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(-)-(2S,3aR,7aS)-1- [(S)-N- [(S)-1-乙氧羰基-3-苯丙基]丙氨酰基]六氢-2-吲哚羧酸(群多普利)在豚鼠中由咳嗽诱导的活性。

Cough-induced activity of (-)-(2S, 3aR, 7aS)-1-[(S)-N-[(S)-1-ethoxycarbonyl-3- phenylpropyl]alanyl]hexahydro-2-indolinecarboxylic acid (trandolapril) in guinea pigs.

作者信息

Kamei J, Iwamoto Y, Misawa M

机构信息

Department of Pharmacology, School of Pharmacy, Hoshi University, Tokyo, Japan.

出版信息

Res Commun Mol Pathol Pharmacol. 1994 Jul;85(1):105-8.

PMID:7953188
Abstract

We examined the effect of trandolapril ((-)-(2S, 3aR, 7aS)-1-[(S)-N-[(S)-1-ethoxycarbonyl-3- phenylpropyl]alanyl]hexahydro-2-indolinecarboxylic acid), a potent angiotensin converting enzyme (ACE) inhibitor, on the number of capsaicin-induced coughs in guinea pigs and compared it with that of enalapril. Chronic treatment with enalapril, at a dose of 3 mg/kg, p.o., significantly enhanced the number of capsaicin-induced coughs. Chronic treatment with trandolapril, at doses of 1 and 3 mg/kg, p.o., slightly enhanced the number of capsaicin-induced coughs. However, there were no significant differences in the number of capsaicin-induced coughs between trandolapril-treated and vehicle-treated animals. These results suggest that cough induced activity, one of the most serious side effects associated with chronic treatment with ACE inhibitors, of trandolapril is relatively lower than that of enalapril.

摘要

我们研究了强效血管紧张素转换酶(ACE)抑制剂群多普利((-)-(2S, 3aR, 7aS)-1-[(S)-N-[(S)-1-乙氧羰基-3-苯丙基]丙氨酰基]六氢-2-吲哚羧酸)对豚鼠辣椒素诱发咳嗽次数的影响,并将其与依那普利进行比较。口服给予依那普利3 mg/kg进行慢性治疗,可显著增加辣椒素诱发的咳嗽次数。口服给予群多普利1 mg/kg和3 mg/kg进行慢性治疗,可轻微增加辣椒素诱发的咳嗽次数。然而,群多普利治疗组和赋形剂治疗组动物的辣椒素诱发咳嗽次数没有显著差异。这些结果表明,群多普利作为ACE抑制剂慢性治疗相关最严重副作用之一的咳嗽诱发活性相对低于依那普利。

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