Pharmacological Evaluation of Halogenated and Non-halogenated Arylpiperazin-1-yl-ethyl-benzimidazoles as D2 and 5-HT2A Receptor Ligands
2011
Аутори:
Tomić, MirkoIgnjatović, Đurđica
Tovilović-Kovačević, Gordana
Andrić, Deana
Penjišević, Jelena
Kostić-Rajačić, Slađana
Тип документа:
Чланак у часопису (Објављена верзија)
,
© 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Метаподаци
Приказ свих података о документуАпстракт:
Five groups of previously synthesized and initially screened non-substituted and 4-halogenated arylpiperazin-1-yl-ethyl-benzimidazoles were estimated for their in-vitro binding affinities at the rat D2, 5-HT2A, and a1-adrenergic receptors. Among all these compounds, 2-methoxyphenyl and 2-chlorophenyl piperazines demonstrate the highest affinities for the tested receptors. The effects of 4-halogenation of benzimidazoles reveal that substitution with bromine may greatly increase the affinity of the compounds for the studied receptors, while the effect of substitution with chlorine is less remarkable. Most of the tested components show 5-HT2A/D2 pKi binding ratios slightly above or less than 1, while only 4-chloro-6-(2-{4-[3-(trifluoromethyl)phenyl]piperazin-1-yl}ethyl)-1H-benzimidazole expresses an appropriate higher binding ratio (1.14), which was indicated for atypical neuroleptics. This compound exhibits a non-cataleptic action in rats and prevents d-amphetamine-induced hyperlocomotion in mice, which suggest its atypical antipsychotic potency.
Кључне речи:
Arylpiperazines; Atypical antipsychotics; D2 receptors; 5-HT2A receptors; Pharmacological screeningИзвор:
Archiv der Pharmazie, 2011, 344, 5, 287-291Финансирање / пројекти:
- Биомедицинска испитивања и развој неких нових психотропних супстанци (RS-MESTD-MPN2006-2010-143032)
- Синтеза и карактеризација биолошки активних супстанци и компјутерска симулација биолошких система (RS-MESTD-MPN2006-2010-142009)
DOI: 10.1002/ardp.200900168
ISSN: 0365-6233
PubMed: 21509803