Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential

Tomić, Mirko; Kundaković, M; Butorović, B; Janać, B; Andrić, Deana; Roglić, Goran; Ignjatović, D; Kostić Rajačić, Slađana

doi:10.1016/j.bmcl.2004.06.005

Authorized Users Only

2004

Authors

Tomić, Mirko
Kundaković, M
Butorović, B
Janać, B
Andrić, Deana

Roglić, Goran

Ignjatović, D
Kostić Rajačić, Slađana

Article (Published version)

Elsevier

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Abstract

Six active compounds, among previously synthesized and screened arylpiperazines, were selected and evaluated for the binding affinity to rat dopamine, serotonin and α 1 receptors. Two compounds with benztriazole group had a 5-HT 2A /D 2 binding ratio characteristic for atypical neuroleptics (>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-HT 2A and α1 receptors and a higher affinity for 5-HT 1A receptors than clozapine. Also, it exhibited the noncataleptic behavioural pattern of atypical antipsychotics and antagonized d-amphetamine-induced hyperlocomotion in rats. © 2004 Elsevier Ltd. All rights reserved.

Keywords:

Arylpiperazine / Dopamine receptors / Serotonin receptors

Source:
Bioorganic and Medicinal Chemistry Letters, 2004, 14, 16, 4263-4266

Publisher:

Elsevier

Funding / projects:

Ministry for Science, Technology and Development of Serbia, grants #1704 and #1698

DOI: 10.1016/j.bmcl.2004.06.005

ISSN: 0960-894X

PubMed: 15261283

WoS: 000222923300029

Scopus: 2-s2.0-3142691095

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TY  - JOUR
AU  - Tomić, Mirko
AU  - Kundaković, M
AU  - Butorović, B
AU  - Janać, B
AU  - Andrić, Deana
AU  - Roglić, Goran
AU  - Ignjatović, D
AU  - Kostić Rajačić, Slađana
PY  - 2004
UR  - https://cer.ihtm.bg.ac.rs/handle/123456789/2820
AB  - Six active compounds, among previously synthesized and screened arylpiperazines, were selected and evaluated for the binding affinity to rat dopamine, serotonin and α 1 receptors. Two compounds with benztriazole group had a 5-HT 2A /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-HT 2A and α1 receptors and a higher affinity for 5-HT 1A receptors than clozapine. Also, it exhibited the noncataleptic behavioural pattern of atypical antipsychotics and antagonized d-amphetamine-induced hyperlocomotion in rats. © 2004 Elsevier Ltd. All rights reserved.
PB  - Elsevier
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 = "Tomić, Mirko and Kundaković, M and Butorović, B and Janać, B and Andrić, Deana and Roglić, Goran and Ignjatović, D 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 α 1 receptors. Two compounds with benztriazole group had a 5-HT 2A /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-HT 2A and α1 receptors and a higher affinity for 5-HT 1A receptors than clozapine. Also, it exhibited the noncataleptic behavioural pattern of atypical antipsychotics and antagonized d-amphetamine-induced hyperlocomotion in rats. © 2004 Elsevier Ltd. All rights reserved.",
publisher = "Elsevier",
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"
}

Tomić, M., Kundaković, M., Butorović, B., Janać, B., Andrić, D., Roglić, G., Ignjatović, D.,& Kostić Rajačić, S.. (2004). Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential. in Bioorganic and Medicinal Chemistry Letters
Elsevier., 14(16), 4263-4266.
https://doi.org/10.1016/j.bmcl.2004.06.005

Tomić M, Kundaković M, Butorović B, Janać B, Andrić D, Roglić G, Ignjatović D, 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 .

Tomić, Mirko, Kundaković, M, Butorović, B, Janać, B, Andrić, Deana, Roglić, Goran, Ignjatović, D, 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 . .