pH对局部麻醉药抑制平滑肌收缩作用的影响。
Influence of pH on the inhibitory action of local anaesthetics on smooth muscle contraction.
作者信息
Antonio A, Rocha e Silva M, Yashuda Y
出版信息
Br J Pharmacol. 1970 Nov;40(3):501-7. doi: 10.1111/j.1476-5381.1970.tb10631.x.
Abstract
- The guinea-pig isolated ileum kept in a calcium-free depolarizing solution contracts when calcium is added; the responses are proportional to the concentration of calcium and are reversed by washing.2. The contractions elicited by calcium are inhibited by three different classes of compounds: local anaesthetics, pentobarbitone and ethanol. The inhibitory action of the local anaesthetics increases with an increase in pH, the inhibitory action of pentobarbitone increases with a decrease in pH and the inhibitory action of ethanol is not affected by variations in Tyrode pH.3. It is suggested that the antagonists are active when unionized and that the inhibition is obtained when unionized compounds have dissolved in the lipid material of the cell membrane. The possible site of action of the antagonists is discussed.
摘要
置于无钙去极化溶液中的豚鼠离体回肠，在添加钙时会收缩；反应与钙浓度成正比，且通过冲洗可逆转。
钙引发的收缩受到三类不同化合物的抑制：局部麻醉药、戊巴比妥和乙醇。局部麻醉药的抑制作用随pH升高而增强，戊巴比妥的抑制作用随pH降低而增强，乙醇的抑制作用不受台氏液pH变化的影响。
提示拮抗剂在非离子化状态时具有活性，且当非离子化化合物溶解于细胞膜的脂质物质中时会产生抑制作用。讨论了拮抗剂可能的作用位点。
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