Biomaterial Database

Modulation of nitric oxide effects by flurbiprofen enantiomers and nefopam and its relation to antinociception. 1994

D Pallapies, and B A Peskar, and K Brune, and H U Zeilhofer

Department of Pharmacology and Toxicology, Ruhr-Universität, Bochum, Germany.

We have examined the interactions of the analgesics, R- and S-flurbiprofen and nefopam, with nitric oxide (NO) in several experimental systems. Phenylephrine-precontracted rat aortic strips with intact endothelium were relaxed by R- and S-flurbiprofen and nefopam in a concentration-dependent manner. Removal of endothelium, inhibition of guanylate cyclase, inhibition of NO biosynthesis and inactivation of NO significantly reduced these relaxations. R- and S-flurbiprofen as well as nefopam enhanced the inhibition of platelet aggregation caused by rat peritoneal neutrophils or 3-morpholinosydnonimine. The antinociceptive effects of R- and S-flurbiprofen in the mouse writhing test as well as those of nefopam in the hot plate test were not significantly affected by administration of NO synthase inhibitors. We conclude that the increase in the biological activity of NO by R- and S-flurbiprofen and nefopam does not play a major role in the antinociceptive activity of the drugs, but might contribute to acute hypotension, a side-effect occasionally seen with flurbiprofen and nefopam.

UI	MeSH Term	Description	Entries
D008297	Male		Males
D009340	Nefopam	Non-narcotic analgesic chemically similar to ORPHENADRINE. Its mechanism of action is unclear. It is used for the relief of acute and chronic pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p26)	Acupan,Ajan,Fenazoxine,Nefopam Hydrochloride,Silentan Nefopam,Hydrochloride, Nefopam,Nefopam, Silentan
D009569	Nitric Oxide	A free radical gas produced endogenously by a variety of mammalian cells, synthesized from ARGININE by NITRIC OXIDE SYNTHASE. Nitric oxide is one of the ENDOTHELIUM-DEPENDENT RELAXING FACTORS released by the vascular endothelium and mediates VASODILATION. It also inhibits platelet aggregation, induces disaggregation of aggregated platelets, and inhibits platelet adhesion to the vascular endothelium. Nitric oxide activates cytosolic GUANYLATE CYCLASE and thus elevates intracellular levels of CYCLIC GMP.	Endogenous Nitrate Vasodilator,Mononitrogen Monoxide,Nitric Oxide, Endothelium-Derived,Nitrogen Monoxide,Endothelium-Derived Nitric Oxide,Monoxide, Mononitrogen,Monoxide, Nitrogen,Nitrate Vasodilator, Endogenous,Nitric Oxide, Endothelium Derived,Oxide, Nitric,Vasodilator, Endogenous Nitrate
D010974	Platelet Aggregation	The attachment of PLATELETS to one another. This clumping together can be induced by a number of agents (e.g., THROMBIN; COLLAGEN) and is part of the mechanism leading to the formation of a THROMBUS.	Aggregation, Platelet
D005480	Flurbiprofen	An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.	2-Fluoro-alpha-methyl-(1,1'-biphenyl)-4-acetic Acid,Ansaid,Apo-Flurbiprofen,BTS-18322,Cebutid,Dobrofen,E-7869,Flubiprofen,Flugalin,Flurbiprofen Sodium,Fluriproben,Froben,Froben SR,Neo Artrol,Novo-Flurprofen,Nu-Flurbiprofen,Ocufen,Ocuflur,Strefen,ratio-Flurbiprofen,Apo Flurbiprofen,BTS 18322,BTS18322,E 7869,E7869,Novo Flurprofen,Nu Flurbiprofen,ratio Flurbiprofen
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000700	Analgesics	Compounds capable of relieving pain without the loss of CONSCIOUSNESS.	Analgesic,Anodynes,Antinociceptive Agents,Analgesic Agents,Analgesic Drugs,Agents, Analgesic,Agents, Antinociceptive,Drugs, Analgesic
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D001120	Arginine	An essential amino acid that is physiologically active in the L-form.	Arginine Hydrochloride,Arginine, L-Isomer,DL-Arginine Acetate, Monohydrate,L-Arginine,Arginine, L Isomer,DL Arginine Acetate, Monohydrate,Hydrochloride, Arginine,L Arginine,L-Isomer Arginine,Monohydrate DL-Arginine Acetate
D013237	Stereoisomerism	The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)	Molecular Stereochemistry,Stereoisomers,Stereochemistry, Molecular,Stereoisomer