3,6-[二甲氨基]-二苯骈碘杂六环葡萄糖酸盐对家兔主动脉条收缩的影响

Effect of 3,6-Dimethamidodibenzopyriodonium Gluconate on Contraction of Rabbit aortic Strips

目的 :观察 3,6-[二甲氨基 ]-二苯骈碘杂六环葡萄糖酸盐 ( -93)对家兔主动脉条收缩的影响。方法 :采用离体血管张力实验法 ,观察 -93的扩血管作用。结果 : -93 1 0～ 30 μmol/ L能剂量依赖性抑制 KCl、Ca Cl2 和 NE引起的家兔主动脉条的收缩 ,使量效曲线右移 ,最大收缩反应降低 ,属非竞争性拮抗 ;在 NE引起的家兔主动脉条收缩两相反应中 , -931 0 μmol/ L明显抑制 NE依赖细胞内 Ca2 + 释放的快相收缩反应 ,对依赖细胞外 Ca2 + 内流的慢相收缩反应无明显影响。结论 : -93呈剂量依赖性、非竞争性拮抗 KCl、Ca Cl2 和 NE引起的家兔主动脉条的收缩 , -93既能抑制肌膜电压依赖性 Ca2 + 通道 ,又能抑制肌浆网的 Ca2 + 释放。

AIM: To study the effect of 3,6 dimethamidodibenzopyriodonium gluconate(Ⅰ 93) on contraction of rabbit aortic stripes. METHODS: Using isolated vascular methods to study the dilating effect of Ⅰ 93. RESULTS: The contractions induced by KCl, CaCl\-2, NE in rabbit aortic strips were dose dependently inhibited by Ⅰ 93 10~30 mol·L\+\{-1\}. Their concentration response curves were in the same manner of noncompetitive antagonism and the pD2 values had no significant difference. Ⅰ 93 inhibited the intracellular Ca\+\{2+\} dependent component (fast phae) of contraction evoked by NE in rabbit aortic strips and had little effect on the extracellular Ca\+\{2+\} dependent component (slow phase). CONCLUSION: Ⅰ 93 showed a dose dependent and noncompetitive antagonist effect on contraction of rabbit aortic stripes induced by KCl, CaCl\-2, NE. The Ca\+\{2+\} releaes from intracellular stores of vascular smooth muscle cells was the main step blocked by Ⅰ 93 and Ⅰ 93 also blocked Ca\+\{2+\} influx through potential dependent calcium channel.