二乙烯三胺对NMDA诱导的大鼠血压升高的影响。

Effects of diethylenetriamine on NMDA-induced increase of blood pressure in rats.

作者信息

Maione S, Pallotta M, Leyva J, Palazzo E, Rossi F

机构信息

Institute of Pharmacology and Toxicology, Faculty of Medicine and Surgery, 2nd University of Naples, Italy.

出版信息

Pharmacol Biochem Behav. 1998 Jan;59(1):233-7. doi: 10.1016/s0091-3057(97)00337-7.

DOI:10.1016/s0091-3057(97)00337-7

PMID:9443560

Abstract

We investigated the effects of three doses of diethylenetriamine (DET; 0.1-1-10 nmol/rat), putative ligand at the polyamine site on NMDA receptors, on blood pressure increase induced by N-methyl-D-aspartate (NMDA, 2 nmol/rat) microinjected at the periaqueductal gray (PAG) matter. Said doses of DET did not modify basal arterial blood pressure. Pretreatment with DET, depending on the dose used, either potentiated (DET, 0.1 nmol/rat), reduced (DET, 1 nmol/rat) the NMDA effects or left them unchanged (DET, 10 nmol/rat). DET 10 nmol/rat, microinjected 5 min before spermidine (SPD, 0.02-2 nmol/rat), significantly antagonized SPD modulation on the NMDA-induced pressor changes. These data, in agreement with the functional findings in vitro, suggest that also in vivo DET has pharmacological activities quite different from a pure antagonist but shows multiple actions on the NMDA receptors.

摘要

我们研究了三种剂量的二亚乙基三胺（DET；0.1 - 1 - 10 nmol/大鼠）对经脑导水管周围灰质（PAG）微量注射N - 甲基 - D - 天冬氨酸（NMDA，2 nmol/大鼠）所致血压升高的影响，DET是一种假定的多胺位点NMDA受体配体。所述剂量的DET并未改变基础动脉血压。根据所用剂量不同，DET预处理对NMDA效应的影响也不同，0.1 nmol/大鼠的DET增强了NMDA效应，1 nmol/大鼠的DET降低了NMDA效应，而10 nmol/大鼠的DET则使NMDA效应保持不变。在注射亚精胺（SPD，0.02 - 2 nmol/大鼠）前5分钟微量注射10 nmol/大鼠的DET，可显著拮抗SPD对NMDA诱导的升压变化的调节作用。这些数据与体外功能研究结果一致，表明在体内DET也具有与纯拮抗剂截然不同的药理活性，且对NMDA受体具有多种作用。