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Pharmacological Evaluation of Halogenated and Non-halogenated Arylpiperazin-1-yl-ethyl-benzimidazoles as D-2 and 5-HT2A Receptor Ligands

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2011
Authors
Tomić, Mirko
Vaskovic, Djurdjica
Tovilović, Gordana
Andrić, Deana
Penjišević, Jelena
Kostić Rajačić, Slađana
Article (Published version)
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Abstract
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 D-2, 5-HT2A, and alpha(1)-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 brominemay 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/D-2 pK(i) 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 hype...rlocomotion in mice, which suggest its atypical antipsychotic potency.

Keywords:
Arylpiperazines / Atypical antipsychotics / D-2 receptors / 5-HT2A receptors / Pharmacological screening
Source:
Archiv der Pharmazie, 2011, 344, 5, 287-291
Publisher:
  • Wiley-Blackwell, Malden
Projects:
  • Biomedicinska ispitivanja i razvoj nekih novih psihotropnih supstanci (RS-143032)
  • Sinteza i karakterizacija biološki aktivnih supstanci i kompjuterska simulacija bioloških sistema (RS-142009)

DOI: 10.1002/ardp.200900168

ISSN: 0365-6233

PubMed: 21509803

WoS: 000290441500002

Scopus: 2-s2.0-79955416905
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URI
http://cer.ihtm.bg.ac.rs/handle/123456789/916
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