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Synthesis and radiolabelling of [ 123 I]‐4‐iodo‐N‐(4‐(4‐(2‐methoxyphenyl)‐piperazin‐1‐yl)butyl)‐benzamide, a potential dopamine D 3 antagonist for SPECT studies
Author(s) -
Staelens L.,
Dumont F.,
Vos F. De,
Oltenfreiter R.,
Vandecapelle M.,
Dierckx R.A.,
Slegers G.
Publication year - 2003
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.671
Subject(s) - chemistry , benzamide , antagonist , d 1 , dopamine , iodine 123 , stereochemistry , technetium , medicinal chemistry , radiochemistry , nuclear chemistry , nuclear medicine , medicine , biochemistry , receptor
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.