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α和β肾上腺素能受体介导的兔肠道抑制作用。

Inhibition of rabbit intestine mediated by alpha- and beta-adrenoceptors.

作者信息

Bowman W C, Hall M T

出版信息

Br J Pharmacol. 1970 Feb;38(2):399-415. doi: 10.1111/j.1476-5381.1970.tb08528.x.

Abstract
  1. The effects of some alpha- and beta-adrenoceptor agonists and antagonists were studied on isolated segments of rabbit intestine in an attempt to characterize the two types of inhibitory response produced by sympathomimetic amines.2. Phenylephrine, an alpha-adrenoceptor agonist, produced an inhibition of rapid onset, from which recovery occurred despite the continued presence of the drug. On washout there was an overshoot in contraction height. Isoprenaline, a beta-adrenoceptor agonist, produced an inhibition of slow onset which was maintained throughout the presence of the drug and there was no overshoot on washout.3. Adrenaline resembled phenylephrine more closely than it resembled isoprenaline, in that it showed more affinity for alpha-adrenoceptors, whereas noradrenaline, and the transmitter released on periarterial nerve stimulation, behaved more like isoprenaline, although both types of receptor were affected.4. Adenosine-5'-triphosphate produced an inhibition resembling that produced by an alpha-adrenoceptor agonist, whereas the dibutyryl analogue of cyclic adenosine 3',5'-monophosphate (cyclic 3',5'-AMP) produced an inhibition resembling that produced by a beta-adrenoceptor agonist.5. In critical concentrations theophylline augmented and imidazole inhibited beta-adrenoceptor mediated responses, as well as responses to dibutyryl cyclic AMP. However, additional actions of theophylline and imidazole were also demonstrated.6. Responses mediated by alpha-adrenoceptors, but not those mediated by beta-adrenoceptors, were blocked by membrane stabilizers, quinidine being the most potent of those studied.7. The results are discussed in relation to the possible mechanisms of action of alpha- and beta-adrenoceptor agonists.
摘要
  1. 研究了一些α和β肾上腺素能受体激动剂及拮抗剂对兔离体肠段的作用,以试图明确拟交感胺产生的两种抑制反应类型。

  2. 苯肾上腺素,一种α肾上腺素能受体激动剂,可迅速产生抑制作用,尽管药物持续存在,仍可恢复。冲洗后收缩高度出现过冲。异丙肾上腺素,一种β肾上腺素能受体激动剂,产生缓慢起效的抑制作用,在药物存在期间一直维持,冲洗后无过冲现象。

  3. 肾上腺素与苯肾上腺素的相似性高于与异丙肾上腺素的相似性,因为它对α肾上腺素能受体表现出更高的亲和力,而去甲肾上腺素以及动脉周围神经刺激时释放的递质,尽管两种受体都受到影响,但表现更像异丙肾上腺素。

  4. 三磷酸腺苷产生的抑制作用类似于α肾上腺素能受体激动剂产生的抑制作用,而环磷腺苷3',5'-二丁酰基类似物(环3',5'-AMP)产生的抑制作用类似于β肾上腺素能受体激动剂产生的抑制作用。

  5. 在临界浓度下,茶碱增强而咪唑抑制β肾上腺素能受体介导的反应以及对二丁酰环磷腺苷的反应。然而,也证明了茶碱和咪唑的其他作用。

  6. α肾上腺素能受体介导的反应,但不是β肾上腺素能受体介导的反应,被膜稳定剂阻断,奎尼丁是所研究的药物中最有效的。

  7. 讨论了与α和β肾上腺素能受体激动剂可能的作用机制相关的结果。

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1
On the nature of inhibition in the intestine.论肠道抑制的本质。
J Physiol. 1930 Sep 18;70(2):145-57. doi: 10.1113/jphysiol.1930.sp002683.
3
Sympatholytic effects of quinine and quinidine.奎宁和奎尼丁的抗交感神经作用。
Am J Physiol. 1950 Jan;160(1):212-6. doi: 10.1152/ajplegacy.1949.160.1.212.
9
Derivatives of cyclic 3',5'-adenosine monophosphate.环磷腺苷的衍生物。
Biochim Biophys Acta. 1962 Dec 17;65:558-60. doi: 10.1016/0006-3002(62)90475-4.

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