Gibson A
J Pharm Pharmacol. 1985 Dec;37(12):890-3. doi: 10.1111/j.2042-7158.1985.tb04995.x.
The sensitivity of the mouse anococcygeus to contraction by oxytocin was shown to be Mg2+-dependent. Decreasing [Mg2+]0 from the optimal concentration of 1 to 0 mM caused a 20-fold parallel rightward displacement of the oxytocin dose-response curve. Contractions to oxytocin-related peptides (Arg-vasotocin, Arg-vasopressin and Lys-vasopressin) were also Mg2+-dependent, but those to other drugs (carbachol, methoxamine and thyrotrophin releasing hormone) were not. The onset of the potentiating effect of Mg2+ was rapid, full potentiation occurring within 70 s. 1-Deaminopenicillamine 8-ornithine-vasotocin produced competitive antagonism of responses to oxytocin, but was more potent in the absence (pA2 = 8.01) than in the presence of Mg2+ (1 mM; pA2 = 7.52). Thus, physiological concentrations of [Mg2+]0 enhanced oxytocin agonist potency but decreased oxytocin antagonist potency; possible mechanisms are discussed.
已证明小鼠肛门尾骨肌对催产素收缩的敏感性依赖于Mg2+。将[Mg2+]0从最佳浓度1 mM降至0 mM会导致催产素剂量反应曲线平行向右位移20倍。对催产素相关肽(精氨酸加压催产素、精氨酸加压素和赖氨酸加压素)的收缩也依赖于Mg2+,但对其他药物(卡巴胆碱、甲氧明和促甲状腺激素释放激素)的收缩则不依赖于Mg2+。Mg2+增强作用的起效迅速,在70秒内即可实现完全增强。1-脱氨青霉胺8-鸟氨酸加压催产素对催产素反应产生竞争性拮抗作用,但在无Mg2+(pA2 = 8.01)时比在有Mg2+(1 mM;pA2 = 7.52)时更有效。因此,生理浓度的[Mg2+]0增强了催产素激动剂的效力,但降低了催产素拮抗剂的效力;文中讨论了可能的机制。