Hoskin F C, Rosenberg P
Science. 1967 May 19;156(3777):966-7. doi: 10.1126/science.156.3777.966.
The tertiary analogute of phospholine, namely, (C(2)H(5)O)(2)P(O)SCH(2)CH(2)N(CH(3))(2), is a potent, irreversible inhibitor of cholinesterase which, when externally applied to the sqluid giant axon, readily penetrates in its inhibitory form into the axoplasm. However, even a 10(-2) molar solution of this compound does not block axonal conduction unless the axon is first treated with a low concentration of venom from the cottonmouth moccasin. The question of the activity of acetylcholinesterase in these axons is considered, and the possibility of subcellular permeability barriers for indivisual components of the excitable membrane is discussed.
磷酰胆碱的叔类似物，即(C₂H₅O)₂P(O)SCH₂CH₂N(CH₃)₂，是一种强效、不可逆的胆碱酯酶抑制剂，当将其外部应用于枪乌贼巨大轴突时，它会以抑制形式轻易地渗透到轴浆中。然而，除非轴突先用低浓度的棉口蛇毒液处理，否则即使是这种化合物的10⁻²摩尔溶液也不会阻断轴突传导。文中考虑了这些轴突中乙酰胆碱酯酶的活性问题，并讨论了可兴奋膜单个成分存在亚细胞通透性屏障的可能性。
