首页> 外文期刊>British Journal of Pharmacology >Rilmenidine reveals differences in the pharmacological characteristics of prejunctional α_2-adrenoceptors in the guinea-pig, rat and pig
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Rilmenidine reveals differences in the pharmacological characteristics of prejunctional α_2-adrenoceptors in the guinea-pig, rat and pig

机译:利美替尼揭示了豚鼠,大鼠和猪的结前α_2-肾上腺素能受体药理特性的差异

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摘要

The α_2A and α_2D-adrenoceptor subtypes are thought to be species homologs most easily differentiated on the basis of the potency of antagonists. In the present study we have compared the effect of rilmenidine with two other selective α_2-adrenoceptor agonists, UK-14304(5-bromo-6-[2-imidazolin-2- ylamino]-quinoxaline) and clonidine, against electrically-evoked contractions in five isolated preparations from the rat, guinea-pig and pig, and, where possible, determined the receptor subtype involved. Uk-14034, clonidine and rilmenidine produced concentration-dependent inhibition of the electrically- Evoked contractions of the rat isolated vas deferens and tail artery and the guinea-pig ileum.
机译:α_2A和α_2D肾上腺素受体亚型被认为是最容易根据拮抗剂的功效进行区分的物种同源物。在本研究中,我们比较了瑞美尼定与其他两种选择性α_2-肾上腺素受体激动剂UK-14304(5-溴-6- [2-咪唑啉-2-基氨基]-喹喔啉)和可乐定对电诱发收缩的作用从大鼠,豚鼠和猪中分离出五种制剂,并在可能的情况下确定涉及的受体亚型。 Uk-14034,可乐定和瑞美尼定对大鼠离体输精管和尾动脉以及豚鼠回肠的电诱发的收缩产生浓度依赖性的抑制作用。

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