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Two new phenylpiperazines with atypical antipsychotic potential

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2007
Authors
Tomić, Mirko
Ignjatović, D.
Tovilović, Gordana
Andrić, Deana
Roglić, Goran
Kostić Rajačić, Slađana
Article (Published version)
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Abstract
Two new series of substituted arylpiperazines with heterocyclic 3-propoxy-benzimidazole or 3-propoxy-benzimidazole-2-thione groups were synthesized and their in vitro binding affinities for the D2, 5-HT1A, 5-HT2A, and α1-adrenergic receptors determined. Among them, only two compounds with phenyl aryl-constituent (8a and 9a) showed 5-HT2A/D2 pKi binding ratios proposed for atypical neuroleptics. As to their behavioral screening on rodents, both compounds exhibited a non-cataleptic action in rats and antagonized d-amphetamine-induced hyperlocomotion in mice, suggesting their possible atypical antipsychotic potency.
Keywords:
Arylpiperazines / Atypical antipsychotics / Dopamine receptors / Serotonin receptors
Source:
Bioorganic and Medicinal Chemistry Letters, 2007, 17, 21, 5749-5753
Publisher:
  • Pergamon-Elsevier Science Ltd, Oxford
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: 10.1016/j.bmcl.2007.08.066

ISSN: 0960-894X

PubMed: 17870534

WoS: 000250287800003

Scopus: 2-s2.0-34648847078
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URI
http://cer.ihtm.bg.ac.rs/handle/123456789/354
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IHTM

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