Kontani H, Koshiura R
Jpn J Pharmacol. 1983 Jun;33(3):503-13. doi: 10.1254/jjp.33.503.
Effects of local anesthetics, tetrodotoxin (TTX), aconitine and verapamil on the rate of afferent discharges from the mechanoreceptors of isolated hearts of the bullfrog were studied. When procaine (1 X 10(-4) M), tetracaine (1 X 10(-6) M) and dibucaine (1 X 10(-5) M) decreased the contractile force and beating rate of the heart, high frequency discharges that were synchronized with the contraction of the heart appeared. When concentrations of these local anesthetics were increased, the afferent discharges were abolished. When TTX (1 X 10(-8) M - 1 X 10(-7) M) caused a cardiac arrest, high frequency discharges, consisting of maintained discharges and the discharges synchronized with small contractions of the ventricle, appeared. Occasionally, in the presence of TTX (1 X 10(-7) M) the cardiac arrest occurred, and then very irregular contractions appeared. At that time, high frequency discharges synchronized with contractions appeared. On the other hand, aconitine (1 X 10(-7) M - 1 X 10(-6) M) initially increased the rate of afferent discharges from mechanoreceptors in the atrium and ventricle and then abolished the discharges without significantly affecting beating rhythms and contractile force. When verapamil (1 X 10(-6) M - 1 X 10(-5) M) was applied, the beating rate and contractile force were significantly decreased, but high frequency discharges synchronized with contractions were observed. These results indicate that local anesthetics, TTX and verapamil at those concentrations which depressed the cardiac functions did not inhibit the heart mechanoreceptor excitability and the concentration of aconitine that markedly affected the cardiac functions stimulated the heart mechanoreceptor.
研究了局部麻醉药、河豚毒素(TTX)、乌头碱和维拉帕米对牛蛙离体心脏机械感受器传入放电频率的影响。当普鲁卡因(1×10⁻⁴M)、丁卡因(1×10⁻⁶M)和布比卡因(1×10⁻⁵M)降低心脏收缩力和心率时,出现了与心脏收缩同步的高频放电。当这些局部麻醉药的浓度增加时,传入放电被消除。当TTX(1×10⁻⁸M - 1×10⁻⁷M)导致心脏停搏时,出现了由持续放电和与心室小收缩同步的放电组成的高频放电。偶尔,在TTX(1×10⁻⁷M)存在的情况下会发生心脏停搏,然后出现非常不规则的收缩。此时,出现了与收缩同步的高频放电。另一方面,乌头碱(1×10⁻⁷M - 1×10⁻⁶M)最初增加了心房和心室机械感受器的传入放电频率,然后在不显著影响搏动节律和收缩力的情况下消除了放电。当应用维拉帕米(1×10⁻⁶M - 1×10⁻⁵M)时,心率和收缩力显著降低,但观察到与收缩同步的高频放电。这些结果表明,在那些降低心脏功能的浓度下,局部麻醉药、TTX和维拉帕米并未抑制心脏机械感受器的兴奋性,而显著影响心脏功能的乌头碱浓度刺激了心脏机械感受器。