Leung E, Mitchelson F
Clin Exp Pharmacol Physiol. 1983 Nov-Dec;10(6):629-39. doi: 10.1111/j.1440-1681.1983.tb00850.x.
The effect of pancuronium in the rabbit ear artery was investigated in order to measure the inhibition it produces at the prejunctional muscarinic receptor on sympathetic nerve endings in this tissue. Pancuronium (0.1-0.2 mmol/l) produced an enhancement of responses to transmural electrical stimulation but this effect was absent in experiments conducted in the presence of cocaine (10 mumol/l) suggesting that an inhibition of the uptake1 mechanism occurs with pancuronium in this tissue. Pancuronium (10 mumol/l) in the presence of cocaine (10 mumol/l) and yohimbine (1 mumol/l) caused a small transient increase in resting output of tritium from arteries preincubated with 3H-noradrenaline but did not affect stimulated output of tritium nor the perfusion pressure in perfused preparations. Pancuronium in the presence of cocaine or cocaine plus yohimbine caused a parallel shift of the concentration-response curve for the inhibitory effect of carbachol (CCh) on the increase in perfusion pressure induced by nervous stimulation. An Arunlakshana-Schild plot of the data was linear but the slopes of 0.92 and 0.95 respectively, were significantly different from unity (P less than 0.05). The calculated pKB value suggests that pancuronium has a different affinity for prejunctional muscarinic receptors on sympathetic nerve endings in this tissue compared to that previously reported in cardiac or ileal smooth muscle.
为了测定泮库溴铵对兔耳动脉组织交感神经末梢节前毒蕈碱受体的抑制作用，对其效应进行了研究。泮库溴铵（0.1 - 0.2 mmol/l）可增强对跨壁电刺激的反应，但在存在可卡因（10 μmol/l）的实验中此效应消失，这表明该组织中泮库溴铵会抑制摄取1机制。在存在可卡因（10 μmol/l）和育亨宾（1 μmol/l）的情况下，泮库溴铵（10 μmol/l）使预先用3H - 去甲肾上腺素孵育的动脉的静息氚输出量出现短暂小幅增加，但不影响刺激后的氚输出量，也不影响灌注制剂中的灌注压力。在存在可卡因或可卡因加育亨宾的情况下，泮库溴铵使卡巴胆碱（CCh）对神经刺激诱导的灌注压力增加的抑制作用的浓度 - 反应曲线发生平行移动。对数据进行的阿伦拉克沙纳 - 希尔（Arunlakshana - Schild）作图呈线性，但斜率分别为0.92和0.95，与1显著不同（P小于0.05）。计算得出的pKB值表明，与先前在心脏或回肠平滑肌中报道的情况相比，泮库溴铵对该组织交感神经末梢节前毒蕈碱受体的亲和力不同。
