有证据表明，一种非典型β-肾上腺素能受体介导了利托君和沙丁胺醇对兔离体空肠自发性节律性收缩的抑制作用。
Evidence that an atypical beta-adrenoceptor mediates the inhibition of spontaneous rhythmical contractions of rabbit isolated jejunum induced by ritodrine and salbutamol.
作者信息
Norman B J, Leathard H L
机构信息
Department of Pharmacology, Charing Cross and Westminster Medical School, London.
出版信息
Br J Pharmacol. 1990 Sep;101(1):27-30. doi: 10.1111/j.1476-5381.1990.tb12083.x.
Abstract
- The nature of the adrenoceptors mediating the inhibitory action of noradrenaline, ritodrine and salbutamol on the spontaneous activity of longitudinal muscle of the rabbit jejunum in vitro was investigated by use of a range of adrenoceptor antagonists. 2. The actions of ritodrine and salbutamol were antagonized competitively by propranolol. The pA2 values of 6.4 and 6.6 respectively were smaller than those found elsewhere for beta 1- and beta 2-adrenoceptors. 3. In contrast, the responses to ritodrine and salbutamol were antagonized only by high concentrations (greater than 2.7 microM) of phentolamine and were unaffected by yohimbine (2.6 microM), mepyramine (2.5 microM) or cimetidine (4.0 microM). 4. Ritodrine which is less potent than salbutamol in tissues with typical beta 2-adrenoceptors was found to be 8 times more potent than salbutamol in the rabbit jejunum. 5. It is suggested that in the rabbit jejunum ritodrine and salbutamol may act at an atypical beta-adrenoceptor, at which propranolol is a competitive but not very potent antagonist.
摘要
- 利用一系列肾上腺素能受体拮抗剂，研究了介导去甲肾上腺素、利托君和沙丁胺醇对体外兔空肠纵肌自发活动抑制作用的肾上腺素能受体的性质。2. 普萘洛尔竞争性拮抗利托君和沙丁胺醇的作用。其pA2值分别为6.4和6.6，低于其他地方报道的β1和β2肾上腺素能受体的pA2值。3. 相比之下，仅高浓度（大于2.7微摩尔）的酚妥拉明能拮抗对利托君和沙丁胺醇的反应，而育亨宾（2.6微摩尔）、美吡拉敏（2.5微摩尔）或西咪替丁（4.0微摩尔）对此无影响。4. 在具有典型β2肾上腺素能受体的组织中效力低于沙丁胺醇的利托君，在兔空肠中的效力却比沙丁胺醇高8倍。5. 提示在兔空肠中，利托君和沙丁胺醇可能作用于一种非典型β肾上腺素能受体，普萘洛尔是该受体的竞争性拮抗剂，但效力不强。
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