Sadavongvivad C, Satayavivad J
Br J Pharmacol. 1974 Sep;52(1):93-6. doi: 10.1111/j.1476-5381.1974.tb09691.x.
1 The interaction of pilocarpine and isoprenaline on heart rate was investigated in the spontaneously beating, right isolated atrium of the rat.2 The log dose-effect curve of isoprenaline, measured in the presence of various concentrations of pilocarpine, was not modified when the concentration of the latter did not exceed 10(-6)M even though significant slowing of the heart had occurred. At concentrations higher than 10(-6)M a rapid but graded shift to the right of isoprenaline response curves occurred so that at pilocarpine 10(-5)M the pD(2) of isoprenaline was reduced from 11 to 3.3; cocaine slightly reduced this antagonism.3 It is concluded that pilocarpine antagonizes isoprenaline by some mechanism which is not of the simple competitive type.
1 在大鼠右心房离体自搏标本上研究了毛果芸香碱与异丙肾上腺素对心率的相互作用。
2 在存在不同浓度毛果芸香碱的情况下测定异丙肾上腺素的对数剂量效应曲线,当后者浓度不超过10⁻⁶M时,尽管已出现明显的心率减慢,但异丙肾上腺素的效应曲线未发生改变。当浓度高于10⁻⁶M时,异丙肾上腺素反应曲线迅速但呈梯度地向右移位,以至于在毛果芸香碱浓度为10⁻⁵M时,异丙肾上腺素的pD₂从11降至3.3;可卡因可轻微减轻这种拮抗作用。
3 结论是,毛果芸香碱通过某种并非简单竞争性类型的机制拮抗异丙肾上腺素。