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本文引用的文献

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Some quantitative uses of drug antagonists.药物拮抗剂的一些定量应用。
Br J Pharmacol Chemother. 1959 Mar;14(1):48-58. doi: 10.1111/j.1476-5381.1959.tb00928.x.
2
Heterogeneity of postsynaptic Alpha adrenergic receptors in mammalian aortas.哺乳动物主动脉中突触后α肾上腺素能受体的异质性。
J Pharmacol Exp Ther. 1982 May;221(2):309-14.
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Mini-review. The postsynaptic alpha 2-adrenoreceptor.小型综述。突触后α2肾上腺素能受体。
J Auton Pharmacol. 1981 Mar;1(2):171-83. doi: 10.1111/j.1474-8673.1981.tb00509.x.
4
Smooth muscle of rabbit aorta contains alpha 1-but not alpha 2-adrenoceptors.兔主动脉平滑肌含有α1肾上腺素能受体,但不含有α2肾上腺素能受体。
Naunyn Schmiedebergs Arch Pharmacol. 1981 Aug;317(1):5-7. doi: 10.1007/BF00506248.
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Uneven distribution of postjunctional alpha 1-and alpha 2-like adrenoceptors in canine arterial and venous smooth muscle.犬动脉和静脉平滑肌中节后α1和α2样肾上腺素能受体的分布不均。
Circ Res. 1981 Jun;48(6 Pt 1):875-84. doi: 10.1161/01.res.48.6.875.
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Alpha-adrenoceptor subclassification.α-肾上腺素能受体亚分类
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Receptor interactions of imidazolines. V. clonidine differentiates postsynaptic alpha adrenergic receptor subtypes in tissues from the rat.咪唑啉的受体相互作用。V.可乐定对大鼠组织中突触后α肾上腺素能受体亚型的区分
J Pharmacol Exp Ther. 1980 Jun;213(3):557-61.
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Selectivity of a series of clonidine-like drugs for alpha 1 and alpha 2 adrenoceptors in rat brain.一系列可乐定样药物对大鼠脑内α1和α2肾上腺素能受体的选择性
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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。
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Differences in pharmacological properties of postjunctional alpha-adrenergic receptors among arteries and veins.动脉和静脉之间节后α-肾上腺素能受体药理学特性的差异。
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大鼠主动脉条和门静脉突触后α-肾上腺素能受体的特性研究

Characterization of postsynaptic alpha-adrenoceptors in rat aortic strips and portal veins.

作者信息

Digges K G, Summers R J

出版信息

Br J Pharmacol. 1983 Jul;79(3):655-65. doi: 10.1111/j.1476-5381.1983.tb10002.x.

DOI:10.1111/j.1476-5381.1983.tb10002.x
PMID:6140044
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2044909/
Abstract

Postsynaptic alpha-adrenoceptors in rat isolated aortic strips and portal veins have been examined using a number of agonist and antagonist drugs which have varying selectivity for alpha 1- and alpha 2-adrenoceptors. In both tissues (-)-noradrenaline [-)-NA), (-)-adrenaline [-) Adr) (-)-alpha-methyl noradrenaline [-)-alpha-Me-NA) and (-)-phenylephrine [-)-PE) were full agonists, while clonidine, oxymetazoline and (2-(2,6-dichlorophenyl)-5,6-dihydroimidazo(2,1,b) thiazole (44,549) were partial agonists. Guanfacine was a full agonist in aortic strips but only a partial agonist in portal veins. In aortic strips, pA2 values for prazosin and yohimbine were not significantly different using (-)-NA, (-)-PE or guanfacine as the agonist, suggesting a single population of alpha-adrenoceptors. The order of potency of the antagonists, prazosin = 2-(beta-(4-hydroxyphenyl)-ethylaminomethyl)-tetralone (BE2254) greater than phentolamine greater than yohimbine greater than rauwolscine, is indicative of an alpha 1-type of receptor. In portal veins, the order of potency of the antagonists was prazosin greater than BE2254 greater than phentolamine greater than yohimbine greater than rauwolscine, again indicating an alpha 1-type of receptor. The mean pA2 value for yohimbine was not significantly different in either tissue. However, mean pA2 values for prazosin, BE-2254 and phentolamine were approximately one order of magnitude lower in portal veins than in aortic strips, suggesting that the receptors in the two tissues may not be identical.

摘要

利用多种对α1和α2肾上腺素能受体具有不同选择性的激动剂和拮抗剂药物,对大鼠离体主动脉条和门静脉中的突触后α-肾上腺素能受体进行了研究。在这两种组织中,(-)-去甲肾上腺素[(-)-NA]、(-)-肾上腺素[(-)-Adr]、(-)-α-甲基去甲肾上腺素[(-)-α-Me-NA]和(-)-去氧肾上腺素[(-)-PE]是完全激动剂,而可乐定、羟甲唑啉和(2-(2,6-二氯苯基)-5,6-二氢咪唑并[2,1,b]噻唑(44,549)是部分激动剂。胍法辛在主动脉条中是完全激动剂,但在门静脉中只是部分激动剂。在主动脉条中,以(-)-NA、(-)-PE或胍法辛为激动剂时,哌唑嗪和育亨宾的pA2值无显著差异,提示存在单一群体的α-肾上腺素能受体。拮抗剂的效能顺序为哌唑嗪 = 2-(β-(4-羟基苯基)-乙胺甲基)-四氢萘酮(BE2254)>酚妥拉明>育亨宾>萝芙木碱,表明是α1型受体。在门静脉中,拮抗剂的效能顺序为哌唑嗪>BE2254>酚妥拉明>育亨宾>萝芙木碱,同样表明是α1型受体。育亨宾的平均pA2值在两种组织中无显著差异。然而,哌唑嗪、BE-2254和酚妥拉明的平均pA2值在门静脉中比在主动脉条中约低一个数量级,提示两种组织中的受体可能不相同。