Prostran M, Varagic V M
Department of Pharmacology, Faculty of Medicine, Belgrado, Yugoslavia.
Arch Int Pharmacodyn Ther. 1988 Jul-Aug;294:137-48.
5'-N-Ethylcarboxamide adenosine (NECA) (2.2-22 nmol l-1) produced a concentration-dependent depression of both the isometric contraction and the atrial rate of the isolated, spontaneously beating guinea-pig atria. In the presence of a standard concentration of verapamil (73 nmol l-1), the dose-response curves for NECA, both for the isometric contraction and the atrial rate, were significantly shifted to the left. The inhibitory effect of NECA on the atria was almost completely reversed by the addition of calcium chloride (1.8 mmol l-1) into the organ bath. The depressive actions of NECA on the isolated atria were also antagonized by aminophylline (32 mumol l-1) and isoprenaline (24 nmol l-1). In the presence of XAC (Xanthine Amine Congener) (0.5 mumol l-1) the dose-response curve for the effect of NECA on the isometric contraction was significantly shifted to the right. In the concentration used, XAC produced no changes either in the isometric contraction or in the atrial rate. These experiments indicate that NECA may act on the adenosine A1-receptors present in the guinea-pig atria because its effects on the atria are antagonized by XAC, a more selective A1-receptor antagonist. It is concluded that NECA might act through depression of calcium channel function in the heart atria, and that the action of NECA most probably implicates A1-receptors.
5'-N-乙基甲酰胺腺苷(NECA)(2.2 - 22纳摩尔/升)可使离体自发搏动的豚鼠心房的等长收缩和心房率产生浓度依赖性降低。在标准浓度维拉帕米(73纳摩尔/升)存在的情况下,NECA对等长收缩和心房率的剂量反应曲线均显著左移。向器官浴槽中加入氯化钙(1.8毫摩尔/升)后,NECA对心房的抑制作用几乎完全逆转。NECA对离体心房的抑制作用也受到氨茶碱(32微摩尔/升)和异丙肾上腺素(24纳摩尔/升)的拮抗。在黄嘌呤胺类化合物(XAC)(0.5微摩尔/升)存在的情况下,NECA对等长收缩作用的剂量反应曲线显著右移。在所使用的浓度下,XAC对等长收缩或心房率均无影响。这些实验表明,NECA可能作用于豚鼠心房中存在的腺苷A1受体,因为其对心房的作用受到XAC(一种更具选择性的A1受体拮抗剂)的拮抗。结论是,NECA可能通过抑制心房中的钙通道功能起作用,并且NECA的作用很可能涉及A1受体。