1Bioorg. Med. Chem. 2002 Aug 10: 2611-23
TitleSynthesis of a fluorine-18-labelled derivative of 6-nitroquipazine, as a radioligand for the in vivo serotonin transporter imaging with PET.
AbstractConsiderable efforts have been engaged in the design, synthesis and pharmacological characterization of radioligands for imaging the serotonin transporter, based on its implication in several neuropsychiatric diseases, such as depression, anxiety and schizophrenia. In the 5-halo-6-nitroquipazine series, the fluoro derivative has been designed for positron emission tomography (PET). The corresponding 5-iodo-, 5-bromo- and 5-chloro N-BOC-protected quipazines as labelling precursors, as well as 5-fluoro-6-nitroquipazine as a reference compound have been synthesized. 5-[(18)F]Fluoro-6-nitroquipazine has been radiolabelled with fluorine-18 (positron-emitting isotope, 109.8 min half-life) by nucleophilic aromatic substitution from the corresponding N-BOC protected 5-bromo- and 5-chloro-precursors using K[(18)F]F-K(222) complex in DMSO by conventional heating (145 degrees C, 2 min) or microwave activation (50 W, 30-45 s), followed by removal of the protective group with TFA. Typically, 15-25 mCi (5.5-9.2 GBq) of 5-[(18)F]fluoro-6-nitroquipazine (1-2 Ci/micromol or 37-72 GBq/micromol) could be obtained in 70-80 min starting from a 550-650 mCi (20.3-24.0 GBq) aliquot of a cyclotron [(18)F]F(-) production batch (2.7-3.8% non decay-corrected yield based on the starting [(18)F]fluoride). Ex vivo studies (biodistribution in rat), as well as PET imaging (in monkey) demonstrated that 5-[(18)F]fluoro-6-nitroquipazine ([(18)F]-1d) readily crossed the blood brain barrier and accumulated in the regions rich in 5-HT transporter (frontal- and posterial cortex, striata). However, the low accumulation of the tracer in the thalamus (rat and monkey) as well as the comparable displacement of the tracer observed with both citalopram, a -HT re-uptake inhibitor and maprotiline, a norepinephrine re-uptake inhibitor (rat), indicate that 5-[(18)F]fluoro-6-nitroquipazine ([(18)F]-1d) does not have the suggested potential for PET imaging of the serotin transporter (SERT).
SCZ Keywordsschizophrenia, schizophrenics
2Iran J Psychiatry 2012 -1 7: 140-5
TitleThe Relationship between Obsessions and Compulsions and Negative and Positive Symptoms in Schizophrenia.
AbstractThe aim of the present study is to investigate the relationship between obsessive-compulsive symptoms (OCSs) and negative and positive symptoms in schizophrenia.
Subjects of the study comprised of 31 schizophrenia with obsessive-compulsive symptoms (19 men and 12 women) selected by convenience sampling method from Iran psychiatric Hospital. The diagnoses were established on the basis of DSM-IV-TR. The required data were obtained using Positive and Negative Syndrome Scale (PANSS) and Yale-Brown Obsessive-Compulsive scale (Y-BOC).
The results of multiple regression analysis indicated that obsessive symptoms inversely predict negative symptoms. In other words, as the obsessive symptoms increase, the negative symptoms of schizophrenia decrease. Nevertheless, no significant relationship was found between OCSs and positive symptoms.
This study reveals that OCSs exert a protective effect on schizophrenia and do not necessarily cause poorer prognosis.
SCZ Keywordsschizophrenia, schizophrenics