蜂毒明肽对豚鼠盲肠带对BRL 34915、尼可地尔及其他舒张剂反应的影响
Effect of apamin on responses to BRL 34915, nicorandil and other relaxants in the guinea-pig taenia caeci.
作者信息
Weir S W, Weston A H
出版信息
Br J Pharmacol. 1986 May;88(1):113-20. doi: 10.1111/j.1476-5381.1986.tb09477.x.
BRL 34915 (4-64 X 10(-7) M), isoprenaline (0.5-32 X 10(-8) M) and nicorandil (4-64 X 10(-6) M) produced a slowly-developing relaxation of spontaneous tone of the guinea-pig taenia caeci; with no after-contraction on washout. These inhibitory responses were unaffected by apamin (10(-7) M). Adenosine triphosphate (0.06-2 X 10(-3) M) and noradrenaline (1-16 X 10(-7) M) produced a rapid inhibition of spontaneous tone with a prominent after-contraction, especially on washout. Both the inhibitory effect and the rebound contraction were abolished by apamin (10(-7) M). Exposure to both BRL 34915 (64 X 10(-7) M) and to nicorandil (64 X 10(-6) M) produced an increase in the 86Rb efflux rate coefficient which was unaffected by apamin (10(-7) M). Exposure to isoprenaline (32 X 10(-8) M) had no effect on the 86Rb efflux rate coefficient. Exposure to noradrenaline (16 X 10(-7) M) produced an increase in the 86Rb efflux rate coefficient which was abolished by apamin (10(-7) M). The results confirm that both BRL 34915 and nicorandil are capable of opening potassium channels in smooth muscle but show that the channel is not apamin-sensitive.
BRL 34915（4 - 64×10⁻⁷ M）、异丙肾上腺素（0.5 - 32×10⁻⁸ M）和尼可地尔（4 - 64×10⁻⁶ M）可使豚鼠盲肠带的自发张力缓慢舒张；洗脱后无后收缩现象。这些抑制反应不受蜂毒明肽（10⁻⁷ M）影响。三磷酸腺苷（0.06 - 2×10⁻³ M）和去甲肾上腺素（1 - 16×10⁻⁷ M）可迅速抑制自发张力，伴有明显的后收缩现象，尤其是在洗脱时。蜂毒明肽（10⁻⁷ M）可消除抑制作用和反弹收缩。暴露于BRL 34915（64×10⁻⁷ M）和尼可地尔（64×10⁻⁶ M）均可使⁸⁶Rb流出速率系数增加，且不受蜂毒明肽（10⁻⁷ M）影响。暴露于异丙肾上腺素（32×10⁻⁸ M）对⁸⁶Rb流出速率系数无影响。暴露于去甲肾上腺素（16×10⁻⁷ M）可使⁸⁶Rb流出速率系数增加，该增加被蜂毒明肽（10⁻⁷ M）消除。结果证实BRL 34915和尼可地尔均能够在平滑肌中打开钾通道，但表明该通道对蜂毒明肽不敏感。
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