Fossier P, Baux G, Tauc L
Cell Mol Neurobiol. 1987 Mar;7(1):49-59. doi: 10.1007/BF00734989.
The responsiveness of Aplysia acetylcholine receptors (AChR) was studied using a polyene antibiotic, filipin, which specifically complexes cholesterol, and another compound, chlorpromazine (CPZ), which inserts at the proteolipidic interface. Both substances enhanced the evoked postsynaptic responses or responses to iontophoretic application of carbachol only on the H-type receptor (opening a Cl-permeability), whereas at the same concentrations filipin was without effect on the D-type receptor (opening a cationic permeability) while CPZ depressed the D-type response. The facilitation observed specifically for the H-type receptor was similar to that previously described after acetylcholinesterase (AChE) inhibition or when low concentrations of detergents were applied to this preparation. No additive effect was obtained after the addition of chlorpromazine following a maximal potentiation obtained with an anticholinesterase agent. Since at Aplysia central neurons, AChE is a membranal protein, we propose that the facilitation of H-type responses is attributable to the removal of a modulatory action of AChE on AChR. Filipin or chlorpromazine might disrupt the interaction between AChR and AChE.
利用多烯抗生素制霉菌素（一种能特异性结合胆固醇的物质）和另一种化合物氯丙嗪（CPZ，一种插入蛋白脂质界面的物质），对海兔乙酰胆碱受体（AChR）的反应性进行了研究。这两种物质仅对H型受体（开启氯离子通透性）增强了诱发的突触后反应或对离子电渗法施加卡巴胆碱的反应，而在相同浓度下，制霉菌素对D型受体（开启阳离子通透性）无影响，而氯丙嗪则抑制D型反应。对H型受体特异性观察到的易化作用与先前在乙酰胆碱酯酶（AChE）抑制后或向该制剂中施加低浓度去污剂时所描述的相似。在用抗胆碱酯酶剂获得最大增强作用后添加氯丙嗪，未观察到相加效应。由于在海兔中枢神经元中，AChE是一种膜蛋白，我们推测H型反应的易化作用归因于AChE对AChR调节作用的消除。制霉菌素或氯丙嗪可能会破坏AChR与AChE之间的相互作用。
