Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential
Samo za registrovane korisnike
2004
Autori
Tomic, MKundakovic, M
Butorovi, B
Janac, B
Andrić, Deana
Roglić, Goran
Ignjatović, Đurđica
Kostić-Rajačić, Slađana
Članak u časopisu (Objavljena verzija)
Metapodaci
Prikaz svih podataka o dokumentuApstrakt
Six active compounds, among previously synthesized and screened arylpiperazines, were selected and evaluated for the binding affinity to rat dopamine, serotonin and alpha(1) receptors. Two compounds with benztriazole group had a 5-HT2A/D-2 binding ratio characteristic for atypical neuroleptics ( gt 1, pK(i) values). Compound 2, 5-{2-[4-(2,3-dimethyl-phenyl)-piperazin-1-yl]ethyl}1H-benzotriazole, expressed clozapine-like in vitro binding profile at D-2, 5-HT2A and alpha1 receptors and a higher affinity for 5-HT1A receptors than clozapine. Also, it exhibited the noncataleptic behavioural pattern of atypical antipsychotics and antagonized d-amphetamine-induced hyperlocomotion in rats. (C) 2004 Elsevier Ltd. All rights reserved.
Ključne reči:
arylpiperazine / dopamine receptors / serotonin receptors / atypical antipsychoticIzvor:
Bioorganic and Medicinal Chemistry Letters, 2004, 14, 16, 4263-4266Izdavač:
- Pergamon-Elsevier Science Ltd, Oxford
DOI: 10.1016/j.bmcl.2004.06.005
ISSN: 0960-894X
PubMed: 15261283
WoS: 000222923300029
Scopus: 2-s2.0-3142691095
Kolekcije
Institucija/grupa
Hemijski fakultet / Faculty of ChemistryTY - JOUR AU - Tomic, M AU - Kundakovic, M AU - Butorovi, B AU - Janac, B AU - Andrić, Deana AU - Roglić, Goran AU - Ignjatović, Đurđica AU - Kostić-Rajačić, Slađana PY - 2004 UR - https://cherry.chem.bg.ac.rs/handle/123456789/652 AB - Six active compounds, among previously synthesized and screened arylpiperazines, were selected and evaluated for the binding affinity to rat dopamine, serotonin and alpha(1) receptors. Two compounds with benztriazole group had a 5-HT2A/D-2 binding ratio characteristic for atypical neuroleptics ( gt 1, pK(i) values). Compound 2, 5-{2-[4-(2,3-dimethyl-phenyl)-piperazin-1-yl]ethyl}1H-benzotriazole, expressed clozapine-like in vitro binding profile at D-2, 5-HT2A and alpha1 receptors and a higher affinity for 5-HT1A receptors than clozapine. Also, it exhibited the noncataleptic behavioural pattern of atypical antipsychotics and antagonized d-amphetamine-induced hyperlocomotion in rats. (C) 2004 Elsevier Ltd. All rights reserved. PB - Pergamon-Elsevier Science Ltd, Oxford T2 - Bioorganic and Medicinal Chemistry Letters T1 - Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential VL - 14 IS - 16 SP - 4263 EP - 4266 DO - 10.1016/j.bmcl.2004.06.005 ER -
@article{ author = "Tomic, M and Kundakovic, M and Butorovi, B and Janac, B and Andrić, Deana and Roglić, Goran and Ignjatović, Đurđica and Kostić-Rajačić, Slađana", year = "2004", abstract = "Six active compounds, among previously synthesized and screened arylpiperazines, were selected and evaluated for the binding affinity to rat dopamine, serotonin and alpha(1) receptors. Two compounds with benztriazole group had a 5-HT2A/D-2 binding ratio characteristic for atypical neuroleptics ( gt 1, pK(i) values). Compound 2, 5-{2-[4-(2,3-dimethyl-phenyl)-piperazin-1-yl]ethyl}1H-benzotriazole, expressed clozapine-like in vitro binding profile at D-2, 5-HT2A and alpha1 receptors and a higher affinity for 5-HT1A receptors than clozapine. Also, it exhibited the noncataleptic behavioural pattern of atypical antipsychotics and antagonized d-amphetamine-induced hyperlocomotion in rats. (C) 2004 Elsevier Ltd. All rights reserved.", publisher = "Pergamon-Elsevier Science Ltd, Oxford", journal = "Bioorganic and Medicinal Chemistry Letters", title = "Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential", volume = "14", number = "16", pages = "4263-4266", doi = "10.1016/j.bmcl.2004.06.005" }
Tomic, M., Kundakovic, M., Butorovi, B., Janac, B., Andrić, D., Roglić, G., Ignjatović, Đ.,& Kostić-Rajačić, S.. (2004). Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential. in Bioorganic and Medicinal Chemistry Letters Pergamon-Elsevier Science Ltd, Oxford., 14(16), 4263-4266. https://doi.org/10.1016/j.bmcl.2004.06.005
Tomic M, Kundakovic M, Butorovi B, Janac B, Andrić D, Roglić G, Ignjatović Đ, Kostić-Rajačić S. Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential. in Bioorganic and Medicinal Chemistry Letters. 2004;14(16):4263-4266. doi:10.1016/j.bmcl.2004.06.005 .
Tomic, M, Kundakovic, M, Butorovi, B, Janac, B, Andrić, Deana, Roglić, Goran, Ignjatović, Đurđica, Kostić-Rajačić, Slađana, "Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential" in Bioorganic and Medicinal Chemistry Letters, 14, no. 16 (2004):4263-4266, https://doi.org/10.1016/j.bmcl.2004.06.005 . .