Rosenfeld G C
J Pharmacol Exp Ther. 1984 Jun;229(3):763-7.
Isoproterenol (Iso), epinephrine and norepinephrine each stimulated isolated gastric mucosal parietal cells as shown by an increased accumulation of [14C]aminopyrine (AP), an indirect measure of acid secretion. The beta receptor selective agonists metaproterenol, terbutaline and zinterol stimulated AP accumulation to the same extent as Iso, whereas the beta-1 receptor selective agonist dobutamine was only 20% as effective. The general beta receptor antagonists oxprenolol and dl-propranolol and the beta-2 receptor antagonist H35/25 inhibited Iso-stimulated AP accumulation. Receptor stereoselectivity was shown by the approximately 100-fold difference in potency of the I- and d-isomers of propranolol. The alpha receptor antagonists phentolamine and phenoxybenzamine, the beta-1 receptor antagonists metoprolol and practolol and the muscarinic receptor antagonist atropine were without effect. The histamine H2-receptor antagonist cimetidine inhibited Iso-stimulated AP accumulation an average of 40% at a concentration which inhibits completely histamine-stimulated AP accumulation. The data demonstrate that cells of the rat gastric mucosa have adrenergic beta-2 receptors which when stimulated result in an increase in acid secretion. The results also show that the response is in part mediated indirectly by catecholamine-stimulated release of histamine.
异丙肾上腺素(Iso)、肾上腺素和去甲肾上腺素均刺激离体胃黏膜壁细胞,表现为[14C]氨基比林(AP)蓄积增加,这是酸分泌的一种间接测量方法。β受体选择性激动剂间羟异丙肾上腺素、特布他林和辛特罗对AP蓄积的刺激程度与Iso相同,而β-1受体选择性激动剂多巴酚丁胺的效力仅为Iso的20%。一般β受体拮抗剂氧烯洛尔和dl-普萘洛尔以及β-2受体拮抗剂H35/25抑制Iso刺激的AP蓄积。普萘洛尔的I-和d-异构体效力相差约100倍,显示出受体立体选择性。α受体拮抗剂酚妥拉明和酚苄明、β-1受体拮抗剂美托洛尔和普拉洛尔以及毒蕈碱受体拮抗剂阿托品均无作用。组胺H2受体拮抗剂西咪替丁在完全抑制组胺刺激的AP蓄积的浓度下,平均抑制Iso刺激的AP蓄积40%。数据表明,大鼠胃黏膜细胞具有肾上腺素能β-2受体,受到刺激时会导致酸分泌增加。结果还表明,该反应部分是由儿茶酚胺刺激组胺释放间接介导的。