速激肽受体拮抗剂与咳嗽

C. Advenier , X. Emonds-Alt
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引用次数: 26

摘要

目前已有几种有效的选择性速激肽受体拮抗剂,它们是研究速激肽生理和病理作用以及确定参与其作用的受体类型的有力工具。事实上,大量研究表明,速激肽nk2受体拮抗剂(SR 48968, MEN 10627)能够抑制未麻醉豚鼠中柠檬酸、辣椒素或过敏原刺激或猫气管机械刺激引起的咳嗽。速激肽nk1受体拮抗剂的作用仍有争议,而速激肽nk3受体拮抗剂SR 142801对柠檬酸诱导的豚鼠咳嗽的抑制作用已被报道。对不穿过血脑屏障的速激肽受体拮抗剂的实验表明,速激肽受体拮抗剂的作用部位很可能是外周的,但中枢作用,至少在不受血脑屏障保护的区域,不能排除。最后,速激肽nk2受体的刺激似乎与咳嗽反射的致敏有关。
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Tachykinin Receptor Antagonists and Cough

Several potent and selective antagonists for tachykinin receptors are now available and appear as powerful tools to investigate the physiological and pathological roles of tachykinins and to identify the type of receptor involved in their effect. Indeed, a lot of studies have shown that tachykinin NK2receptor antagonists (SR 48968, MEN 10627) are able to inhibit cough induced by citric acid, capsaicin or allergen challenge in the unanesthetized guinea-pig or mechanical stimulation of the trachea in the cat. The effects of tachykinin NK1receptor antagonists are still debated, whereas an inhibitory effect of SR 142801, a tachykinin NK3receptor antagonist, has been reported against citric acid-induced cough in the guinea-pig. Experiments with tachykinin receptor antagonists which do not cross the blood brain barrier suggest that the site of action of tachykinin receptor antagonists is most probably peripheral, but a central action, at least in an area not protected by the blood brain barrier, cannot be excluded. Finally, tachykinin NK2receptor stimulation seems to be involved in sensitisation of cough reflex.

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