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对来自兔子的几种离体血管中 (-)-去甲肾上腺素的节后α-肾上腺素能受体亚型的研究。

An examination of the postjunctional alpha-adrenoceptor subtypes for (-)-noradrenaline in several isolated blood vessels from the rabbit.

作者信息

Daly C J, McGrath J C, Wilson V G

机构信息

Autonomic Physiology Unit, University of Glasgow, Scotland.

出版信息

Br J Pharmacol. 1988 Oct;95(2):473-84. doi: 10.1111/j.1476-5381.1988.tb11668.x.

Abstract
  1. Postjunctional alpha-adrenoceptors in several isolated blood vessels from the rabbit have been characterized on the basis of the relative potency of the agonists noradrenaline (NA, non-selective), phenylephrine (alpha 1-selective) and UK-14304 (alpha 2-selective), and the potency of antagonists rauwolscine (alpha 2-selective) and corynanthine (alpha 1-selective) against contractions elicited by NA. In addition, the potency of prazosin against NA was also assessed in the venous preparations. 2. The thoracic aorta, ear artery and left renal vein appear to possess alpha 1-adrenoceptors since the agonist potency order was NA greater than phenylephrine greater than UK-14304, while corynanthine was 3-10 fold more potent than rauwolscine. 3. The ear vein appears to possess alpha 2-adrenoceptors. The rank order of agonist potency was UK-14304 greater than NA much greater than phenylephrine and all three agonists elicited responses of similar magnitude. Furthermore, rauwolscine was 30 fold more potent than corynanthine while prazosin failed to produce a concentration-dependent inhibition. 4. The saphenous vein and the plantaris vein appear to possess a mixture of both subtypes since the rank order of agonist potency was UK-14304 greater than NA much greater than phenylephrine, while responses elicited by UK-14304 were smaller than those to the other agonists. However, although rauwolscine was 20 to 100 fold more potent than corynanthine in both preparations, suggestive of predominantly alpha 2-adrenoceptors, prazosin was either potent (saphenous vein) or relatively inactive (plantaris vein). 5. The characteristics of postjunctional alpha 1- and alpha 2-adrenoceptors on isolated blood vessels from the rabbit are discussed in relation to the value of both the agonists, particularly NA, and the antagonists used in this study.
摘要
  1. 基于激动剂去甲肾上腺素(NA,非选择性)、苯肾上腺素(α1选择性)和UK-14304(α2选择性)的相对效价,以及拮抗剂萝芙辛(α2选择性)和育亨宾(α1选择性)对NA引起的收缩的拮抗效价,对来自家兔的几种离体血管中的节后α-肾上腺素能受体进行了表征。此外,还在静脉制剂中评估了哌唑嗪对NA的效价。2. 胸主动脉、耳动脉和左肾静脉似乎具有α1-肾上腺素能受体,因为激动剂效价顺序为NA>苯肾上腺素>UK-14304,而育亨宾的效价比萝芙辛强3至10倍。3. 耳静脉似乎具有α2-肾上腺素能受体。激动剂效价顺序为UK-14304>NA>>苯肾上腺素,且所有三种激动剂引起的反应幅度相似。此外,萝芙辛的效价比育亨宾强30倍,而哌唑嗪未能产生浓度依赖性抑制。4. 隐静脉和跖静脉似乎同时具有两种亚型,因为激动剂效价顺序为UK-14304>NA>>苯肾上腺素,而UK-14304引起的反应比其他激动剂小。然而,尽管在两种制剂中萝芙辛的效价比育亨宾强20至100倍,提示主要为α2-肾上腺素能受体,但哌唑嗪要么有效(隐静脉),要么相对无活性(跖静脉)。5. 结合本研究中使用的激动剂尤其是NA和拮抗剂的价值,讨论了家兔离体血管中节后α1和α2-肾上腺素能受体的特征。

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