Søli N E, Karlsen R L, Opsahl M, Fonnum F
J Neurochem. 1980 Sep;35(3):723-8. doi: 10.1111/j.1471-4159.1980.tb03712.x.
Acetylcholinesterase (AChE) in guinea pig iris was inhibited by methylisocyclopentylfluorophosphate (soman) administered topically or parenterally, and enzyme activity was correlated to pupillary diameter by infrared pupillography. After a single topical soman instillation into the conjunctival sac there was an almost linear relationship between the reduction in AChE activity and pupillary diameter. Topical administration of soman at 24-h intervals in doses capable of almost complete inhibition of AChE in iris was accompanied by a reduced miotic effect of this drug. This was indicated by a reduced rate of the soman-induced pupillary constriction, a less pronounced reduction in pupillary diameter, and a more rapid return of the pupillary diameter to normal size. The change in pupillary diameter occurred after three daily administrations and remained constant during 31 days of treatment. These observations were seen irrespective of inhibition of blood AChE. The decrease in response to repeated administration could not be explained by a reduced inhibitory effect of soman on AChE, by a more rapid de novo synthesis of AChE, or by a change in the number of the muscarinic receptors as determined by quinuclidinyl benzilate binding. When soman or DFP was administered subcutaneously in high doses a severe AChE inhibition was obtained in iris without any concomitant miosis.
局部或经胃肠外途径给予豚鼠虹膜甲基异环戊基氟磷酸酯（梭曼）可抑制乙酰胆碱酯酶（AChE），并通过红外瞳孔描记法将酶活性与瞳孔直径相关联。在向结膜囊单次局部滴注梭曼后，AChE活性降低与瞳孔直径之间几乎呈线性关系。以能够几乎完全抑制虹膜中AChE的剂量每隔24小时局部给予梭曼，该药物的缩瞳作用会减弱。这表现为梭曼诱导的瞳孔收缩速率降低、瞳孔直径缩小不明显以及瞳孔直径更快恢复至正常大小。瞳孔直径的变化在每日给药三次后出现，并在治疗的31天内保持不变。无论血液中AChE是否受到抑制，均可观察到这些现象。对重复给药反应的降低无法通过梭曼对AChE抑制作用的减弱、AChE更快的从头合成或由奎宁环基苯甲酸酯结合所确定的毒蕈碱受体数量的变化来解释。当大剂量皮下注射梭曼或二异丙基氟磷酸酯（DFP）时，虹膜中的AChE受到严重抑制，但未伴随任何缩瞳现象。
