New 3-[4-(3-substituted phenyl)piperazin-1-yl]-1-(benzo[b]thiophen-3-yl)propanol derivatives with dual action at 5-HT1A serotonin receptors and serotonin transporter as a new class of antidepressants.
Pharmazie
; 57(8): 515-8, 2002 Aug.
Article
em En
| MEDLINE
| ID: mdl-12227188
ABSTRACT
In this paper a series of new 3-[4-(3-substituted phenyl)piperazin-1-yl]-1-(benzo[b]thiophen-3-yl)propanol derivatives is presented as a new class of antidepressant drugs with dual activity at 5-HT1A serotonin receptors and serotonin transporter. The 5-HT1A receptor and 5-HT transporter binding affinities of hydroxylic compounds 4 a-e have been determined. The new compounds present nanomolar affinity for both activities, and 1-(benzo[b]thiophen-3-yl)-3-[4-(3-methoxyphenyl)piperazin-1-yl]propan-1-ol (4d) shows values (nM) of Ki = 86 for 5-HT1A receptors and Ki = 76 for the serotonin transporter, respectively.
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Base de dados:
MEDLINE
Assunto principal:
Proteínas de Membrana Transportadoras
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Tiofenos
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Glicoproteínas de Membrana
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Proteínas de Transporte
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Receptores de Serotonina
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Antidepressivos de Segunda Geração
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Propanóis
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Proteínas do Tecido Nervoso
Idioma:
En
Ano de publicação:
2002
Tipo de documento:
Article