Hageman G R, Neely B H, Urthaler F, Rosenshtraukh L V
J Pharmacol Exp Ther. 1986 Jan;236(1):75-9.
This study examined the effects of the diethylamino analog of ethmozin (ethacizin) (1 mg/kg i.v.) on the spontaneous and reflexly elicited efferent activity in thoracic cardiac sympathetic and parasympathetic nerves. Nitroglycerin and phenylephrine (4 and 8 micrograms/kg i.v.) were administered to 15 anesthetized mongrel dogs while monitoring blood pressure and heart rate. In each dog two cardiac nerves were isolated and efferent neurograms were recorded simultaneously and analyzed by microprocessor. Ethacizin significantly attenuated the spontaneous sympathetic efferent activity in both left and right, preganglionic (n = 8) and postganglionic (n = 14) sympathetic nerves to the heart. In contrast, reflex changes in sympathetic activity elicited by baroreceptor challenges were not affected by ethacizin. Also, ethacizin did not significantly affect either spontaneous or baroreceptor reflex-induced parasympathetic efferent activities in eight preganglionic nerves. Thus, this new phenothiazine derivative may exert part of its antiarrhythmic action through a reduction of the spontaneous sympathetic tonic discharges to the heart. The fact that ethacizin reduced neither the reflex-induced changes in sympathetic or parasympathetic activities nor influenced the tonic vagal discharges further suggests that the compound is not likely to interfere with reflexly mediated cardiovascular adaptive changes.
本研究考察了乙吗噻嗪(ethacizin)的二乙氨基类似物(1毫克/千克静脉注射)对胸段心交感神经和副交感神经的自发及反射性传出活动的影响。对15只麻醉的杂种犬静脉注射硝酸甘油和去氧肾上腺素(4和8微克/千克),同时监测血压和心率。在每只犬中分离出两条心脏神经,同时记录传出神经电图并通过微处理器进行分析。乙吗噻嗪显著减弱了左右两侧节前(n = 8)和节后(n = 14)心交感神经的自发交感传出活动。相比之下,压力感受器刺激引起的交感活动反射性变化不受乙吗噻嗪影响。此外,乙吗噻嗪对8条节前神经的自发或压力感受器反射诱发的副交感传出活动均无显著影响。因此,这种新的吩噻嗪衍生物可能通过减少心脏的自发交感紧张性放电发挥其部分抗心律失常作用。乙吗噻嗪既不降低交感或副交感活动的反射性变化,也不影响迷走神经的紧张性放电,这一事实进一步表明该化合物不太可能干扰反射介导的心血管适应性变化。