Byrne N G, Large W A
Department of Pharmacology and Clinical Pharmacology, St George's Hospital Medical School, London.
Br J Pharmacol. 1987 Oct;92(2):371-9. doi: 10.1111/j.1476-5381.1987.tb11333.x.
1 The mechanism of action of carbachol was studied on freshly dispersed cells of the rat anococcygeus using microelectrodes and patch pipettes. 2 Micro-ionophoretic application of carbachol evoked reproducible depolarizations which were reduced or blocked by atropine (10(-7)-10(-6) M). The time courses of the responses to noradrenaline and carbachol were similar. 3 The reversal potential of the carbachol-induced response was -3.8 mV and similar to the value (-6.2 mV) found for noradrenaline. 4 During the response to carbachol the membrane conductance was increased. At depolarized membrane potentials carbachol evoked biphasic membrane responses suggesting an increase in two separate ionic conductances. 5 With patch pipettes in the whole-cell configuration under voltage-clamp, carbachol produced an inward current at a holding potential of -50 mV. The inward current was associated with an increase in membrane conductance with an equilibrium potential of about 0 mV. 6 It is suggested that muscarinic receptors and adrenoceptors in the rat anococcygeus may activate similar membrane conductances. The most prominent mechanism is an increase in chloride ion conductance.
1 使用微电极和膜片吸管,在大鼠肛门尾骨肌的新鲜分散细胞上研究了卡巴胆碱的作用机制。2 微离子电泳施加卡巴胆碱可引起可重复的去极化,这种去极化可被阿托品(10⁻⁷ - 10⁻⁶ M)降低或阻断。对去甲肾上腺素和卡巴胆碱反应的时间进程相似。3 卡巴胆碱诱导反应的反转电位为 -3.8 mV,与去甲肾上腺素的反转电位值(-6.2 mV)相似。4 在对卡巴胆碱的反应过程中,膜电导增加。在去极化膜电位下,卡巴胆碱引起双相膜反应,提示两种独立离子电导增加。5 使用处于电压钳全细胞模式的膜片吸管,在 -50 mV 的钳制电位下,卡巴胆碱产生内向电流。该内向电流与膜电导增加相关,平衡电位约为 0 mV。6 提示大鼠肛门尾骨肌中的毒蕈碱受体和肾上腺素能受体可能激活相似的膜电导。最主要的机制是氯离子电导增加。