The TRPA1 channel mediates the analgesic action of dipyrone and pyrazolone derivatives.

ABSTRACT:

Background and purpose

Although still used by hundreds of millions of people worldwide, the mechanism of the analgesic action of the pyrazolone derivatives (PDs), dipyrone, propyphenazone and antipyrine remains unknown. The transient receptor potential ankyrin 1 (TRPA1) channel, expressed by nociceptors, is emerging as a major pain transduction pathway. We hypothesized that PDs target the TRPA1 channel and by this mechanism produce their analgesic effect.

Experimental approach

Calcium responses and currents were studied in cultured TRPA1-expressing rodent dorsal root ganglion neurons and human cells. Acute nociception and mechanical hypersensitivity were investigated in naïve and genetically manipulated mice.

Key results

Pyrazolone and PDs selectively inhibited calciu

SUBMITTER: Nassini R 

PROVIDER: S-EPMC4500374 | biostudies-literature | 2015 Jul

REPOSITORIES: biostudies-literature