Synthesis and antidepressant effect of novel aralkyl piperazine and piperidine derivatives targeting SSRI/5-HT1A/5-HT7.
Bioorg Med Chem Lett
; 29(23): 126703, 2019 12 01.
Article
em En
| MEDLINE
| ID: mdl-31627993
ABSTRACT
A series of novel aralkyl piperazine and piperidine derivatives were synthesized, and evaluated for their serotonin reuptake inhibitory and 5-HT1A/5-HT7 receptors affinities activity. Antidepressant activities in vivo of the selective compound were screened using the forced swimming test (FST) and tail suspension test (TST). The results indicated that compound 19a exhibited high affinities for the 5-HT1A/5-HT7 receptors (5-HT1A, Kiâ¯=â¯12â¯nM; 5-HT7, Kiâ¯=â¯3.2â¯nM) coupled with potent serotonin reuptake inhibition (IC50â¯=â¯14â¯nM) and showed a marked antidepressant-like effect in the FST and TST models.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piperidinas
/
Inibidores Seletivos de Recaptação de Serotonina
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Piperazina
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Antidepressivos
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2019
Tipo de documento:
Article