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α1肾上腺素能受体部分阻断后,α2肾上腺素能受体介导的对所谓选择性α1肾上腺素能受体激动剂的反应。

Alpha 2-adrenoceptor-mediated responses to so-called selective alpha 1-adrenoceptor agonists after partial blockade of alpha 1-adrenoceptors.

作者信息

Guimarães S, Paiva M Q, Moura D

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1987 Apr;335(4):397-402. doi: 10.1007/BF00165554.

Abstract

In dog saphenous vein--a tissue possessing both postsynaptic alpha 1- and alpha 2-adrenoceptors--the effects of two selective alpha 1-adrenoceptor agonists (phenylephrine and methoxamine) were compared with that of the selective alpha 2-adrenoceptor agonist, UK-14,304, before and after phenoxybenzamine. Furthermore, the influence exerted by prazosin, yohimbine and verapamil on the effects of these agonists was also studied before and after phenoxybenzamine. In the absence of phenoxybenzamine, prazosin (56 nmol/l) caused a parallel shift of the concentration-response curves of both phenylephrine and methoxamine to the right (by 0.94 and 1.1 log units, respectively) and had no effect on the concentration-response curve of UK-14,304, while 20 nmol/l yohimbine caused a marked parallel shift of the concentration-response curve of UK-14,304 to the right (by 1.18 log units) and caused only minor displacements of those of phenylephrine and methoxamine (by 0.2 and 0.33 log units, respectively). After exposure of the strips to 30 nmol/l phenoxybenzamine, prazosin (56 nmol/l) caused small shifts of the concentration-response curves of both phenylephrine (by 0.36 log units) and methoxamine (by 0.31 log units) and did not change that of UK-14,304, while yohimbine (20 nmol/l) caused pronounced parallel shifts of the concentration-response curves (to the right) of all the agonists: phenylephrine (by 1.0 log units), methoxamine (by 0.93 log units) and UK-14,304 (by 1.28 log units).(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

在犬隐静脉(一种同时具有突触后α1和α2肾上腺素能受体的组织)中,比较了两种选择性α1肾上腺素能受体激动剂(去氧肾上腺素和甲氧明)与选择性α2肾上腺素能受体激动剂UK-14,304在酚苄明处理前后的作用。此外,还研究了哌唑嗪、育亨宾和维拉帕米在酚苄明处理前后对这些激动剂作用的影响。在没有酚苄明的情况下,哌唑嗪(56 nmol/l)使去氧肾上腺素和甲氧明的浓度-反应曲线均平行右移(分别右移0.94和1.1对数单位),而对UK-14,304的浓度-反应曲线无影响;而20 nmol/l育亨宾使UK-14,304的浓度-反应曲线明显平行右移(右移1.18对数单位),对去氧肾上腺素和甲氧明的浓度-反应曲线仅产生微小位移(分别右移0.2和0.33对数单位)。将组织条暴露于30 nmol/l酚苄明后,哌唑嗪(56 nmol/l)使去氧肾上腺素(右移0.36对数单位)和甲氧明(右移0.31对数单位)的浓度-反应曲线有小幅度右移,对UK-14,304的浓度-反应曲线无改变;而育亨宾(20 nmol/l)使所有激动剂的浓度-反应曲线均明显平行右移(右移):去氧肾上腺素(右移1.0对数单位)、甲氧明(右移0.93对数单位)和UK-14,304(右移1.28对数单位)。(摘要截短于第250个词)

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