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
相关论文
共 22 条
[11]   NITRIC-OXIDE SYNTHASE - IRREVERSIBLE INHIBITION BY L-NG-NITROARGININE IN BRAIN INVITRO AND INVIVO [J].
DWYER, MA ;
BREDT, DS ;
SNYDER, SH .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1991, 176 (03) :1136-1141
[12]  
Garthwaite J, 1988, NATURE, V336, P383
[13]  
HALEY JE, 1992, NEUROPHARMACOLOGY, V31, P209
[14]   AN INHIBITOR OF NITRIC-OXIDE SYNTHESIS PREVENTS MEMORY FORMATION IN THE CHICK [J].
HOLSCHER, C ;
ROSE, SPR .
NEUROSCIENCE LETTERS, 1992, 145 (02) :165-167
[15]   THE FORMALIN TEST IN MICE - DISSOCIATION BETWEEN INFLAMMATORY AND NONINFLAMMATORY PAIN [J].
HUNSKAAR, S ;
HOLE, K .
PAIN, 1987, 30 (01) :103-114
[16]   ENDOTHELIAL NITRIC-OXIDE SYNTHASE - MOLECULAR-CLONING AND CHARACTERIZATION OF A DISTINCT CONSTITUTIVE ENZYME ISOFORM [J].
LAMAS, S ;
MARSDEN, PA ;
LI, GK ;
TEMPST, P ;
MICHEL, T .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1992, 89 (14) :6348-6352
[17]   PRODUCTION OF ENDOGENOUS NITRIC-OXIDE AND ACTIVATION OF SOLUBLE GUANYLATE-CYCLASE ARE REQUIRED FOR N-METHYL-D-ASPARTATE-PRODUCED FACILITATION OF THE NOCICEPTIVE TAIL-FLICK REFLEX [J].
MELLER, ST ;
DYKSTRA, C ;
GEBHART, GF .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1992, 214 (01) :93-96
[18]   L-NG-NITRO ARGININE METHYL-ESTER EXHIBITS ANTINOCICEPTIVE ACTIVITY IN THE MOUSE [J].
MOORE, PK ;
OLUYOMI, AO ;
BABBEDGE, RC ;
WALLACE, P ;
HART, SL .
BRITISH JOURNAL OF PHARMACOLOGY, 1991, 102 (01) :198-202
[19]   NITRIC-OXIDE MEDIATES NEURONAL DEATH AFTER FOCAL CEREBRAL-ISCHEMIA IN THE MOUSE [J].
NOWICKI, JP ;
DUVAL, D ;
POIGNET, H ;
SCATTON, B .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1991, 204 (03) :339-340
[20]   ROLE OF ENDOTHELIUM-DERIVED NITRIC-OXIDE IN THE REGULATION OF BLOOD-PRESSURE [J].
REES, DD ;
PALMER, RMJ ;
MONCADA, S .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1989, 86 (09) :3375-3378