Bury R W, Mashford M L
J Pharmacol Exp Ther. 1976 Jun;197(3):633-40.
The effect of various local anesthetics and other substances known to modify calcium fluxes in cells, on submaximal responses of guinea-pig ileum to substance P, acetylcholine, histamine and barium chloride was determined. Procaine caused a dose-related depression of the response to all the agonists but the response to substance P was far less susceptible to this depression. Lidocaine, bupivacaine, pramoxine and W 6211 also caused a lower degree of attenuation of the response to substance P than the responses to acetylcholine, histamine and barium chloride. Verapamil caused a dose-related depression of responses to all the agonists equally. The use of calcium-free solutions abolished responses to substance P, acetylcholine and histamine. The response to barium chloride was less affected by calcium withdrawal but was reduced markedly. In the presence of 10 mM lanthanum chloride, the response to all the agonists was abolished. The relative resistance of the substance P responses to antagonism by local anesthetics suggests that different and more efficient channels for calcium entry into the smooth muscle cell are involved.
测定了各种局部麻醉药和其他已知可改变细胞钙通量的物质，对豚鼠回肠对P物质、乙酰胆碱、组胺和氯化钡的次最大反应的影响。普鲁卡因导致对所有激动剂的反应呈剂量相关的抑制，但对P物质的反应对这种抑制的敏感性要低得多。利多卡因、布比卡因、丙氧卡因和W 6211对P物质反应的减弱程度也低于对乙酰胆碱、组胺和氯化钡的反应。维拉帕米导致对所有激动剂的反应呈剂量相关的同等程度抑制。使用无钙溶液可消除对P物质、乙酰胆碱和组胺的反应。对氯化钡的反应受钙缺失的影响较小，但明显降低。在存在10 mM氯化镧的情况下，对所有激动剂的反应均被消除。P物质反应对局部麻醉药拮抗作用的相对抗性表明，涉及不同且更有效的钙进入平滑肌细胞的通道。
