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Synthesis and dopaminergic features of six novel 3-arylpiperidines

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Authors
Kostić Rajačić, Slađana
Šoškić, Vukić
Joksimovic, J
Article (Published version)
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Abstract
Four substituted 3-aryl-1-{2-[5-(1H-benzimidazole)]ethyl}piperidines and two 3-aryl-1-{2-[6-(1,4-dihydroxyquinoxaline-2,3-dione)]ethyl} piperidines were synthesized, characterized and evaluated for in vitro binding affinity at the D1 and D2 dopamine and 5-HT1A serotonin receptors using synaptosomal membranes of fresh bovine caudate nuclei and hippocampi as a source of the dopamine and serotonin receptors, respectively, and the corresponding specific radioligands. All six novel compounds expressed no binding affinity at the D1 and 5-HT1A receptors. Derivatives of 1,4- dihydroxyquinoxaline-2,3-dione (compounds 8a and 8b) and of 2- dihalomethylbenzimidazole (ligands 9 and 10) were moderate competitors of [ 3 H]spiperone binding at the D2 dopamine receptors. However, benzimidazole- 2-thiones (compounds 7a and 7b) behaved as selective D2 receptor ligands with the binding affinity in the nanomolar range of concentrations.
Keywords:
binding affinity / Dopamine Agents / Dopamine Receptors / Piperidines / serotoninergic system
Source:
Bollettino Chimico Farmaceutico, 1998, 137, 10, 417-421

ISSN: 0006-6648

PubMed: 10025971

Scopus: 2-s2.0-0032406630
[ Google Scholar ]
Handle
https://hdl.handle.net/21.15107/rcub_cer_2826
URI
https://cer.ihtm.bg.ac.rs/handle/123456789/2826
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  • Radovi istraživača / Researchers' publications
Institution/Community
IHTM
TY  - JOUR
AU  - Kostić Rajačić, Slađana
AU  - Šoškić, Vukić
AU  - Joksimovic, J
PY  - 1998
UR  - https://cer.ihtm.bg.ac.rs/handle/123456789/2826
AB  - Four substituted 3-aryl-1-{2-[5-(1H-benzimidazole)]ethyl}piperidines and two 3-aryl-1-{2-[6-(1,4-dihydroxyquinoxaline-2,3-dione)]ethyl} piperidines were synthesized, characterized and evaluated for in vitro binding affinity at the D1 and D2 dopamine and 5-HT1A serotonin receptors using synaptosomal membranes of fresh bovine caudate nuclei and hippocampi as a source of the dopamine and serotonin receptors, respectively, and the corresponding specific radioligands. All six novel compounds expressed no binding affinity at the D1 and 5-HT1A receptors. Derivatives of 1,4- dihydroxyquinoxaline-2,3-dione (compounds 8a and 8b) and of 2- dihalomethylbenzimidazole (ligands 9 and 10) were moderate competitors of [ 3 H]spiperone binding at the D2 dopamine receptors. However, benzimidazole- 2-thiones (compounds 7a and 7b) behaved as selective D2 receptor ligands with the binding affinity in the nanomolar range of concentrations.
T2  - Bollettino Chimico Farmaceutico
T1  - Synthesis and dopaminergic features of six novel 3-arylpiperidines
VL  - 137
IS  - 10
SP  - 417
EP  - 421
UR  - https://hdl.handle.net/21.15107/rcub_cer_2826
ER  - 
@article{
author = "Kostić Rajačić, Slađana and Šoškić, Vukić and Joksimovic, J",
year = "1998",
abstract = "Four substituted 3-aryl-1-{2-[5-(1H-benzimidazole)]ethyl}piperidines and two 3-aryl-1-{2-[6-(1,4-dihydroxyquinoxaline-2,3-dione)]ethyl} piperidines were synthesized, characterized and evaluated for in vitro binding affinity at the D1 and D2 dopamine and 5-HT1A serotonin receptors using synaptosomal membranes of fresh bovine caudate nuclei and hippocampi as a source of the dopamine and serotonin receptors, respectively, and the corresponding specific radioligands. All six novel compounds expressed no binding affinity at the D1 and 5-HT1A receptors. Derivatives of 1,4- dihydroxyquinoxaline-2,3-dione (compounds 8a and 8b) and of 2- dihalomethylbenzimidazole (ligands 9 and 10) were moderate competitors of [ 3 H]spiperone binding at the D2 dopamine receptors. However, benzimidazole- 2-thiones (compounds 7a and 7b) behaved as selective D2 receptor ligands with the binding affinity in the nanomolar range of concentrations.",
journal = "Bollettino Chimico Farmaceutico",
title = "Synthesis and dopaminergic features of six novel 3-arylpiperidines",
volume = "137",
number = "10",
pages = "417-421",
url = "https://hdl.handle.net/21.15107/rcub_cer_2826"
}
Kostić Rajačić, S., Šoškić, V.,& Joksimovic, J.. (1998). Synthesis and dopaminergic features of six novel 3-arylpiperidines. in Bollettino Chimico Farmaceutico, 137(10), 417-421.
https://hdl.handle.net/21.15107/rcub_cer_2826
Kostić Rajačić S, Šoškić V, Joksimovic J. Synthesis and dopaminergic features of six novel 3-arylpiperidines. in Bollettino Chimico Farmaceutico. 1998;137(10):417-421.
https://hdl.handle.net/21.15107/rcub_cer_2826 .
Kostić Rajačić, Slađana, Šoškić, Vukić, Joksimovic, J, "Synthesis and dopaminergic features of six novel 3-arylpiperidines" in Bollettino Chimico Farmaceutico, 137, no. 10 (1998):417-421,
https://hdl.handle.net/21.15107/rcub_cer_2826 .

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