Suzuki R, Yoshino H, Kobayashi S
Department of Ophthalmology, Yamaguchi University School of Medicine, Ube, Japan.
Doc Ophthalmol. 1988 May;69(1):73-81. doi: 10.1007/BF00154419.
We investigated the effect of pilocarpine on the bovine iris sphincter. This muscle contracted in a dose-dependent manner from 2 x 10(-6) M, with a maximal response at 3 x 10(-3) M. The ED50 values was (1.6 +/- 0.3) x 10(-4) M. Pilocarpine generated a desensitization while desensitization was not significant in the case of other cholinergic agents such as acetylcholine (Ach) and carbachol. Desensitization was profoundly increased in the presence of Ach, neostigmine or eserine: the responses to the second and third trials of pilocarpine were reduced to approximately 8-10% or 30% of the corresponding first responses. Pilocarpine reportedly releases transmitters and alters choline-acetyltransferase activity. These results taken together suggest that either variable Ach synthesis, inhibitory transmitter release or possible toxic action in high concentrations may be involved in the pilocarpine-induced responses of the bovine iris sphincter muscle. The desensitization and partial agonist-antagonist action of pilocarpine could not explain the characteristics of the bovine iris sphincter muscle.
我们研究了毛果芸香碱对牛虹膜括约肌的作用。该肌肉从2×10⁻⁶ M开始呈剂量依赖性收缩,在3×10⁻³ M时出现最大反应。半数有效剂量(ED50)值为(1.6±0.3)×10⁻⁴ M。毛果芸香碱会产生脱敏作用,而在其他胆碱能药物如乙酰胆碱(Ach)和卡巴胆碱的情况下,脱敏作用并不显著。在存在Ach、新斯的明或毒扁豆碱的情况下,脱敏作用会显著增强:毛果芸香碱第二次和第三次试验的反应分别降至相应第一次反应的约8 - 10%或30%。据报道,毛果芸香碱会释放递质并改变胆碱乙酰转移酶活性。综合这些结果表明,毛果芸香碱诱导的牛虹膜括约肌反应可能涉及可变的Ach合成、抑制性递质释放或高浓度时可能的毒性作用。毛果芸香碱的脱敏作用和部分激动剂 - 拮抗剂作用无法解释牛虹膜括约肌的特性。