Anti-tussive activity of benproperine enantiomers on citric-acid-induced cough in conscious guinea-pigs.

Abstract

The anti-tussive effect of the R-(+)- and S-(-)-enantiomers of benproperine was evaluated and compared with that of the racemate on cough induced by 7.5% citric acid in conscious guinea-pigs. All the three compounds, intraperitoneally administered 1.5 h before the test, significantly inhibited citric-acid-induced cough. The ID50 values (effective doses for 50% inhibition) (with 95% confidence intervals) were 16.1 (9.1-28.4), 23.3 (11.2-48.6), 25.4 (11.7-55.1) mg kg(-1) for the number of coughs in the 3 min of challenge, and 11.9 (5.3-26.6), 13.5 (5.6-32.4), 19.2 (12.8-28.9) mg kg(-1) for the number of coughs in the 5 min immediately after the challenge, for (+/-)-benproperine, R-(+)-benproperine and S-(-)-benproperine, respectively. These findings suggest that the use of either enantiomer does not show any advantage over the racemate with regard to their anti-tussive effect.

• Authors: Siwei Chen, Li Min, Yan Li, Weijing Li, Dafang Zhong, Weixi Kong
• Journal: The Journal of pharmacy and pharmacology (J Pharm Pharmacol) Vol. 56 Issue 2 Pg. 277-80 (Feb 2004) ISSN: 0022-3573 [Print] England
• PMID: 15005888 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antitussive Agents
• Benzhydryl Compounds
• Piperidines
• Citric Acid
• benproperine

Topics

• Animals
• Antitussive Agents (pharmacokinetics, therapeutic use)
• Benzhydryl Compounds (pharmacokinetics, therapeutic use)
• Citric Acid (administration & dosage, adverse effects)
• Cough (chemically induced, prevention & control)
• Disease Models, Animal
• Dose-Response Relationship, Drug
• Female
• Guinea Pigs
• Male
• Piperidines (pharmacokinetics, therapeutic use)
• Stereoisomerism
• Time Factors