CHARACTERIZATION OF THE BINDING OF [H-3] L-N(G)-NITRO-ARGININE IN RAT-BRAIN

被引:34
作者
MICHEL, AD
PHUL, RK
STEWART, TL
HUMPHREY, PPA
机构
[1] Glaxo Institute of Applied Pharmacology, Department of Pharmacology, University of Cambridge, Cambridge, CB2 1QJ, Tennis Court Road
关键词
NITRIC OXIDE SYNTHASE; H-3]-L-N(G)-NITRO-ARGININE; RADIOLIGAND BINDING; NITRIC OXIDE SYNTHASE INHIBITORS;
D O I
10.1111/j.1476-5381.1993.tb13566.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In the present study tritiated L-N(G)-nitro-arginine (L-NOARG) has been shown to label specific binding sites in rat brain cytosol. We conclude that this ligand is directly labelling nitric oxide synthase (NOS). This conclusion is based on our observations (i) that binding was stereoselectively inhibited by L-arginine, in preference to D-arginine, and (ii) that a number of different NOS inhibitors were able to displace [H-3]-L-NOARG binding at similar concentrations to those required to inhibit the activity of rat brain cytosol NOS in functional studies.
引用
收藏
页码:287 / 288
页数:2
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