Antitussive activity of moguisteine enantiomers in guinea-pigs and rats.
The antitussive effect of the R-(+)- and S-(-)-enantiomers of moguisteine were evaluated in comparison with the racemate in cough induced by 7.5% citric acid and 30 microM capsaicin aerosol in conscious guinea-pigs. No difference in potency was observed between moguisteine and the enantiomers. The oral ED50 values (with 95% confidence limits) for moguisteine, R-(+)- and S-(-)-enantiomers were respectively: 20.4 (12.9-26.6), 20.9 (14.9-26) and 21.6 (11.8-30.0) mg/kg-1 in cough provoked by citric acid and 17.7 (12.5-29.8), 18.9 (14.1-30.1) and 20.5 (15.1-36.6) mg/kg-1 in cough induced by capsaicin. The acute oral and intraperitoneal toxicities of the enantiomers and moguisteine in the rat are very similar. These findings suggest that the use of either enantiomer does not offer any advantage over the racemate.
Gallico
L
L
Boehringer Mannheim Italia, Research Centre, Monza, Italy.
Borghi
A
A
Cavalletti
E
E
Ceserani
R
R
Tognella
S
S
D000284:Administration, Oral; D000336:Aerosols; D000818:Animals; D000863:Antacids / Q000008:administration & dosage / Q000633:toxicity; D000996:Antitussive Agents / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D002211:Capsaicin / Q000008:administration & dosage / Q000633:toxicity; D019343:Citric Acid / Q000008:administration & dosage / Q000633:toxicity; D003371:Cough / Q000139:chemically induced / Q000188:drug therapy*; D004305:Dose-Response Relationship, Drug; D005260:Female; D006168:Guinea Pigs; D007274:Injections, Intraperitoneal; D007928:Lethal Dose 50; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D013045:Species Specificity; D013237:Stereoisomerism; D013844:Thiazoles / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D053778:Thiazolidines
D000336:Aerosols; D000863:Antacids; D000996:Antitussive Agents; D013844:Thiazoles; D053778:Thiazolidines; D019343:Citric Acid; C087933:moguisteine; D002211:Capsaicin