L-NG-NITRO ARGININE P-NITROANILIDE (L-NAPNA) IS ANTINOCICEPTIVE IN THE MOUSE

被引:25
作者
BABBEDGE, RC [1 ]
WALLACE, P [1 ]
GAFFEN, ZA [1 ]
HART, SL [1 ]
MOORE, PK [1 ]
机构
[1] UNIV LONDON,KINGS COLL,DIV BIOMED SCI,PHARMACOL GRP,MANRESA RD,LONDON SW3 6LX,ENGLAND
关键词
ANTI-NOCICEPTION; NITRIC OXIDE; NITRIC OXIDE SYNTHASE; L-NAME; L-NG-NITRO ARGININE P-NITROANILIDE; L-NAPNA; BLOOD PRESSURE; MOUSE;
D O I
10.1097/00001756-199303000-00020
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
L-N(G)-NITRo arginine p-nitroanilide (L-NAPNA), L-N(G) nitro arginine methyl ester (L-NAME) and L-N(G)-monomethyl arginine (L-NMMA) inhibit rat cerebellar nitric oxide synthase (NOS) with IC50s of 1.4 +/- 0.1 muM, 0.81 +/-0.16 muM and 5.1 +/- 0.07 muM respectively. L-NAPNA inhibits the late phase of formalin-induced hindpaw licking (ED50, 57.2 mg kg-1) and acetic acid induced abdominal constrictions (ED50 25 mg kg-1) in the mouse. L-NAPNA is approximately 65 times less active than L-NAME as an inhibitor of endothelium-dependent relaxation in the rabbit aorta and about 10 fold less potent as a vasopressor in the anaesthetized mouse. LNAPNA shows some degree of selectivity for the central NOS isoform and may be of clinical interest for the treatment of pain.
引用
收藏
页码:307 / 310
页数:4
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