Hydroxylated analogs of mexiletine as tools for structural-requirements investigation of the sodium channel blocking activity.
Arch Pharm (Weinheim)
; 343(6): 325-32, 2010 Jun.
Article
em En
| MEDLINE
| ID: mdl-20509146
[2-(2-Aminopropoxy)-1,3-phenylene]dimethanol 1 and 4-(2-aminopropoxy)-3-(hydroxymethyl)-5-methylphenol 2, two dihydroxylated analogs of mexiletine - a well known class IB anti-arrhythmic drug - were synthesized and used as pharmacological tools to investigate the blocking-activity requirements of human skeletal muscle, voltage-gated sodium channel. The very low blocking activity shown by newly synthesized compounds corroborates the hypothesis that the presence of a phenolic group in the para-position to the aromatic moiety and/or benzylic hydroxyl groups on the aromatic moiety of local anesthetic-like drugs impairs either the transport to or the interaction with the binding site in the pore of Na(+) channels.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Canais de Sódio
/
Bloqueadores dos Canais de Sódio
/
Mexiletina
/
Antiarrítmicos
Limite:
Humans
Idioma:
En
Revista:
Arch Pharm (Weinheim)
Ano de publicação:
2010
Tipo de documento:
Article
País de afiliação:
Itália
País de publicação:
Alemanha