Antitussive activity of iodo-resiniferatoxin in guinea pigs

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Abstract

Background: Iodo-resiniferatoxin (I-RTX) has recently been described as an ultra potent antagonist of the transient receptor potential vanilloid-1 (TRPV1). Methods: The ability of I-RTX to inhibit cough induced by inhalation of two putative TRPV1 stimulants (capsaicin and citric acid) was tested in non-anaesthetised guinea pigs. Results: Pretreatment with I-RTX either intraperitoneally (0.03-0.3 μmol/kg) or by aerosol (0.1-3 μM) reduced the number of coughs produced by inhalation of citric acid (0.25 M) and capsaicin (30 μM) in a dose dependent manner. Capsazepine (CPZ) also reduced citric acid and capsaicin induced cough, but the activity of I-RTX was 10-100 times more potent than CPZ in all the experimental conditions tested. Conclusions: I-RTX is a novel and potent antitussive drug which inhibits cough mediated by agents possibly acting via TRPV1 activation.

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Trevisani, M., Milan, A., Gatti, R., Zanasi, A., Harrison, S., Fontana, G., … Geppetti, P. (2004). Antitussive activity of iodo-resiniferatoxin in guinea pigs. Thorax, 59(9), 769–772. https://doi.org/10.1136/thx.2003.012930

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