Patil P N, Mauger T F
Division of Pharmacology, College of Pharmacy, Ohio State University, Columbus 43210.
Naunyn Schmiedebergs Arch Pharmacol. 1992 Dec;346(6):620-8. doi: 10.1007/BF00168734.
In vitro, iris contractions after muscarinic agonists were measured in mg of tension change and the concentration producing 50% of the response was expressed as EC50 mumol/l. Although the average EC50 value of carbachol in the iris sphincter of the donors with diabetes or Parkinson's disease did not change significantly when compared with the control, the maximum contraction of the tissue from the diseased state was increased significantly. Thus, in addition to the well known denervation supersensitivity of the iris-dilator, the iris-sphincter also develops adaptive sensitivity changes. Antimuscarinic drug treatment in some Parkinson's patients interfered with the estimation of supersensitivity in vitro studies. The enhanced response of carbachol at the low temperatures or the relative potency of carbachol and pilocarpine in the tissue obtained from the diseased donors was not significantly different from that of controls. Based on EC50 values, the potency of arecoline on the iris was 1/3 that of carbachol. Significantly lower EC50 values of carbachol were found in irides which were in contact with open loop type anterior chamber lens implants compared with those in contact with the closed loop anterior chamber lens implants. Maximum responses of irides to carbachol were less when the tissue was in contact with open loop lens compared with those in contact with closed loop anterior chamber implants. Irides from many donors having unilateral or bilateral replacement of the artificial lenses responded with EC50 of carbachol which was approximately equal to that of the contralateral eye. The maximum difference between EC50 values of the left and right iris was less than 5 fold.(ABSTRACT TRUNCATED AT 250 WORDS)
在体外,测量毒蕈碱激动剂作用后虹膜的收缩情况,以张力变化的毫克数表示,产生50%反应的浓度表示为半数有效浓度(EC50,微摩尔/升)。尽管与对照组相比,患有糖尿病或帕金森病的供体虹膜括约肌中卡巴胆碱的平均EC50值没有显著变化,但患病状态下组织的最大收缩明显增加。因此,除了众所周知的虹膜扩张肌去神经超敏反应外,虹膜括约肌也会发生适应性敏感性变化。一些帕金森病患者的抗毒蕈碱药物治疗干扰了体外研究中超敏反应的评估。患病供体组织中卡巴胆碱在低温下增强的反应或卡巴胆碱与毛果芸香碱的相对效价与对照组无显著差异。根据EC50值,槟榔碱对虹膜的效价是卡巴胆碱的1/3。与接触闭环式前房晶状体植入物的虹膜相比,接触开环式前房晶状体植入物的虹膜中卡巴胆碱的EC50值显著更低。当组织接触开环式晶状体时,虹膜对卡巴胆碱的最大反应小于接触闭环式前房植入物时。许多接受单侧或双侧人工晶状体置换的供体的虹膜对卡巴胆碱的反应,其EC50值与对侧眼大致相等。左右虹膜EC50值之间的最大差异小于5倍。(摘要截短于250字)