Suzuki N, Inagaki O, Kasuya Y
Jpn J Pharmacol. 1986 Mar;40(3):455-62. doi: 10.1254/jjp.40.455.
Inhibitory effects of propranolol on the contractions to various treatments were investigated in the epididymal half of the rat vas deferens. Reportedly, 10(-5)-3 X 10(-4) M propranolol inhibited 150 mM K-induced contractions dose-dependently; 3 X 10(-4) M propranolol abolished the contractions. The present results showed that propranolol at concentrations up to 10(-4) M did not inhibit the maximal contractions to 10(-3) M norepinephrine (NE) or 10(-2) M methacholine (MCh). Propranolol at 3 X 10(-4) M slightly inhibited contractions to NE and MCh by 11% and 12%, respectively. In contrast, propranolol inhibited twitch components of the contractions induced by nerve stimulations at similar doses to those reported for high K contractions. Propranolol also inhibited contractions to Ca in high K-containing solution and shifted the dose-response curve to the right. Propranolol did not affect the depolarizations by high K measured by microelectrodes. Propranolol at concentrations of 10(-5)-3 X 10(-5) M diminished the magnitude of spikes dose-dependently. Spikes were rarely observed in the presence of 10(-4) M propranolol in spite of generation of e.j.p.s with amplitudes that would be sufficient to induce spikes in the absence of propranolol. These results suggest that propranolol inhibits contractions by decreasing Ca-influx through the potential-operated Ca-channels in the smooth muscle cells of rat vas deferens.
在大鼠输精管附睾段研究了普萘洛尔对各种处理引起的收缩的抑制作用。据报道,10^(-5)-3×10^(-4)M的普萘洛尔剂量依赖性地抑制150mM钾诱导的收缩;3×10^(-4)M的普萘洛尔可消除收缩。目前的结果表明,浓度高达10^(-4)M的普萘洛尔不会抑制对10^(-3)M去甲肾上腺素(NE)或10^(-2)M乙酰甲胆碱(MCh)的最大收缩。3×10^(-4)M的普萘洛尔分别使对NE和MCh的收缩轻微抑制11%和12%。相比之下,普萘洛尔以与高钾收缩报道的相似剂量抑制神经刺激诱导的收缩的抽搐成分。普萘洛尔还抑制含高钾溶液中对钙的收缩,并使剂量反应曲线右移。普萘洛尔不影响微电极测量的高钾引起的去极化。浓度为10^(-5)-3×10^(-5)M的普萘洛尔剂量依赖性地减小动作电位幅度。尽管产生了幅度足以在无普萘洛尔时诱导动作电位的终板电位,但在存在10^(-4)M普萘洛尔时很少观察到动作电位。这些结果表明,普萘洛尔通过减少大鼠输精管平滑肌细胞中通过电压门控钙通道的钙内流来抑制收缩。