Taylor S E, McWhorter K
Department of Pharmacology, Baylor College of Dentistry, Dallas, Texas.
J Pharmacol Exp Ther. 1991 May;257(2):582-6.
Previous studies have reported that maximally effective concentrations of the "mixed" alpha and beta adrenoceptor agonists, epinephrine and norepinephrine, cause greater amounts of mucin secretion than the "pure" beta adrenoceptor agonist, isoproterenol, and that this response requires extracellular calcium. The purpose of the present study was to examine directly the nature of the effect of the putative pure alpha adrenoceptor agonist, phenylephrine, on isoproterenol-induced mucin secretion and the role of extracellular calcium in this interaction. We used a graphical method which provides a procedure for determining whether interaction between two drugs is additive, antagonistic or synergistic to analyze this interaction. Submandibular glands were removed from male rats, divided into sections and placed in modified Hank's balanced salt solution. Mucin secretion was measured as acid precipitable disintegrations per minute after labeling the submandibular gland with [14C]glucosamine. Phenylephrine caused a small but significant secretion of mucin which was blocked partially by phentolamine and completely by propranolol. Phenylephrine caused a significant shift of the isoproterenol concentration-response curve to the left of the theoretical curve expected if two drugs act additively. Mucin secretion induced by isoproterenol alone was independent of extracellular calcium concentration; however, the combination of isoproterenol and phenylephrine caused a concentration-dependency on extracellular calcium.
以往的研究报道,“混合性”α和β肾上腺素能受体激动剂肾上腺素和去甲肾上腺素的最大有效浓度所引起的粘蛋白分泌量,比“单纯性”β肾上腺素能受体激动剂异丙肾上腺素所引起的更多,而且这种反应需要细胞外钙。本研究的目的是直接检测推定的单纯α肾上腺素能受体激动剂去氧肾上腺素对异丙肾上腺素诱导的粘蛋白分泌的影响性质,以及细胞外钙在这种相互作用中的作用。我们采用一种图解法来分析这种相互作用,该方法提供了一种确定两种药物之间的相互作用是相加、拮抗还是协同的程序。从雄性大鼠身上取出下颌下腺,切成小块,置于改良的汉克平衡盐溶液中。用[14C]葡糖胺标记下颌下腺后,以每分钟酸沉淀分解数来测量粘蛋白分泌量。去氧肾上腺素引起少量但显著的粘蛋白分泌,酚妥拉明可部分阻断,普萘洛尔则可完全阻断。如果两种药物呈相加作用,去氧肾上腺素使异丙肾上腺素浓度-反应曲线显著左移至预期的理论曲线左侧。单独使用异丙肾上腺素诱导的粘蛋白分泌与细胞外钙浓度无关;然而,异丙肾上腺素和去氧肾上腺素的组合对细胞外钙呈现浓度依赖性。