NG108-15细胞中δ-阿片样物质的测定。

Determination of delta-opioid in NG108-15 cells.

作者信息

Ho B Y, Holmes B B, Zhao J, Fujimoto J

机构信息

Department of Pharmacology, Medical College of Wisconsin, Milwaukee 53226, USA.

出版信息

Eur J Pharmacol. 1997 Jan 14;319(1):109-14. doi: 10.1016/s0014-2999(96)00827-8.

DOI:10.1016/s0014-2999(96)00827-8

PMID:9030905

Abstract

The delta-opioid receptors in mouse neuroblastoma x rat glioma NG108-15 cells were characterized by receptor binding and cAMP assays. Saturation binding assays using [3H][D-Pen5]enkephalin (DPDPE) or [3H][D-Ser2, Leu5, Thr6]enkephalin (DSLET) gave similar binding capacities (Bmax). Competition binding assays showed that DPDPE and DSLET have similar affinity for the [3H]DPDPE or 3[H]DSLET binding sites. The rank order of potency of competition with [3H]DPDPE and [3H]DSLET was similar: naltriben approximately DSLET > or = DPDPE > 7-benzylidenenaltrexone (BNTX). Both DPDPE and DSLET were found to decrease cAMP formation. The action of DSLET was antagonized by naltriben but not BNTX, while the action of DPDPE was reversed by both antagonists. Therefore, the delta-opioid receptor in NG108-15 cells has similar affinity for the agonists DPDPE and DSLET, and a higher affinity for the antagonist naltriben than BNTX.

摘要

通过受体结合和环磷酸腺苷（cAMP）检测对小鼠神经母细胞瘤x大鼠胶质瘤NG108 - 15细胞中的δ阿片受体进行了表征。使用[3H][D - Pen5]脑啡肽（DPDPE）或[3H][D - Ser2，Leu5，Thr6]脑啡肽（DSLET）进行的饱和结合检测给出了相似的结合容量（Bmax）。竞争结合检测表明，DPDPE和DSLET对[3H]DPDPE或[3H]DSLET结合位点具有相似的亲和力。与[3H]DPDPE和[3H]DSLET竞争的效力排序相似：纳曲苄≈DSLET≥DPDPE＞7 - 亚苄基纳曲酮（BNTX）。发现DPDPE和DSLET均可降低cAMP的生成。DSLET的作用被纳曲苄拮抗，但不被BNTX拮抗，而DPDPE的作用被两种拮抗剂逆转。因此，NG108 - 15细胞中的δ阿片受体对激动剂DPDPE和DSLET具有相似的亲和力，且对拮抗剂纳曲苄的亲和力高于BNTX。