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Comparative study on anti-motion sickness efficacy of R-phencynonate hydrochloride and its optical isomers
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- Author:
- No author available
- Journal Title:
- CHINESE JOURNAL OF AEROSPACE MEDICINE
- Issue:
- 2
- DOI:
- 10.3760/cma.j.issn.1007-6239.2006.02.002
- Key Word:
- 盐酸苯环壬酯;晕动病;受体;胆碱能;手性药物
Abstract： 目的 评价盐酸苯环壬酯左旋体[R(-)-PCH]对晕动病的防治作用.方法 建立两个实验动物模型:①家兔右侧颈总动脉局部帖敷强胆碱酯酶抑制剂对氧磷10 μl(380 μg/10 μl),家兔出现逆向(左侧)转圈,逆向转圈3圈/min以上为晕动病阳性症状,实验前20 min灌胃给药,观察盐酸苯环壬酯及其光学异构体对家兔晕动病的防治作用;②家猫右侧大腿深部肌肉注射毒扁豆碱(0.6 mg/kg),引起家猫腹部不适、恶心、呕吐等晕动病(MS)样综合征,实验前20 min灌胃给药.观察盐酸苯环壬酯消旋体及其光学异构体对家猫晕动病样综合征的预防和治疗作用.结果 兔逆向转圈综合症模型中盐酸苯环壬酯左旋体的半数有效剂量(ED50)为4.01 mg/kg,外消旋体的ED50为8.94 mg/kg,两者的ED50比为1∶2.23(P＜0.05),而盐酸苯环壬酯的右旋体[S(+)-PCH]在34 mg/kg没有表现出明显的抗晕动病效果(P＞0.05); 在家猫晕动病样综合症模型中,R(-)-PCH的ED50值为0.07 mg/kg,外消旋体的ED50值为0.58 mg/kg,两者的ED50值比为1∶8.29(P＜0.01), 而S(+)-PCH在3.0 mg/kg没有表现出明显的抗晕动病效果(P＞0.05).结论 盐酸苯环壬酯的左旋体抗晕动病效果明显强于外消旋体和右旋体,将来可能会成为抗晕动病的新药.
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