6β-乙酰氧基去甲茛菪烷的眼科药理及临床研究  

The pharmacological and clinical studies of 6β-Acetoxynortropane in ophthalmology

作　　者：孙琛[1] 俞霭瑶[1] 姚渭珍 冯菊妹[1] 崔永跃[1] 张明珩[2] 陈达生[2] 李经庭 

机构地区：[1]上海第二医科大学药理学教研室 [2]上海第二医科大学附属瑞金医院眼科

出　　处：《上海第二医科大学学报》1991年第3期199-203,共5页Acta Universitatis Medicinalis Secondae Shanghai

基　　金：上海市高教局重点科研项目资助

摘　　要：6β-乙酰氧基去甲茛菪烷(6β-acetoxynortropane,6β-AN)属合成拟胆硷茛菪烷类化合物。动物试验证明6β-AN 0.003%的缩瞳作用和匹罗卡品2%者相同。6β-AN 0.003%对家兔正常眼压和水负荷引起的高眼压都有明显降压作用。6β-AN 0.003%-0.0045%给家兔滴眼4个月,未见眼部育任何不正常变化,临床试用6β-AN 0.004%于14例原发性青光眼病人,眼压平均下降0.83 kPa,而匹罗卡品2%则为0.77kPa。全血胆硷酯酶活性测定,离体兔虹膜药效动力学试验及放射配体受体结合试验显示6β-AN的作用机制主要是直接兴奋M-胆硷受体,也有极微弱的毒扁豆硷样作用,作者认为6β-AN在原发性青光眼的治疗上是匹罗卡品的良好替代品。6β-Acetoxynortropane (6β-AN) belongs to the synthetic cholinergic tropanes. Animal test proved that the miotic effect of 0.003% 6β-AN is equivalent to that of 2% pilocarpine. Both normal and water-loading-induced high intraocular pressure of rabbits were lowered significantly by 0.003% 6β-AN. Prolonged use of 0.003-0.0045% 6β-AN eyedrop into rabbits' eyes for 4 months and ophthalmologic examination performed evey month showed that there were no abnormal changes in the eyes. Clinical trials were performed in 14 patients with various typees of primary glaucoma. 0.004% 6β-AN lowered the intraocular pressure by 0.83 kPa while 2% pilocarpine by 0.77 kPa. Estimation of the whole blood cholinesterase activity, harmacodynamic test on isolated iris of rabbits and radiolisand binding assay on homogenate of rabbits' iris revealed that the mechanism of action of 6β-AN was mainly through the direct stimulating action on M-cholinoceptor in the iris and there was a very weak physostigmine-like action. The authors suggest that 6β-AN is a good alternative for pilocarpine in primary glaucoma therapy.

关 键 词：6β-AN 青光眼 药理 缩瞳 降眼压 

分 类 号：R969.4[医药卫生—药理学]