Pharmacological Evaluation of Halogenated and Non-halogenated Arylpiperazin-1-yl-ethyl-benzimidazoles as D2 and 5-HT2A Receptor Ligands
Samo za registrovane korisnike
2011
Autori
Tomic, MirkoVaskovic, Djurdjica
Tovilović, Gordana
Andrić, Deana
Penjišević, Jelena
Kostić-Rajačić, Slađana
Članak u časopisu (Objavljena verzija)
Metapodaci
Prikaz svih podataka o dokumentuApstrakt
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 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/D2 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 hyperl...ocomotion in mice, which suggest its atypical antipsychotic potency.
Ključne reči:
Arylpiperazines / Atypical antipsychotics / D2 receptors / 5-HT2A receptors / Pharmacological screeningIzvor:
Archiv der Pharmazie, 2011, 344, 5, 287-291Izdavač:
- Wiley-Blackwell, Malden
Finansiranje / projekti:
- Biomedicinska ispitivanja i razvoj nekih novih psihotropnih supstanci (RS-MESTD-MPN2006-2010-143032)
- Sinteza i karakterizacija biološki aktivnih supstanci i kompjuterska simulacija bioloških sistema (RS-MESTD-MPN2006-2010-142009)
DOI: 10.1002/ardp.200900168
ISSN: 0365-6233
PubMed: 21509803
WoS: 000290441500002
Scopus: 2-s2.0-79955416905
Kolekcije
Institucija/grupa
Hemijski fakultet / Faculty of ChemistryTY - JOUR AU - Tomic, Mirko AU - Vaskovic, Djurdjica AU - Tovilović, Gordana AU - Andrić, Deana AU - Penjišević, Jelena AU - Kostić-Rajačić, Slađana PY - 2011 UR - https://cherry.chem.bg.ac.rs/handle/123456789/1337 AB - 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 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/D2 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 hyperlocomotion in mice, which suggest its atypical antipsychotic potency. PB - Wiley-Blackwell, Malden T2 - Archiv der Pharmazie T1 - Pharmacological Evaluation of Halogenated and Non-halogenated Arylpiperazin-1-yl-ethyl-benzimidazoles as D2 and 5-HT2A Receptor Ligands VL - 344 IS - 5 SP - 287 EP - 291 DO - 10.1002/ardp.200900168 ER -
@article{ author = "Tomic, Mirko and Vaskovic, Djurdjica and Tovilović, Gordana and Andrić, Deana and Penjišević, Jelena and Kostić-Rajačić, Slađana", year = "2011", 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 D2, 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/D2 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 hyperlocomotion in mice, which suggest its atypical antipsychotic potency.", publisher = "Wiley-Blackwell, Malden", journal = "Archiv der Pharmazie", title = "Pharmacological Evaluation of Halogenated and Non-halogenated Arylpiperazin-1-yl-ethyl-benzimidazoles as D2 and 5-HT2A Receptor Ligands", volume = "344", number = "5", pages = "287-291", doi = "10.1002/ardp.200900168" }
Tomic, M., Vaskovic, D., Tovilović, G., Andrić, D., Penjišević, J.,& Kostić-Rajačić, S.. (2011). Pharmacological Evaluation of Halogenated and Non-halogenated Arylpiperazin-1-yl-ethyl-benzimidazoles as D2 and 5-HT2A Receptor Ligands. in Archiv der Pharmazie Wiley-Blackwell, Malden., 344(5), 287-291. https://doi.org/10.1002/ardp.200900168
Tomic M, Vaskovic D, Tovilović G, Andrić D, Penjišević J, Kostić-Rajačić S. Pharmacological Evaluation of Halogenated and Non-halogenated Arylpiperazin-1-yl-ethyl-benzimidazoles as D2 and 5-HT2A Receptor Ligands. in Archiv der Pharmazie. 2011;344(5):287-291. doi:10.1002/ardp.200900168 .
Tomic, Mirko, Vaskovic, Djurdjica, Tovilović, Gordana, Andrić, Deana, Penjišević, Jelena, Kostić-Rajačić, Slađana, "Pharmacological Evaluation of Halogenated and Non-halogenated Arylpiperazin-1-yl-ethyl-benzimidazoles as D2 and 5-HT2A Receptor Ligands" in Archiv der Pharmazie, 344, no. 5 (2011):287-291, https://doi.org/10.1002/ardp.200900168 . .