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大鼠肛门尾骨肌暴露于苄环烷后α1s-肾上腺素能受体的显示。

Demonstration of alpha 1s-adrenoceptors after exposure of the rat anococcygeus to benextramine.

作者信息

Coates J, Weetman D F

出版信息

Br J Pharmacol. 1983 Oct;80(2):343-6. doi: 10.1111/j.1476-5381.1983.tb10039.x.

DOI:10.1111/j.1476-5381.1983.tb10039.x
PMID:6140059
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2045030/
Abstract

Sgd 101/75 (4(2-imidazoline-amino)-2-methylindazol-chlorhydrate) and noradrenaline exerted similar, full agonist effects on the alpha-adrenoceptors of the rat anococcygeus. Benextramine (30 microM for 30 min, followed by 20 washes over 30 min) abolished contractions of the anococcygeus to Sgd 101/75, but only reduced those to noradrenaline. Sgd 101/75 (400 microM) did not significantly reduce contractions of the benextramine-treated (30 microM) anococcygeus to noradrenaline. It is concluded that benextramine can replace phenoxybenzamine as the alkylating agent in the demonstration of alpha 1s-adrenoceptors in the rat anococcygeus.

摘要

Sgd 101/75(4-(2-咪唑啉氨基)-2-甲基吲唑盐酸盐)和去甲肾上腺素对大鼠肛尾肌的α-肾上腺素能受体产生相似的完全激动剂作用。苄非他明(30微摩尔,作用30分钟,随后在30分钟内冲洗20次)消除了肛尾肌对Sgd 101/75的收缩反应,但仅减弱了对去甲肾上腺素的收缩反应。Sgd 101/75(400微摩尔)并未显著减弱经苄非他明(30微摩尔)处理的肛尾肌对去甲肾上腺素的收缩反应。得出的结论是,在大鼠肛尾肌α1s-肾上腺素能受体的证明中,苄非他明可替代酚苄明作为烷基化剂。

相似文献

1
Demonstration of alpha 1s-adrenoceptors after exposure of the rat anococcygeus to benextramine.大鼠肛门尾骨肌暴露于苄环烷后α1s-肾上腺素能受体的显示。
Br J Pharmacol. 1983 Oct;80(2):343-6. doi: 10.1111/j.1476-5381.1983.tb10039.x.
2
The existence of a new subtype of alpha-adrenoceptor on the rat anococcygeus is revealed by SGD 101/75 and phenoxybenzamine.SGD 101/75和酚苄明揭示了大鼠肛门尾骨肌上存在一种新的α-肾上腺素能受体亚型。
Br J Pharmacol. 1982 Mar;75(3):549-52. doi: 10.1111/j.1476-5381.1982.tb09172.x.
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Occurrence of alpha 1s-adrenoceptors in the mouse but not in the rabbit isolated anococcygeus preparations.α1s -肾上腺素能受体在小鼠离体肛门尾骨肌制备物中存在,但在兔离体肛门尾骨肌制备物中不存在。
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4
Sgd 101/75: a sympathomimetic that can be used to identify a new subtype of alpha-adrenoceptor, the alpha 1s-adrenoceptor.Sgd 101/75:一种拟交感神经药,可用于识别α-肾上腺素能受体的一种新亚型,即α1s-肾上腺素能受体。
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Analysis of putative alpha-1s adrenoceptor agonism by Sgd 101/75 in the rat anococcygeus muscle.Sgd 101/75对大鼠肛门尾骨肌假定的α-1s肾上腺素能受体激动作用的分析。
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Reactivation by cysteamine of vascular alpha adrenoceptors blocked by the tetramine disulfide benextramine and interaction of benextramine with phenoxybenzamine.半胱胺对被四胺二硫化物苄环烷阻断的血管α肾上腺素能受体的重新激活作用以及苄环烷与酚苄明的相互作用
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Effects of the irreversible alpha-adrenoceptor antagonists phenoxybenzamine and benextramine on the effectiveness of nifedipine in inhibiting alpha 1- and alpha 2-adrenoceptor mediated vasoconstriction in pithed rats.不可逆性α-肾上腺素能受体拮抗剂酚苄明和苄奈明对硝苯地平抑制去脑大鼠α1和α2肾上腺素能受体介导的血管收缩作用的影响。
Naunyn Schmiedebergs Arch Pharmacol. 1985 Jun;329(4):404-13. doi: 10.1007/BF00496376.
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Reversible inhibition of neuronal uptake by benextramine, an irreversible presynaptic alpha-adrenoceptor antagonist.苄非他明对神经元摄取的可逆性抑制,苄非他明是一种不可逆的突触前α-肾上腺素能受体拮抗剂。
Eur J Pharmacol. 1984 Feb 10;98(1):27-34. doi: 10.1016/0014-2999(84)90105-5.

本文引用的文献

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Cumulative dose-response curves. II. Technique for the making of dose-response curves in isolated organs and the evaluation of drug parameters.累积剂量-反应曲线。II. 离体器官中剂量-反应曲线的制作技术及药物参数的评估
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Occurrence of alpha 1s-adrenoceptors in the mouse but not in the rabbit isolated anococcygeus preparations.α1s -肾上腺素能受体在小鼠离体肛门尾骨肌制备物中存在,但在兔离体肛门尾骨肌制备物中不存在。
Br J Pharmacol. 1983 Jan;78(1):117-22. doi: 10.1111/j.1476-5381.1983.tb09370.x.
4
The existence of a new subtype of alpha-adrenoceptor on the rat anococcygeus is revealed by SGD 101/75 and phenoxybenzamine.SGD 101/75和酚苄明揭示了大鼠肛门尾骨肌上存在一种新的α-肾上腺素能受体亚型。
Br J Pharmacol. 1982 Mar;75(3):549-52. doi: 10.1111/j.1476-5381.1982.tb09172.x.
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An in vitro quantitative analysis of the alpha adrenoceptor partial agonist activity of dobutamine and its relevance to inotropic selectivity.多巴酚丁胺α肾上腺素能受体部分激动剂活性的体外定量分析及其与正性肌力选择性的相关性。
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Molecular properties of the adrenergic alpha receptor. 2. Optimum covalent inhibition by two different prototypes of polyamine disulfides.肾上腺素能α受体的分子特性。2. 两种不同原型的多胺二硫化物的最佳共价抑制作用。
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Selectivity of blocking agents for pre-and postsynaptic alpha-adrenoceptors.
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Prazosin, a selective antagonist of post-synaptic alpha-adrenoceptors [proceedings].哌唑嗪,一种突触后α-肾上腺素能受体的选择性拮抗剂[会议论文集]
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