Arylglycine derivatives as potent transient receptor potential melastatin 8 (TRPM8) antagonists.
Bioorg Med Chem Lett
; 23(7): 2234-7, 2013 Apr 01.
Article
em En
| MEDLINE
| ID: mdl-23411075
ABSTRACT
A series of arylglycine-based analogs was synthesized and tested for TRPM8 antagonism in a cell-based functional assay. Following structure-activity relationship studies in vitro, a number of compounds were identified as potent TRPM8 antagonists and were subsequently evaluated in an in vivo pharmacodynamic assay of icilin-induced 'wet-dog' shaking in which compound 12 was fully effective. TRPM8 antagonists of the type described here may be useful in treating pain conditions wherein cold hypersensitivity is a dominant feature.
Texto completo:
1
Bases de dados:
MEDLINE
Assunto principal:
Canais de Cátion TRPM
/
Glicina
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2013
Tipo de documento:
Article
País de afiliação:
Estados Unidos