影响α-肾上腺素能受体药物作用时程的因素：可乐定对脊髓麻醉大鼠作用的研究
The factors influencing the time course of drug action at alpha-adrenoceptors: an investigation of the effects of clonidine in the pithed rat.
作者信息
Docherty J R, McGrath J C
出版信息
Br J Pharmacol. 1980 Feb;68(2):225-34. doi: 10.1111/j.1476-5381.1980.tb10411.x.
Abstract
1 The time courses of the pre- and post-junctional effects of clonidine were examined on heart rate and blood pressure and on the isometric tension responses of the vas deferens and anococcygeus in situ in the pithed rat. Plasma levels of clonidine were also monitored. 2 The time courses of the pre-junctional inhibition of sympathetic nerve mediated responses in all tissues monitored were related to the plasma levels of clonidine, but the degree of inhibition which was observed varied with the tissue and with the test stimulus employed. 3 The post-junctional agonist effects of clonidine, expecially at low doses, exhibited an initial 'peak' followed by a decline to a lower plateau. This decline of the response was not due to receptor desensitization but was related to a decline in the plasma clonidine level from an initially high value caused by injection of a bolus. 4 The factors determining the time course of drugs' effects in the preparation are discussed and it is concluded that pre- and post-junctional responses should be compared at a point in time after injection of the-drug, at which equilibration has occurred.
摘要
- 研究了可乐定对去大脑大鼠心率、血压以及输精管和尾骨肌原位等长张力反应的节前和节后效应的时程。同时监测了可乐定的血浆水平。2. 所监测的所有组织中，交感神经介导反应的节前抑制时程与可乐定的血浆水平相关，但观察到的抑制程度因组织和所用测试刺激而异。3. 可乐定的节后激动剂效应，尤其是低剂量时，呈现出一个初始“峰值”，随后下降至较低的平台期。这种反应的下降并非由于受体脱敏，而是与注射大剂量药物后血浆可乐定水平从最初的高值下降有关。4. 讨论了决定该制剂中药物效应时程的因素，并得出结论，应在注射药物后达到平衡的时间点比较节前和节后反应。
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A method of stimulating different segments of the autonomic outflow from the spinal column to various organs in the pithed cat and rat.一种在脊髓被破坏的猫和大鼠中刺激从脊柱到各个器官的自主神经传出不同节段的方法。
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The rat anococcygeus muscle and its response to nerve stimulation and to some drugs.大鼠肛门尾骨肌及其对神经刺激和某些药物的反应。
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Effects of clonidine and guanethidine on peripheral sympathetic nerve function in the pithed rat.可乐定和胍乙啶对脊髓横断大鼠外周交感神经功能的影响。
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The effect of pithing and of nerve stimulation on the depletion of noradrenaline by reserpine in the rat anococcygeus muscle and vas deferens.脊髓破坏和神经刺激对利血平所致大鼠肛尾肌和输精管去甲肾上腺素耗竭的影响。
Br J Pharmacol. 1974 Dec;52(4):585-90. doi: 10.1111/j.1476-5381.1974.tb09727.x.
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On the mechanism of the enhancement by smooth muscle stimulants of the motor responses of the guinea-pig vas deferens to nerve stimulation.
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Time course of the pre- and post-junctional effects of clonidine in the pithed rat [proceedings].可乐定对脊髓麻醉大鼠节前和节后效应的时间进程[会议论文]
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