Sinteza i farmakološko ispitivanje novih derivata N-(2-nitrofenil) piperazina
Synthesis and pharmacological evaluation of several N-(2-nitrophenyl) piperazine derivatives
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2007
Authors:
Andrić, DeanaTovilović-Kovačević, Gordana
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Roglić, Goran
Ignjatović, Đurđica
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Šoškić, Vukić
Tomić, Mirko
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Kostić-Rajačić, Slađana V.
Document Type:
Article (Published version)
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@ 2007 by the Serbian Chemical Society
Metadata
Show full item recordAbstract:
Six newly synthesized heterocyclic (2-nitrophenyl)piperazines, with a specific structure of the heteroaryl group, whichmimics the catechol moiety of dopamine (benzimidazoles and substituted benzimidazoles), were evaluated for their binding affinity to rat dopamine (DA), serotonin (5-HT) and _1 receptors. All compounds with a benzimidazole group had a 5-HT2A/D2 receptors binding ratio characteristic for atypical neuroleptics (>1, pK i values). Compound 7c, 4-bromo-6-{2-_4-(2-nitrophenyl)piperazin- 1-yl_ethyl}-1H-benzimidazole, expressed higher affinities for all receptor classes than clozapine. Also, it exhibited the best characteristic for atypical neuroleptics and presents a compound with the best profile for further in vivo investigations.
Keywords:
arylpiperazines; benzimidazoles; dopamine receptors; serotonin receptors; atypical antipsychoticSource:
Journal of the Serbian Chemical Society, 2007, 72, 5, 429-435
DOI: 10.2298/JSC0705429A
ISSN: 0352-5139