Ontology highlight
ABSTRACT:
SUBMITTER: Nyman E
PROVIDER: S-EPMC3565573 | biostudies-literature | 2013
REPOSITORIES: biostudies-literature
Nyman Eva E Franzén Bo B Nolting Andreas A Klement Göran G Liu Gang G Nilsson Maria M Rosén Annika A Björk Charlotta C Weigelt Dirk D Wollberg Patrik P Karila Paul P Raboisson Patrick P
Journal of pain research 20130130
AZ465 is a novel selective transient receptor potential cation channel, member A1 (TRPA1) antagonist identified during a focused drug discovery effort. In vitro, AZ465 fully inhibits activation by zinc, O-chlorobenzylidene malononitrile (CS), or cinnamaldehyde of the human TRPA1 channel heterologously expressed in human embryonic kidney cells. Our data using patch-clamp recordings and mouse/human TRPA1 chimeras suggest that AZ465 binds reversibly in the pore region of the human TRPA1 channel. Fi ...[more]