Synthesis of new 4-butyl-arylpiperazine-3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives and evaluation for their 5-HT1A and D2 receptor affinity and serotonin transporter inhibition.
Bioorg Chem
; 97: 103662, 2020 04.
Article
em En
| MEDLINE
| ID: mdl-32086055
ABSTRACT
A series of novel 4-butyl-arylpiperazine-3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives were synthesized and evaluated for their 5-HT1A/D2 receptor affinity and serotonin reuptake inhibition. The compounds exhibited high affinity for the 5-HT1A receptor, (especially 4dKi = 0.4 nM) which depended on the substitution pattern at the phenylpiperazine moiety. From this series screen, compound 4c emerged with promising mixed receptor profiles for the 5-HT1A/D2 receptors and the serotonin transporter (Ki = 1.3 nM, 182 nM and 64 nM, respectively).
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MEDLINE
Assunto principal:
Pirrolidinas
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Inibidores Seletivos de Recaptação de Serotonina
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Receptores de Dopamina D2
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Receptor 5-HT1A de Serotonina
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article