Pyridyl-phenyl ether monoamine reuptake inhibitors: Impact of lipophilicity on dual SNRI pharmacology and off-target promiscuity.
Bioorg Med Chem Lett
; 18(9): 2896-9, 2008 May 01.
Article
em En
| MEDLINE
| ID: mdl-18417343
ABSTRACT
A novel series of pyridyl-phenyl ethers are disclosed, which possess dual 5-HT and NA reuptake pharmacology with good selectivity over dopamine reuptake inhibition. An analysis of the relationship between lipophilicity and pharmacology highlighted that potent dual SNRI activity was only achievable at c log P>3.5. The series was found to possess significant polypharmacology issues, and we concluded that this off-target promiscuity was related to lipophilicity.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Éteres Fenílicos
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Piridinas
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Norepinefrina
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Inibidores Seletivos de Recaptação de Serotonina
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Hepatócitos
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Antagonistas do Receptor 5-HT1 de Serotonina
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Aminas
Limite:
Humans
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article