Antitussive activity of the tachykinin NK1 receptor antagonist, CP-99994, in dogs
Antitussive activity of the tachykinin NK1 receptor antagonist, CP-99994, in dogs
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DOI：
10.1016/j.ejphar.2003.11.048
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发表时间：
2004-02-06
影响因子：
5
通讯作者：
Hey, JA
中科院分区：
文献类型：
--
作者：
Chapman, RW;House, A;Hey, JA
CP-99994 [(+)-(2S,3S)-3-（2-甲氧基苄基氨基）-2-苯基哌啶]是一种选择性速激肽NK1受体拮抗剂，可抑制豚鼠和猫的咳嗽。本研究考察了CP-99994对机械刺激犬胸内气管产生的止咳作用。CP-99994 （10 mg/kg, p.o）在第2 h、第6 h和第24 h抑制咳嗽频率分别为52%、31%和21%，第6 h抑制咳嗽幅度为45%，第2和24 h无明显变化。CP-99994的血浆水平在2小时时最高（75 +/- 26 ng/ml），在6小时时降至22 +/- 6 ng/ml。这些结果表明，CP-99994在狗体内的止咳活性，其剂量被证明可以拮抗该物种的速激肽NK1受体。(C) 2003 Elsevier b.v.版权所有
CP-99994 [(+)-(2S,3S)-3-(2-methoxybenzylamino)-2-phenylpiperidine] is a selective tachykinin NK1 receptor antagonist that inhibits cough in guinea pigs and cats. This study examined the antitussive effects of CP-99994 in dogs produced by mechanical stimulation of the intrathoracic trachea. CP-99994 (10 mg/kg, p.o.) inhibited cough frequency by 52% at 2 h, 31% at 6 h and by 21% at 24 h. Cough amplitude was inhibited by 45% at 6 h but unchanged at 2 and 24 h after CP-99994. Plasma levels of CP-99994 were highest at 2 h (75 +/- 26 ng/ml) and fell to 22 +/- 6 ng/ml at 6 h. These results demonstrate antitussive activity of CP-99994 in dogs at a dose proven to antagonize tachykinin NK1 receptors in this species. (C) 2003 Elsevier B.V All rights reserved.