Two new phenylpiperazines with atypical antipsychotic potential
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2007
Authors
Tomić, MirkoIgnjatović, D.
Tovilović, Gordana
Andrić, Deana
Roglić, Goran
Kostić Rajačić, Slađana
Article (Published version)
Metadata
Show full item recordAbstract
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 receptorsSource:
Bioorganic and Medicinal Chemistry Letters, 2007, 17, 21, 5749-5753Publisher:
- Oxford : Pergamon-Elsevier Science Ltd
Funding / projects:
- 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: 10.1016/j.bmcl.2007.08.066
ISSN: 0960-894X
PubMed: 17870534
WoS: 000250287800003
Scopus: 2-s2.0-34648847078
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IHTMTY - JOUR AU - Tomić, Mirko AU - Ignjatović, D. AU - Tovilović, Gordana AU - Andrić, Deana AU - Roglić, Goran AU - Kostić Rajačić, Slađana PY - 2007 UR - https://cer.ihtm.bg.ac.rs/handle/123456789/354 AB - 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. PB - Oxford : Pergamon-Elsevier Science Ltd T2 - Bioorganic and Medicinal Chemistry Letters T1 - Two new phenylpiperazines with atypical antipsychotic potential VL - 17 IS - 21 SP - 5749 EP - 5753 DO - 10.1016/j.bmcl.2007.08.066 ER -
@article{ author = "Tomić, Mirko and Ignjatović, D. and Tovilović, Gordana and Andrić, Deana and Roglić, Goran and Kostić Rajačić, Slađana", year = "2007", 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.", publisher = "Oxford : Pergamon-Elsevier Science Ltd", journal = "Bioorganic and Medicinal Chemistry Letters", title = "Two new phenylpiperazines with atypical antipsychotic potential", volume = "17", number = "21", pages = "5749-5753", doi = "10.1016/j.bmcl.2007.08.066" }
Tomić, M., Ignjatović, D., Tovilović, G., Andrić, D., Roglić, G.,& Kostić Rajačić, S.. (2007). Two new phenylpiperazines with atypical antipsychotic potential. in Bioorganic and Medicinal Chemistry Letters Oxford : Pergamon-Elsevier Science Ltd., 17(21), 5749-5753. https://doi.org/10.1016/j.bmcl.2007.08.066
Tomić M, Ignjatović D, Tovilović G, Andrić D, Roglić G, Kostić Rajačić S. Two new phenylpiperazines with atypical antipsychotic potential. in Bioorganic and Medicinal Chemistry Letters. 2007;17(21):5749-5753. doi:10.1016/j.bmcl.2007.08.066 .
Tomić, Mirko, Ignjatović, D., Tovilović, Gordana, Andrić, Deana, Roglić, Goran, Kostić Rajačić, Slađana, "Two new phenylpiperazines with atypical antipsychotic potential" in Bioorganic and Medicinal Chemistry Letters, 17, no. 21 (2007):5749-5753, https://doi.org/10.1016/j.bmcl.2007.08.066 . .