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局部麻醉药对人隐静脉和牛冠状动脉对神经递质、乙酰胆碱、去甲肾上腺素和5-羟色胺反应的影响。

Effects of local anaesthetics on responses of human saphenous vein and bovine coronary artery to neurotransmitters, acetylcholine, noradrenaline and 5-hydroxytryptamine.

作者信息

Wali F A

出版信息

Gen Pharmacol. 1986;17(4):405-11. doi: 10.1016/0306-3623(86)90182-5.

Abstract

The effects of 5 different local anaesthetics, lignocaine, etidocaine, prilocaine, mepivacaine, bupivacaine, and 3 different neurotransmitters, acetylcholine (ACh), noradrenaline (NA), 5-hydroxytryptamine (5-HT) on tone and contractility of human saphenous vein and bovine coronary artery were studied and compared in vitro. The experiments were carried out to see if there were species or tissue differences in the action of local anaesthetics and neurotransmitters at vascular smooth muscle, i.e. saphenous vein and coronary artery. Another important aspect was to see if local anaesthetics modified cholinergic (ACh), adrenergic (NA) and serotoninergic (5-HT) responses in vascular smooth muscle. Among the local anaesthetics studied, lignocaine and etidocaine produced prolonged relaxations, whereas prilocaine, mepivacaine, bupivacaine produced contractions in the saphenous vein and coronary artery. High concentrations of the latter drugs produced relaxations in the blood vessels. Among the local anaesthetics, lignocaine produced differential effects on saphenous vein and coronary artery, its effect on the latter was 3 times larger than on the saphenous vein. ACh, NA and 5-HT contracted the saphenous vein. In the coronary artery, ACh and 5-HT contracted whereas NA relaxed the vessel. On a molar basis, ACh was less effective than NA in contracting the saphenous vein. 5-HT was equipotent on both the saphenous vein and coronary artery. Lignocaine reduced ACh, NA and 5-HT-induced contractions in the saphenous vein and those of ACh and 5-HT in the coronary artery, and shifted the control curves, non-competitively, to the right. The relaxation produced by NA in the coronary artery was enhanced by lignocaine.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

研究并比较了5种不同的局部麻醉药(利多卡因、依替卡因、丙胺卡因、甲哌卡因、布比卡因)和3种不同的神经递质(乙酰胆碱(ACh)、去甲肾上腺素(NA)、5-羟色胺(5-HT))对人隐静脉和牛冠状动脉张力及收缩性的影响。实验旨在观察局部麻醉药和神经递质在血管平滑肌(即隐静脉和冠状动脉)作用方面是否存在种属或组织差异。另一个重要方面是观察局部麻醉药是否会改变血管平滑肌中的胆碱能(ACh)、肾上腺素能(NA)和5-羟色胺能(5-HT)反应。在所研究的局部麻醉药中,利多卡因和依替卡因产生了长时间的舒张作用,而丙胺卡因、甲哌卡因、布比卡因则使隐静脉和冠状动脉产生收缩。高浓度的后几种药物在血管中产生舒张作用。在局部麻醉药中,利多卡因对隐静脉和冠状动脉产生不同的作用,其对冠状动脉的作用比对隐静脉的作用大3倍。ACh、NA和5-HT使隐静脉收缩。在冠状动脉中,ACh和5-HT使血管收缩,而NA使血管舒张。以摩尔为基础,ACh在使隐静脉收缩方面比NA的作用弱。5-HT在隐静脉和冠状动脉上的作用相当。利多卡因减少了ACh、NA和5-HT在隐静脉中引起的收缩以及ACh和5-HT在冠状动脉中引起的收缩,并将对照曲线非竞争性地向右移动。利多卡因增强了NA在冠状动脉中产生的舒张作用。(摘要截选至250词)

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