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Synthesis of [ 123 I]‐3‐(4‐iodobenzyl)‐1,2,3,4‐tetrahydro‐8‐hydroxychromeno[3,4‐ c ]pyridin‐5‐one, a potential dopamine D 4 ligand for SPECT studies
Author(s) -
Staelens L.,
Oltenfreiter R.,
Cornelissen B.,
Blanckaert P.,
De Vos F.,
Deforce D.,
Dierckx R.A.,
Slegers G.
Publication year - 2005
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.902
Subject(s) - dopaminergic , chemistry , dopamine , schizophrenia (object oriented programming) , dopamine receptor d2 , ligand (biochemistry) , receptor , dopamine receptor , in vivo , psychosis , psychology , dopamine hypothesis of schizophrenia , neuroscience , spect imaging , pharmacology , psychiatry , medicine , biochemistry , microbiology and biotechnology , biology , nuclear medicine
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 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. [ 123 I]‐3‐(4‐iodobenzyl)‐1,2,3,4‐tetrahydro‐8‐hydroxychromeno[3,4‐ c ]pyridin‐5‐one was prepared by electrophillic aromatic substitution of the tributylstannyl derivative. The radiochemical yield was 68±3% ( n =5) and the specific activity was >2.96 Ci/µmol. Copyright © 2005 John Wiley & Sons, Ltd.