Twery M J, Joëls M, Gallagher J P, Orlowski R C, Moss R L
Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston 77550.
Neurosci Lett. 1988 Mar 21;86(1):82-8. doi: 10.1016/0304-3940(88)90187-5.
The effects of [Gly8-des-Leu16-D-Arg24]-salmon calcitonin (CTA) on spontaneous extracellular activity and the passive membrane properties of rat forebrain neurons were studied in vivo and in vitro. This analogue had negligible ability to lower serum calcium relative to salmon calcitonin (SCT), however, the pattern of neuronal membrane sensitivity to CTA was similar to that produced by SCT and calcitonin generelated peptide. Depression of extracellularly recorded spontaneous action potential firing rate was the predominant response of neurons to microiontophoretic application of each peptide in vivo. Intracellular recordings from septal neurons suggest that the extracellularly observed inhibitory effects may be due to changes in membrane potential. We conclude that different structure-activity relationships may apply to the pharmacological effects of calcitonin in brain and its serum calcium-lowering action.
研究了[Gly8 - des - Leu16 - D - Arg24] - 鲑鱼降钙素（CTA）对大鼠前脑神经元自发细胞外活动及被动膜特性的体内和体外效应。与鲑鱼降钙素（SCT）相比，该类似物降低血清钙的能力可忽略不计，然而，神经元膜对CTA的敏感性模式与SCT和降钙素基因相关肽产生的模式相似。在体内，细胞外记录的自发动作电位发放率降低是神经元对每种肽微量离子导入应用的主要反应。来自隔区神经元的细胞内记录表明，细胞外观察到的抑制作用可能是由于膜电位的变化。我们得出结论，不同的构效关系可能适用于降钙素在脑内的药理作用及其降低血清钙的作用。
