FURTHER CHARACTERIZATION OF [H-3] IFENPRODIL BINDING TO SIGMA-RECEPTORS IN RAT-BRAIN

被引：82

作者：

HASHIMOTO, K

LONDON, ED

机构：

[1] JOHNS HOPKINS MED INST,DEPT RADIOL,BALTIMORE,MD 21205

[2] UNIV MARYLAND,SCH MED,DEPT PHARMACOL & EXPTL THERAPEUT,BALTIMORE,MD 21201

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1993年 / 236卷 / 01期

关键词：

IFENPRODIL; SIGMA RECEPTORS; BRAIN (RAT); (SUBTYPES);

D O I：

10.1016/0014-2999(93)90241-9

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

This study was undertaken to examine further the pharmacology of [H-3]ifenprodil binding in rat brain at 37-degrees-C. [H-3]Ifenprodil bound specifically to membranes (K(d) = 5.09 +/- 0.30 nM; B(max) = 2.36 +/- 0.19 pmol/mg protein). [H-3]Ifenprodil binding was potently inhibited by sigma ligands and inhibitors of cytochrome P-450. The levorotatory enantiomers of pentazocine and SKF 10,047 were more potent inhibitors than corresponding dextrorotatory enantiomers. Furthermore, the pharmacological profile of [H-3]ifenprodil binding was highly correlated with that of sigma2 sites, not sigma1 sites. The results suggest that [H-3]ifenprodil labels sigma2 sites in rat brain at 37-degrees-C, and that [H-3]ifenprodil would be useful for studying sigma receptor subtypes

引用

页码：159 / 163

页数：5

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