Anti-tussive activity of benproperine enantiomers on citric-acid-induced cough in conscious guinea-pigs.
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.
Department of Pharmacology, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China.
Siwei
S
Chen
Li
L
Min
Yan
Y
Li
Weijing
W
Li
Dafang
D
Zhong
Weixi
W
Kong
D000818:Animals; D000996:Antitussive Agents / Q000493:pharmacokinetics / Q000627:therapeutic use*; D001559:Benzhydryl Compounds / Q000493:pharmacokinetics / Q000627:therapeutic use*; D019343:Citric Acid / Q000008:administration & dosage / Q000009:adverse effects*; D003371:Cough / Q000139:chemically induced* / Q000517:prevention & control; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D005260:Female; D006168:Guinea Pigs; D008297:Male; D010880:Piperidines / Q000493:pharmacokinetics / Q000627:therapeutic use*; D013237:Stereoisomerism; D013997:Time Factors
D000996:Antitussive Agents; D001559:Benzhydryl Compounds; D010880:Piperidines; D019343:Citric Acid; C477447:benproperine