Ettaiche M, Athias P, Variot N, Klepping J
Can J Physiol Pharmacol. 1985 Oct;63(10):1221-7. doi: 10.1139/y85-202.
The effects of agonists and antagonists, specific for the different adrenoceptor subtypes on the automaticity of cultured ventricular cells from postnatal rat, were studied. Chronotropic responses were assessed by recording monophasic action potentials using intracellular microelectrodes. Contraction was assessed by an electro-optical procedure. (-)-Isoproterenol, salbutamol, (-)-phenylephrine, and methoxamine increased the spontaneous rate in a dose-dependent manner, but the stimulatory potencies of alpha-adrenoceptor agonists were weaker than those of the beta-alternates. The frequency response to (-)-isoproterenol was inhibited by atenolol but not by butoxamine. Atenolol was also more effective than butoxamine in antagonizing the rate acceleration by salbutamol. The chronotropic effects of phenylephrine and methoxamine were inhibited by prazosin. In contrast, neither clonidine nor yohimbine displayed any chronotropic action. These findings suggest that the postjunctional adrenoceptors present in the sarcolemma of the isolated cardiac muscle cells, which mediate automaticity responses to catecholamines, are of beta 1, beta 2, and alpha 1 types, the physiological contribution of the beta 1-adrenoceptors being predominant. Applicability of these conclusions to the in situ myocardiocytes is discussed with respect to the level of functional differentiation achieved by the rat myocardial cells in culture.
研究了针对不同肾上腺素能受体亚型的激动剂和拮抗剂对新生大鼠培养心室细胞自律性的影响。通过使用细胞内微电极记录单相动作电位来评估变时性反应。通过光电程序评估收缩情况。(-)-异丙肾上腺素、沙丁胺醇、(-)-去氧肾上腺素和甲氧明以剂量依赖的方式增加自发频率,但α-肾上腺素能受体激动剂的刺激效力比β-肾上腺素能受体激动剂弱。阿替洛尔抑制对(-)-异丙肾上腺素的频率反应,但布托沙明无此作用。在拮抗沙丁胺醇引起的频率加快方面,阿替洛尔也比布托沙明更有效。哌唑嗪抑制去氧肾上腺素和甲氧明的变时性作用。相反,可乐定和育亨宾均未表现出任何变时性作用。这些发现表明,存在于分离的心肌细胞肌膜中的节后肾上腺素能受体介导对儿茶酚胺的自律性反应,它们属于β1、β2和α1型,其中β1-肾上腺素能受体的生理作用占主导。结合培养的大鼠心肌细胞所达到的功能分化水平,讨论了这些结论对原位心肌细胞的适用性。