Gallico L, Borghi A, Cavalletti E, Ceserani R, Tognella S
Boehringer Mannheim Italia, Research Centre, Monza, Italy.
J Pharm Pharmacol. 1996 Jan;48(1):112-4. doi: 10.1111/j.2042-7158.1996.tb05888.x.
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.
在清醒豚鼠中,比较了莫吉司坦的R-(+)-和S-(-)-对映体与消旋体对7.5%柠檬酸和30微摩尔辣椒素气雾剂诱发咳嗽的镇咳作用。未观察到莫吉司坦与其对映体在效力上的差异。在柠檬酸诱发的咳嗽中,莫吉司坦、R-(+)-和S-(-)-对映体的口服半数有效剂量(ED50)值(及其95%置信区间)分别为:20.4(12.9 - 26.6)、20.9(14.9 - 26)和21.6(11.8 - 30.0)毫克/千克;在辣椒素诱发的咳嗽中,相应值分别为17.7(12.5 - 29.8)、18.9(14.1 - 30.1)和20.5(15.1 - 36.6)毫克/千克。对映体和莫吉司坦在大鼠中的急性经口和腹腔毒性非常相似。这些发现表明,使用任何一种对映体都不会比消旋体具有任何优势。