BURN J H, GIBBONS W R
Br J Pharmacol Chemother. 1964 Jun;22(3):527-39. doi: 10.1111/j.1476-5381.1964.tb01707.x.
The effect of phenoxybenzamine has been determined on the physiological response to sympathetic stimulation in two preparations, the rabbit isolated ileum and the guinea-pig isolated vas deferens. In both preparations phenoxybenzamine increased the response to stimulation of low frequency, the response being inhibitory in the one and motor in the other. This increase was large. As the stimulus frequency was raised, phenoxybenzamine caused a progressively smaller increase in the response, and at high frequencies phenoxybenzamine decreased the response. These observations agree with those of earlier workers who showed that antiadrenaline substances have more than one property. They not only block the motor effects of adrenaline and noradrenaline, but at the same time they may increase the response to sympathetic stimulation. The observations which have been made are not consistent with the interpretation which has been placed by others on the effect of phenoxybenzamine on the amount of noradrenaline appearing in the splenic vein following sympathetic stimulation; this interpretation assumes that phenoxybenzamine will decrease the response to sympathetic stimulation at low frequency. The mode of action of phenoxybenzamine is discussed, and fresh evidence that it has an anticholinesterase action is given.
已在两种标本(兔离体回肠和豚鼠离体输精管)中测定了酚苄明对交感神经刺激的生理反应的影响。在这两种标本中,酚苄明均增强了对低频刺激的反应,在一种标本中反应为抑制性,在另一种标本中反应为运动性。这种增强幅度很大。随着刺激频率升高,酚苄明引起的反应增强逐渐减小,在高频时酚苄明使反应减弱。这些观察结果与早期研究者的结果一致,他们表明抗肾上腺素物质具有多种特性。它们不仅阻断肾上腺素和去甲肾上腺素的运动效应,而且同时可能增强对交感神经刺激的反应。所做的观察结果与其他人对酚苄明对交感神经刺激后脾静脉中去甲肾上腺素含量的影响的解释不一致;这种解释认为酚苄明在低频时会减弱对交感神经刺激的反应。讨论了酚苄明的作用方式,并给出了它具有抗胆碱酯酶作用的新证据。