ANTITUSSIVE EFFECT OF SR 48968, A NONPEPTIDE TACHYKININ NK(2) RECEPTOR ANTAGONIST

被引:55
作者
ADVENIER, C [1 ]
GIRARD, V [1 ]
NALINE, E [1 ]
VILAIN, P [1 ]
EMONDSALT, X [1 ]
机构
[1] SANOFI RECH,F-34184 MONTPELLIER,FRANCE
关键词
TACHYKININ NK2 RECEPTOR; SR; 48968; ANTITUSSIVE EFFECT; COUGH REFLEX; CITRIC ACID; (GUINEA-PIG);
D O I
10.1016/0014-2999(93)90637-W
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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 48908 could be a potential antitussive agent.
引用
收藏
页码:169 / 171
页数:3
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