HUMAN BRAIN SODIUM-CHANNELS AS ONE OF THE MOLECULAR TARGET SITES FOR THE NEW INTRAVENOUS ANESTHETIC PROPOFOL (2,6-DIISOPROPYLPHENOL)

被引：53

作者：

FRENKEL, C

URBAN, BW

机构：

[1] CORNELL UNIV, MED CTR, COLL MED, DEPT ANESTHESIOL, NEW YORK, NY 10021 USA

[2] CORNELL UNIV, MED CTR, COLL MED, DEPT PHYSIOL, NEW YORK, NY 10021 USA

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION | 1991年 / 208卷 / 01期

关键词：

PROPOFOL; NA+ CHANNEL; BRAIN (HUMAN); LIPID BILAYER; VOLTAGE CLAMP; (MECHANISM OF ACTION);

D O I：

10.1016/0922-4106(91)90054-L

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Single sodium channels from human brain cortex tissue were incorporated into voltage-clamped planar lipid bilayers in the presence of batrachotoxin and studied with various doses of the new anaesthetic compound propofol (2,6-diisopropylphenol). Propofol was found to depress two major sodium channel functions, leading to a reduction of the time-averaged fractional channel open-time (half-maximal blocking concentration, ED50, 20-mu-M; maximal block 28%) and an interaction with the steady-state activation. These effects occurred at clinically relevant serum concentrations, suggesting the human brain sodium channel as one of the molecular target sites of action for propofol.

引用

页码：75 / 79

页数：5