Advenier C, Girard V, Naline E, Vilain P, Emonds-Alt X
Laboratoire de Pharmacologie, Faculté de Médecine Paris-Ouest, France.
Eur J Pharmacol. 1993 Nov 30;250(1):169-71. doi: 10.1016/0014-2999(93)90637-w.
The antitussive effects of SR 48968, a non-peptide tachykinin NK2 receptor antagonist, were investigated on citric acid-induced cough in the unanesthetized guinea-pig and compared with the effects of codeine. SR 48968 (0.01-0.3 mg/kg i.p.) inhibited in a dose-dependent manner the number of coughs induced by inhalation of an aqueous solution of citric acid with an ED50 of 0.1 mg/kg (0.17 mumol/kg). Under similar conditions, the codeine ED50 was 8 mg/kg (27 mumol/kg). Naloxone, an opioid receptor antagonist, abolished the effects of codeine but did not modify the effects of SR 48968. These data suggest that NK2 receptor stimulation might play an important role in the regulation of the cough reflex and that SR 48968 could be a potential antitussive agent.
研究了非肽类速激肽NK2受体拮抗剂SR 48968对未麻醉豚鼠柠檬酸诱发咳嗽的镇咳作用，并与可待因的作用进行比较。SR 48968（0.01 - 0.3毫克/千克，腹腔注射）以剂量依赖性方式抑制吸入柠檬酸水溶液诱发的咳嗽次数，半数有效剂量（ED50）为0.1毫克/千克（0.17微摩尔/千克）。在类似条件下，可待因的ED50为8毫克/千克（27微摩尔/千克）。阿片受体拮抗剂纳洛酮消除了可待因的作用，但未改变SR 48968的作用。这些数据表明，NK2受体刺激可能在咳嗽反射调节中起重要作用，且SR 48968可能是一种潜在的镇咳剂。
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