Trevisani M, Milan A, Gatti R, Zanasi A, Harrison S, Fontana G, Morice A H, Geppetti P
Center of Excellence for the Study of Inflammation, University of Ferrara, Ferrara, Italy.
Thorax. 2004 Sep;59(9):769-72. doi: 10.1136/thx.2003.012930.
Iodo-resiniferatoxin (I-RTX) has recently been described as an ultra potent antagonist of the transient receptor potential vanilloid-1 (TRPV1).
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.
Pretreatment with I-RTX either intraperitoneally (0.03-0.3 micromol/kg) or by aerosol (0.1-3 microM) reduced the number of coughs produced by inhalation of citric acid (0.25 M) and capsaicin (30 microM) 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.
I-RTX is a novel and potent antitussive drug which inhibits cough mediated by agents possibly acting via TRPV1 activation.
碘代树脂毒素(I-RTX)最近被描述为瞬时受体电位香草酸亚型1(TRPV1)的超效拮抗剂。
在未麻醉的豚鼠中测试了I-RTX抑制吸入两种假定的TRPV1刺激剂(辣椒素和柠檬酸)所诱发咳嗽的能力。
腹膜内(0.03 - 0.3微摩尔/千克)或通过气雾剂(0.1 - 3微摩尔)给予I-RTX预处理,以剂量依赖方式减少了吸入柠檬酸(0.25摩尔)和辣椒素(30微摩尔)所产生的咳嗽次数。辣椒素拮抗剂(CPZ)也减少了柠檬酸和辣椒素诱发的咳嗽,但在所有测试的实验条件下,I-RTX的活性比CPZ强10 - 100倍。
I-RTX是一种新型强效镇咳药,可抑制可能通过TRPV1激活起作用的药物介导的咳嗽。