Inhibition of sensory neuronal TRPs contributes to anti-nociception by butamben.

Article Details

Citation

Copy to clipboard

Bang S, Yang TJ, Yoo S, Heo TH, Hwang SW

Inhibition of sensory neuronal TRPs contributes to anti-nociception by butamben.

Neurosci Lett. 2012 Jan 11;506(2):297-302. doi: 10.1016/j.neulet.2011.11.026. Epub 2011 Nov 23.

PubMed ID

22133806 [ View in PubMed

]

Abstract

Butamben (n-butyl-p-aminobenzoic acid) is a pain-relieving local anesthetic for topical use. Blockade of voltage-gated channel expressed in the peripheral sensory neurons has been suggested as a mechanism of action. Its effects on another sensory neuronal channel family, transient receptor potential (TRP) have remained unclear. In this study we attempted to address this question using six sensory neuronal TRP channel-expressing heterologous systems, cultured sensory neurons and TRP-mediated acute animal pain tests. In Ca(2+) imaging and whole cell electrophysiology, TRPA1 and TRPV4 were blocked by micromolar butamben. Butamben also activated TRPA1 at millimolar concentrations. The inhibitory effects on the two TRP channels were reproducible in sensory neurons. Moreover, butamben attenuated acute animal pain behaviors in a TRPA1- or TRPV4-dependent manner. Para-aminobenzoic acid (PABA), an analog of a simpler chemical structure, displayed similar in vitro and in vivo properties, suggestive that chemical structure is important for the two TRP-specificity. Our findings suggest that inhibition of TRPA1 and TRPV4 contribute to the peripheral analgesic mechanisms of butamben.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Butamben	Transient receptor potential cation channel subfamily A member 1	Protein	Humans	Unknown	Inhibitor	Details
Butamben	Transient receptor potential cation channel subfamily V member 4	Protein	Humans	Unknown	Inhibitor	Details