Elliott J M, Tayler P J, Young J M
J Pharm Pharmacol. 1978 Jan;30(1):27-35. doi: 10.1111/j.2042-7158.1978.tb13148.x.
The extent of the binding of [3H]propylbenzilylcholine mustard (3H-PrBCM) to muscarinic receptors in longitudinal muscle strips from guinea-pig small intestine is increased by nearly 50% when the strips are preexposed to distilled water before measurement of 3H-PrBCM binding in Krebs-Henseleit solution. The apparent rate constant for 3H-PrBCM-receptor complex formation is more than double that of intact strips. The curves for the inhibition of 3H-PrBCM binding by methylatropinium bromide in normal and treated strips are superimposable, but, in contrast, distilled water pretreatment shifts the inhibition curve for carbachol to lower concentrations by a factor of 5-6. The inhibition curve for methylfurmethide is also shifted, by a factor of approximately 4, but the effect on the curve for hexyltrimethylammonium (C6TMA) is slight. The relative inhibition produced by benzhexol in the two preparations was variable. Comparison of the rate of equilibration of benzhexol with muscarinic receptors in intact and in distilled water pretreated muscle indicates that this inconsistency is unlikely to be due to incomplete equilibration.
当豚鼠小肠纵肌条在克雷布斯 - 亨泽莱特溶液中测量[³H]丙基苯甲酰胆碱氮芥（³H-PrBCM）结合之前预先暴露于蒸馏水中时，³H-PrBCM与毒蕈碱受体的结合程度增加了近50%。³H-PrBCM - 受体复合物形成的表观速率常数是完整肌条的两倍多。在正常和处理过的肌条中，溴甲阿托品对³H-PrBCM结合的抑制曲线是可叠加的，但相比之下，蒸馏水预处理使卡巴胆碱的抑制曲线向更低浓度移动了5 - 6倍。甲呋铵的抑制曲线也移动了约4倍，但对己基三甲基铵（C6TMA）曲线的影响很小。苯海索在两种制剂中产生的相对抑制作用是可变的。比较完整肌条和经蒸馏水预处理的肌肉中苯海索与毒蕈碱受体的平衡速率表明，这种不一致不太可能是由于平衡不完全所致。
