THE POTENT 5-HT(3) RECEPTOR ANTAGONIST (R)-ZACOPRIDE LABELS AN ADDITIONAL HIGH-AFFINITY SITE IN THE CENTRAL-NERVOUS-SYSTEM

被引：25

作者：

KIDD, E ^{[1
]}

DEVENDEGIES, IB ^{[1
]}

LEVY, JC ^{[1
]}

HAMON, M ^{[1
]}

GOZLAN, H ^{[1
]}

机构：

[1] CTR RECH DELANDE,F-92500 RUEIL MALMAISON,FRANCE

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1992年 / 211卷 / 01期

关键词：

H-3](R)-ZACOPRIDE; H-3](S)-ZACOPRIDE; 5-HT3; RECEPTORS; BRAIN (RAT); (HIGH AFFINITY (R)-SITES);

D O I：

10.1016/0014-2999(92)90276-A

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The binding characteristics of [H-3](R)- and [H-3](S)-zacopride were investigated in membranes from the rat entorhinal cortex and NG 108-15 clonal cells. In contrast to [H-3](S)-zacoprid which bound solely to 5-HT3 receptors, [H-3](R)-zacopride recognized another class of binding sites, called the (R)-sites, in both membrane preparations. In addition to (R)-zacopride (K(i) = 3-11 nM), only (R)-iodo-zacopride, (R)-dechloro-zacopride, prazosin and mianserin exhibited high to moderate affinity for the (R)-sites, whose possible functions remain to be established.

引用

页码：133 / 136

页数：4

共 10 条

[1] THE DIFFERENTIAL ACTIVITIES OF R(+)-ZACOPRIDE AND S(-)-ZACOPRIDE AS 5-HT3 RECEPTOR ANTAGONISTS [J].