)-benzamide, a potential dopamine D3 antagonist for SPECT studies

✍ Scribed by L. Staelens; F. Dumont; F. De Vos; R. Oltenfreiter; M. Vandecapelle; R.A. Dierckx; G. Slegers

Publisher
John Wiley and Sons
Year
2003
Tongue
French
Weight
95 KB
Volume
46
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

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~3~ receptor system is thought to be involved in the pathology of schizophrenia. Therefore a new ^123^I‐labelled compound was developed which may allow in vivo visualization of the D~3~ receptor by SPECT. [^123^I]‐4‐iodo‐N‐(4‐(4‐(2‐methoxyphenyl)‐piperazin‐1‐yl)butyl)‐benzamide was synthesized and labelled by electrophilic aromatic substitution of the tributylstannyl derrivative. The radiochemical yield was 82–85% and the specific activity was >2.96 Ci/µmol. Copyright © 2003 John Wiley & Sons, Ltd.

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