Comparative pharmacology of chlorpheniramine (Chlor-Trimeton) and its optical isomers.
Comparative pharmacology of chlorpheniramine (Chlor-Trimeton) and its optical isomers.
复制标题
扑尔敏（Chlor-Trimeton）及其光学异构体的药理学比较。
DOI：
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发表时间：
1958
影响因子：
3.5
通讯作者：
W. Govier
中科院分区：
文献类型：
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作者：
F. E. Roth;W. Govier
豚鼠肠道的体外抗组胺研究表明，d -氯苯那敏的效力约为外消旋化合物的两倍。左旋异构体的效力只有右旋氯苯那敏的百分之一。D -异构体对豚鼠静脉注射或雾化组胺引起的死亡的口服保护作用显示，其平均效力是外消旋化合物的1.8-2.4倍。麻醉犬中d -异构体的一般药效学与dl -化合物相似。在小鼠和猫中，所有3种药物的中枢神经系统效应表现为大致相同程度的全身刺激。在豚鼠、大鼠和小鼠中，d -异构体的急性毒性不大于dl -化合物。在大鼠和猴中进行的经口亚急性研究未发现可归因于d -或dl -扑尔敏给药的任何异常。
In vitro antihistamine studies on guinea pig gut have demonstrated that d -chlorpheniramine was approximately twice as potent as the racemic compound. The l -isomer had only about one-one hundredth the potency of dl -chlorpheniramine. The oral protective action of the d -isomer against death induced by intravenous or aerosolized histamine in guinea pigs revealed an average potency of 1.8-2.4 times that observed for the racemic compound. The general pharmacodynamics of the d -isomer in the anesthetized dog were similar to those of the dl -compound. The central nervous system effect of all 3 drugs in mice and cats was manifested as general stimulation of approximately the same degree. The acute toxicity of the d -isomer in guinea pigs, rats and mice was no greater than that of the dl -compound. Oral subacute studies in the rat and monkey did not reveal any abnormalities which could be attributed to administration of either d -or dl -chlorpheniramine.