Gandhi D N, Gulati O D, Hemavathi K G
Arch Int Pharmacodyn Ther. 1983 Apr;262(2):189-98.
The effects of varying the concentration of Mg++ in the incubation medium on the contractile responses of rat isolated seminal vesicle to 5-hydroxytryptamine (5-HT) were investigated in the absence and presence of EDTA. Preparations incubated in Mg++-free and Mg++ excess media showed supersensitivity and subsensitivity to 5-HT respectively. In the presence of EDTA alterations in the sensitivity to 5-HT produced by varying the concentrations of Mg++ were comparatively less. Preparations obtained from reserpinized animals showed subsensitivity in normal and Mg++ excess media and supersensitivity in Mg++-free medium. In the presence of EDTA, reserpinized preparations showed slight supersensitivity in normal Mg++ medium, marked supersensitivity in Mg++-free medium and lesser subsensitivity in Mg++ excess medium. Probably EDTA by more effectively removing Mg++ from the membrane binding sites by chelation makes the membrane permeable to Ca++ leading to supersensitivity to 5-HT (observed only in the presence of EDTA). These results suggest that the failure of reserpine to induce supersensitivity to 5-HT in rat seminal vesicle may be due to an enhanced antagonism of Mg++ on Ca++ movements in this preparation due to the poor capacity of rat tissue to retain Ca++ (Krishnamurty and Grollman, 1976).
在有无乙二胺四乙酸(EDTA)的情况下,研究了孵育培养基中Mg++浓度变化对大鼠离体精囊对5-羟色胺(5-HT)收缩反应的影响。在无Mg++和Mg++过量的培养基中孵育的制剂分别对5-HT表现出超敏感性和低敏感性。在EDTA存在的情况下,改变Mg++浓度所产生的对5-HT敏感性的变化相对较小。从利血平化动物获得的制剂在正常和Mg++过量培养基中表现出低敏感性,在无Mg++培养基中表现出超敏感性。在EDTA存在的情况下,利血平化制剂在正常Mg++培养基中表现出轻微的超敏感性,在无Mg++培养基中表现出明显的超敏感性,在Mg++过量培养基中表现出较小的低敏感性。可能是EDTA通过螯合更有效地从膜结合位点去除Mg++,使膜对Ca++具有通透性,从而导致对5-HT的超敏感性(仅在EDTA存在时观察到)。这些结果表明,利血平未能在大鼠精囊中诱导对5-HT的超敏感性,可能是由于大鼠组织保留Ca++的能力较差,导致Mg++对该制剂中Ca++运动的拮抗作用增强(克里希纳穆尔蒂和格罗尔曼,1976年)。