PMCCPMCCPMCC

Search tips
Search criteria 

Advanced

 
Logo of aghpsycbiomed central web sitesearch.manuscript submission.see also annals of general psychiatry journal in pmc.registration.reference to the article.journal front page.
 
Ann Gen Hosp Psychiatry. 2004; 3: 1.
Published online Jan 7, 2004. doi:  10.1186/1475-2832-3-1
PMCID: PMC320490
Behavioral and antioxidant activity of a tosylbenz[g]indolamine derivative. A proposed better profile for a potential antipsychotic agent
Chara A Zika,corresponding author1 Ioannis Nicolaou,1 Antonis Gavalas,1 George V Rekatas,1 Ekaterini Tani,1 and Vassilis J Demopoulos1
1Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki, 54124 Greece
corresponding authorCorresponding author.
Chara A Zika: chzika/at/pharm.auth.gr; Ioannis Nicolaou: Inicolao/at/pharm.auth.gr; Antonis Gavalas: vdem/at/pharm.auth.gr; George V Rekatas: vdem/at/pharm.auth.gr; Ekaterini Tani: vdem/at/pharm.auth.gr; Vassilis J Demopoulos: vdem/at/pharm.auth.gr
Received November 29, 2002; Accepted January 7, 2004.
Abstract
Background
Tardive dyskinesia (TD) is a major limitation of older antipsychotics. Newer antipsychotics have various other side effects such as weight gain, hyperglycemia, etc. In a previous study we have shown that an indolamine molecule expresses a moderate binding affinity at the dopamine D2 and serotonin 5-HT1A receptors in in vitro competition binding assays. In the present work, we tested its p-toluenesulfonyl derivative (TPBIA) for behavioral effects in rats, related to interactions with central dopamine receptors and its antioxidant activity.
Methods
Adult male Fischer-344 rats grouped as: i) Untreated rats: TPBIA was administered i.p. in various doses ii) Apomorphine-treated rats: were treated with apomorphine (1 mg kg-1, i.p.) 10 min after the administration of TPBIA. Afterwards the rats were placed individually in the activity cage and their motor behaviour was recorded for the next 30 min The antioxidant potential of TPBIA was investigated in the model of in vitro non enzymatic lipid peroxidation.
Results
i) In non-pretreated rats, TPBIA reduces the activity by 39 and 82% respectively, ii) In apomorphine pretreated rats, TPBIA reverses the hyperactivity and stereotype behaviour induced by apomorphine. Also TPBIA completely inhibits the peroxidation of rat liver microsome preparations at concentrations of 0.5, 0.25 and 0.1 mM.
Conclusion
TPBIA exerts dopamine antagonistic activity in the central nervous system. In addition, its antioxidant effect is a desirable property, since TD has been partially attributed, to oxidative stress. Further research is needed to test whether TPBIA may be used as an antipsychotic agent.
Articles from Annals of General Hospital Psychiatry are provided here courtesy of
BioMed Central