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首页> 外文期刊>Life sciences >Pharmacological characteristics of the endothelial target for acetylcholine induced vascular relaxation.
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Pharmacological characteristics of the endothelial target for acetylcholine induced vascular relaxation.

机译：乙酰胆碱诱导的血管舒张的内皮靶的药理特性。

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摘要

The pharmacological characteristics of the endothelial target for acetylcholine induced vascular relaxation were investigated in this experiment. The isolated preparations of arteries were suspended for the measurement of isometric force in modified Krebs-Ringer bicarbonate solution (37 degrees C aerated with 95% O2 and 5% CO2). Similar to acetylcholine, carbachol rather than thiocholine, butylcholine and choline could induce endothelium-dependent relaxation. Among cholinergic receptor agonists, arecoline and oxotremorine rather than nicotine could mimic the effects of acetylcholine. But muscarinic agonist pilocarpine had no effect. This phenomenon was observed in rat, cat and rabbit aorta, as well as cat mesenteric. femoral and renal arteries. The new compound tricyclopinate and phenyl cyclopentyl hydroxyl-ethoxy quinuclidines, the competitive antagonists against muscarinic receptors, displayed noncompetitive antagonism against the endothelial target for acetylcholine. Among the six isomers of the novel compound 2-(2'-cyclopentyl-2'-phenyl-2'-hydroxyl-ethoxy) tropane, the isomers with IS-2alpha-2'R and 1S-2alpha-2'S configuration caused the dose-response curves of acetylcholine for inducing vascular relaxation shift rightward with a parallel manner, while the isomers IR-2alpha-2'R and IR-2alpha-2'S with a nonparallel manner. In addition, the antagonistic effects of the isomer IS-2alpha-2'R against the endothelial target for acetylcholine and against muscarinic receptors were 4570 and 10 times greater than those of the isomer IS-2alpha-2'S respectively. In conclusion, the endothelial target for acetylcholine had the unique pharmacological characteristics different from those of muscarinic receptors.
机译：在该实验中研究了用于乙酰胆碱诱导的血管舒张的内皮靶的药理学特征。将分离的动脉制剂悬浮在改良的Krebs-Ringer碳酸氢盐溶液（37°C，加注95％O2和5％CO2）中，以测定等轴测力。与乙酰胆碱相似，卡巴胆碱而不是硫胆碱，丁胆碱和胆碱可以诱导内皮依赖性舒张。在胆碱能受体激动剂中，槟榔碱和oxotremorine而不是尼古丁可以模拟乙酰胆碱的作用。但是毒蕈碱激动剂毛果芸香碱没有作用。在大鼠，猫和兔的主动脉以及猫的肠系膜中都观察到了这种现象。股和肾动脉。新的化合物三环松酸酯和苯基环戊基羟基-乙氧基奎宁环烷是对毒蕈碱受体的竞争性拮抗剂，对乙酰胆碱的内皮靶标表现出非竞争性拮抗作用。在新型化合物2-（2'-环戊基-2'-苯基-2'-羟基乙氧基）托烷的六个异构体中，具有IS-2alpha-2'R和1S-2alpha-2'S构型的异构体导致剂量升高乙酰胆碱引起的血管舒张反应曲线以平行方式向右移动，而异构体IR-2alpha-2'R和IR-2alpha-2'S以非平行方式向右移动。此外，异构体IS-2alpha-2'R对乙酰胆碱的内皮靶标和毒蕈碱受体的拮抗作用分别是异构体IS-2alpha-2'S的4570和10倍。总之，乙酰胆碱的内皮靶标具有不同于毒蕈碱受体的独特药理特性。

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