Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential
2004
Аутори:
Tomić, MirkoKundaković, Marija
Butorović, Biljana
Petković, Branka
Andrić, Deana
Roglić, Goran
Ignjatović, Đurđica
Kostić-Rajačić, Slađana
Тип документа:
Чланак у часопису (Објављена верзија)
,
© 2004 Elsevier Ltd.
Метаподаци
Приказ свих података о документуАпстракт:
Six active compounds, among previously synthesized and screened arylpiperazines, were selected and evaluated for the binding affinity to rat dopamine, serotonin and alpha(1) receptors. Two compounds with benztriazole group had a 5-HT2A/D-2 binding ratio characteristic for atypical neuroleptics (>1, pK(i) values). Compound 2, 5-{2-[4-(2,3-dimethyl-phenyl)-piperazin-1-yl]ethyl}1H-benzotriazole, expressed clozapine-like in vitro binding profile at D-2, 5-HT2A and alpha1 receptors and a higher affinity for 5-HT1A receptors than clozapine. Also, it exhibited the noncataleptic behavioural pattern of atypical antipsychotics and antagonized d-amphetamine-induced hyperlocomotion in rats.
Кључне речи:
Arylpiperazine; Dopamine receptors; Serotonin receptors; Atypical antipsychoticИзвор:
Bioorganic and Medicinal Chemistry Letters, 2004, 14, 16, 4263-4266Финансирање / пројекти:
- Ministry of Science, Technology and Development of the Republic of Serbia (Contract #1704)
- Ministry of Science, Technology and Development of the Republic of Serbia (Contract #1698)
DOI: 10.1016/j.bmcl.2004.06.005
ISSN: 0960-894X
PubMed: 15261283