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米安色林与可乐定在α2-肾上腺素能受体上的相互作用。

Interaction between mianserin and clonidine at alpha 2-adrenoceptors.

作者信息

Pommier Y, Andréjak M, Mouillé P, Dabiré H, Lucet B, Schmitt H

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1982 Mar;318(4):288-94. doi: 10.1007/BF00501167.

DOI:10.1007/BF00501167
PMID:6281667
Abstract

The purpose of the present study was to characterize the effects of mianserin at alpha 2-adrenoceptors. Firstly, the action of mianserin on postganglionic sympathetic fibres has been studied using the tachycardia induced by stimulation of the cardiac nerve in dogs. Mianserin increased this tachycardia, but could not prevent the inhibitory effect of clonidine in this model. However, an antagonistic effect of mianserin against clonidine was observed when animals were pretreated with desipramine. Secondly, mianserin antagonized the inhibitory effect of clonidine on the electrically stimulated guinea-pig ileum. In high concentrations, mianserin reduced both electrically and acetylcholine induced contractions. Thirdly, mianserin antagonised the sleep induced by clonidine in chickens. These results are consistent with alpha 2-adrenoceptor blocking properties of mianserin in peripheral noradrenergic fibres in dogs, in cholinergic fibres in guinea-pig ileum and in the central nervous system in chickens.

摘要

本研究的目的是表征米安色林对α2-肾上腺素能受体的作用。首先,利用刺激犬心神经诱发的心动过速,研究了米安色林对节后交感神经纤维的作用。米安色林使这种心动过速加剧,但在该模型中不能阻止可乐定的抑制作用。然而,当动物用去甲丙咪嗪预处理时,观察到米安色林对可乐定有拮抗作用。其次,米安色林拮抗可乐定对电刺激的豚鼠回肠的抑制作用。在高浓度时,米安色林减少电刺激和乙酰胆碱诱导的收缩。第三,米安色林拮抗可乐定在鸡中诱导的睡眠。这些结果与米安色林在犬外周去甲肾上腺素能纤维、豚鼠回肠胆碱能纤维和鸡中枢神经系统中的α2-肾上腺素能受体阻断特性一致。

相似文献

1
Interaction between mianserin and clonidine at alpha 2-adrenoceptors.米安色林与可乐定在α2-肾上腺素能受体上的相互作用。
Naunyn Schmiedebergs Arch Pharmacol. 1982 Mar;318(4):288-94. doi: 10.1007/BF00501167.
2
Comparison of mianserin with desipramine, maprotiline and phentolamine on cardiac presynaptic and vascular postsynaptic alpha-adrenoceptors and noradrenaline reuptake in pithed normotensive rats.米安色林与地昔帕明、马普替林和酚妥拉明对脊髓麻醉正常血压大鼠心脏突触前和血管突触后α-肾上腺素能受体及去甲肾上腺素再摄取的比较
Br J Pharmacol. 1980 Feb;68(2):321-32. doi: 10.1111/j.1476-5381.1980.tb10421.x.
3
Effects of (+)- and (-)-mianserin on alpha-adrenoceptors and tyramine-induced tachycardia in rats.(+)-和(-)-米安色林对大鼠α-肾上腺素能受体及酪胺诱发心动过速的影响。
Eur J Pharmacol. 1983 Jun 3;90(2-3):221-6. doi: 10.1016/0014-2999(83)90240-6.
4
Mianserin--an analysis of its peripheral autonomic actions.米安色林——对其外周自主神经作用的分析
Eur J Pharmacol. 1978 Sep 1;51(1):1-10. doi: 10.1016/0014-2999(78)90055-9.
5
Pharmacological characterization of the presynaptic alpha-adrenoceptors regulating cholinergic activity in the guinea-pig ileum.豚鼠回肠中调节胆碱能活性的突触前α-肾上腺素能受体的药理学特性
Br J Pharmacol. 1978 Oct;64(2):293-300. doi: 10.1111/j.1476-5381.1978.tb17303.x.
6
Effects of some alpha-adrenoceptor agonists and antagonists on the guinea-pig ileum.某些α-肾上腺素能受体激动剂和拮抗剂对豚鼠回肠的作用。
Naunyn Schmiedebergs Arch Pharmacol. 1980 Oct;314(1):83-7. doi: 10.1007/BF00498434.
7
An in vivo model for investigating alpha 1- and alpha 2-receptors in the CNS: studies with mianserin.一种用于研究中枢神经系统中α1和α2受体的体内模型:米安色林的研究
Arch Int Pharmacodyn Ther. 1979 Nov;242(1):59-76.
8
Prejunctional alpha 2-adrenoceptor mediated inhibitory action of clonidine and B-HT 920, but not urapidil in guinea pig ileum.可乐定和B-HT 920对豚鼠回肠有节前α2-肾上腺素能受体介导的抑制作用,而乌拉地尔则没有。
Proc Soc Exp Biol Med. 1985 Jan;178(1):133-8. doi: 10.3181/00379727-178-41994.
9
Mianserin: direct activation of brain norepinephrine neurons by blocking alpha 2-receptors.米安色林:通过阻断α2受体直接激活脑内去甲肾上腺素能神经元。
Commun Psychopharmacol. 1980;4(3):233-9.
10
The tetracyclic antidepressant mianserin: evaluation of its blockade of presynaptic alpha-adrenoceptors in a self-stimulation model using clonidine.四环类抗抑郁药米安色林:在使用可乐定的自我刺激模型中对其对突触前α-肾上腺素能受体阻断作用的评估。
Eur J Pharmacol. 1981 Mar 5;70(1):59-63. doi: 10.1016/0014-2999(81)90432-5.

引用本文的文献

1
Measurement of 3-methoxy-4-hydroxyphenylglycol (MHPG) in mouse brain by h.p.l.c. with electrochemical detection, as an index of noradrenaline utilisation and presynaptic alpha 2-adrenoceptor function.采用高效液相色谱法(h.p.l.c.)并结合电化学检测测定小鼠脑中3-甲氧基-4-羟基苯乙二醇(MHPG),以此作为去甲肾上腺素利用及突触前α2-肾上腺素能受体功能的指标。
Br J Pharmacol. 1989 Mar;96(3):547-56. doi: 10.1111/j.1476-5381.1989.tb11852.x.

本文引用的文献

1
The response of the guineapig ileum to electrical stimulation by coaxial electrodes.豚鼠回肠对同轴电极电刺激的反应。
J Physiol. 1955 Feb 28;127(2):40-1P.
2
The action of morphine and related substances on contraction and on acetylcholine output of coaxially stimulated guinea-pig ileum.吗啡及相关物质对同轴刺激的豚鼠回肠收缩和乙酰胆碱释放的作用。
Br J Pharmacol Chemother. 1957 Mar;12(1):119-27. doi: 10.1111/j.1476-5381.1957.tb01373.x.
3
An examination of factors influencing adrenergic transmission in the pithed rat, with special reference to noradrenaline uptake mechanisms and post-junctional alpha-adrenoceptors.
对影响去大脑大鼠肾上腺素能传递的因素进行研究,特别关注去甲肾上腺素摄取机制和接头后α-肾上腺素能受体。
Naunyn Schmiedebergs Arch Pharmacol. 1980 Aug;313(2):101-11. doi: 10.1007/BF00498564.
4
Comparison of mianserin with desipramine, maprotiline and phentolamine on cardiac presynaptic and vascular postsynaptic alpha-adrenoceptors and noradrenaline reuptake in pithed normotensive rats.米安色林与地昔帕明、马普替林和酚妥拉明对脊髓麻醉正常血压大鼠心脏突触前和血管突触后α-肾上腺素能受体及去甲肾上腺素再摄取的比较
Br J Pharmacol. 1980 Feb;68(2):321-32. doi: 10.1111/j.1476-5381.1980.tb10421.x.
5
Effect of mianserin on noradrenergic transmission in the rat anococcygeus muscle.米安色林对大鼠肛尾肌去甲肾上腺素能传递的影响。
Br J Pharmacol. 1980 Feb;68(2):241-50. doi: 10.1111/j.1476-5381.1980.tb10413.x.
6
The effects of mianserine, amitriptyline, ciclazindol and viloxazine on presynaptic alpha-receptors in isolated rat atria [proceedings].米安色林、阿米替林、环苯扎朵和维洛沙嗪对离体大鼠心房突触前α受体的作用[会议论文集]
Br J Pharmacol. 1980 Jan;68(1):184P-185P.
7
The inability of chronic mianserin to block central alpha 2-adrenoceptors.慢性米安色林无法阻断中枢α2肾上腺素能受体。
Eur J Pharmacol. 1980 Dec 5;68(3):377-80. doi: 10.1016/0014-2999(80)90537-3.
8
Effects of some alpha-adrenoceptor agonists and antagonists on the guinea-pig ileum.某些α-肾上腺素能受体激动剂和拮抗剂对豚鼠回肠的作用。
Naunyn Schmiedebergs Arch Pharmacol. 1980 Oct;314(1):83-7. doi: 10.1007/BF00498434.
9
Differential inhibiton of alpha-1 and alpha-2 adrenoceptor-mediated pressor responses in pithed rats.在脊髓横断大鼠中α-1和α-2肾上腺素能受体介导的升压反应的差异抑制
J Pharmacol Exp Ther. 1980 Aug;214(2):275-81.
10
[Pharmacological effects of 2-(2,6-dichlorophenylamino)-2-imidazoline hydrochloride, a new, antihypertensive substance].新型抗高血压物质2-(2,6-二氯苯基氨基)-2-咪唑啉盐酸盐的药理作用
Arzneimittelforschung. 1966 Aug;16(8):1038-50.