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铽离子对小鼠神经母细胞瘤细胞毒蕈碱型乙酰胆碱受体的动力学影响。

Kinetic effects of terbium ions on muscarinic acetylcholine receptors of murine neuroblastoma cells.

作者信息

El-Fakahany E E, Pfenning M, Richelson E

出版信息

J Neurochem. 1984 Mar;42(3):863-9. doi: 10.1111/j.1471-4159.1984.tb02760.x.

Abstract

Preincubation of murine neuroblastoma cells (clone N1E-115) with terbium chloride resulted in a significant potentiation of carbachol-mediated increase in cyclic GMP formation. This effect was accompanied by a shift of the peak response from 30 s to 120 s and a 6-fold decrease in carbachol concentration producing half-maximal responses, in addition to a significant increase in the Hill coefficient. Terbium ions also caused a significant decrease in the affinity and an increase in the maximum binding of [3H]quinuclidinyl benzilate to muscarinic receptors, the change in affinity being mainly due to a decrease in the association rate. Preincubation of cells with 1 mM carbachol for 4 h (the desensitized state of the muscarinic receptor) resulted in a decrease in the ability of terbium to alter [3H]quinuclidinyl benzilate binding. The effects of terbium reported here might be due to its affecting muscarinic receptor-effector coupling, which is considered to be lost upon receptor desensitization.

摘要

用氯化铽对小鼠神经母细胞瘤细胞(克隆N1E - 115)进行预孵育,可显著增强卡巴胆碱介导的环鸟苷酸生成增加。除了希尔系数显著增加外,这种效应还伴随着峰值反应从30秒移至120秒,以及产生半数最大反应的卡巴胆碱浓度降低6倍。铽离子还导致[3H]喹核醇基苯甲酸酯与毒蕈碱受体的亲和力显著降低,最大结合量增加,亲和力的变化主要是由于结合速率降低。用1 mM卡巴胆碱对细胞预孵育4小时(毒蕈碱受体的脱敏状态)会导致铽改变[3H]喹核醇基苯甲酸酯结合的能力下降。此处报道的铽的作用可能是由于其影响毒蕈碱受体 - 效应器偶联,而这种偶联被认为在受体脱敏时丧失。

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