L-NG-nitro arginine p-nitroanilide (L-NAPNA) is anti-nociceptive in the mouse.
L-NG-nitro arginine p-nitroanilide (L-NAPNA), L-NG nitro arginine methyl ester (L-NAME) and L-NG-monomethyl arginine (L-NMMA) inhibit rat cerebellar nitric oxide synthase (NOS) with IC50s of 1.4 +/- 0.1 microM, 0.81 +/- 0.16 microM and 5.1 +/- 0.07 microM 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.
Babbedge
R C
RC
Biomedical Sciences Division, King's College, University of London, UK.
Wallace
P
P
Gaffen
Z A
ZA
Hart
S L
SL
Moore
P K
PK
D000594:Amino Acid Oxidoreductases / Q000037:antagonists & inhibitors; D000700:Analgesics / Q000494:pharmacology*; D000813:Anilides; D000818:Animals; D001013:Aorta, Thoracic / Q000187:drug effects; D001120:Arginine / Q000031:analogs & derivatives* / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects; D001921:Brain / Q000187:drug effects / Q000201:enzymology; D005557:Formaldehyde; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D019331:NG-Nitroarginine Methyl Ester; D019001:Nitric Oxide Synthase; D010146:Pain / Q000139:chemically induced / Q000517:prevention & control; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D019323:omega-N-Methylarginine
D000700:Analgesics; D000813:Anilides; D005557:Formaldehyde; D019323:omega-N-Methylarginine; C080840:N(G)-nitroarginine-4-nitroanilide; D001120:Arginine; D019001:Nitric Oxide Synthase; D000594:Amino Acid Oxidoreductases; D019331:NG-Nitroarginine Methyl Ester