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J Med Chem ; 60(3): 1076-1088, 2017 02 09.
Artículo en Inglés | MEDLINE | ID: mdl-28051863

RESUMEN

The TWIK-related K+ channel, TREK-1, has recently emerged as an attractive therapeutic target for the development of a novel class of analgesic drugs, suggesting that activation of TREK-1 could result in pain inhibition. Here, we report the synthesis of a series of substituted acrylic acids (1-54) based on our previous work with caffeate esters. The analogues were evaluated for their ability to modulate TREK-1 channel by electrophysiology and for their in vivo antinociceptive activity (acetic acid-induced writhing and hot plate assays), leading to the identification of a series of novel molecules able to activate TREK-1 and displaying potent antinociceptive activity in vivo. Furyl analogue 36 is the most promising of the series.


Asunto(s)
Analgésicos/farmacología , Canales de Potasio de Dominio Poro en Tándem/agonistas , Animales
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