Effects of the novel anti-inflammatory compounds, N-[2-(cyclohexyloxy)-4-nitrophenyl] methanesulphonamide (NS-398) and 5-methanesulphonamido-6-(2,4-difluorothio-phenyl)-1-inda none (L-745,337), on the cyclo-oxygenase activity of human blood prostaglandin endoperoxide synthases

British Journal of Pharmacology
M R PanaraC Patrono

Abstract

1. We have evaluated the selectivity of ketoprofen and two novel nonsteroidal anti-inflammatory drugs, N-[2-(cyclohexyloxy)-4-nitrophenyl]methanesulphonamide (NS-398) and 5-methanesulphonamido-6-(2,4-difluorothiophenyl)-1-indano ne (L-745,337), in inhibiting the cyclo-oxygenase activity of prostaglandin endoperoxide synthase-2 (PGHS-2) vs PGHS-1 in human blood monocytes and platelets, respectively. 2. Heparinized whole blood samples were drawn from healthy volunteers pretreated with aspirin, 300 mg 48 h before sampling, to suppress the activity of platelet PGHS-1 and incubated at 37 degrees C for 24 h with increasing concentrations of the test compounds in the presence of lipopolysaccharide (LPS, 10 micrograms ml-1). Immunoreactive PGE2 levels were measured in plasma by a specific radioimmunoassay as an index of the cyclo-oxygenase activity of LPS-induced monocyte PGHS-2. 3. The effects of the same inhibitors on platelet PGHS-1 activity were assessed by allowing whole blood samples, drawn from the same subjects in aspirin-free periods, to clot at 37 degrees C for 1 h in the presence of the compounds and measuring immunoreactive thromboxane B2 (TXB2) levels in serum by a specific radioimmunoassay. 4. Under these experimental con...Continue Reading

References

Sep 1, 1979·Proceedings of the National Academy of Sciences of the United States of America·H TowbinJ Gordon
Apr 1, 1979·Journal of Endocrinological Investigation·G CiabattoniC Patrono
Aug 1, 1975·Proceedings of the National Academy of Sciences of the United States of America·G J RothP W Majerus
Aug 15, 1992·Proceedings of the National Academy of Sciences of the United States of America·T Hla, K Neilson
Sep 26, 1992·Biochemical and Biophysical Research Communications·M G O'SullivanC E McCall
Jun 1, 1992·Proceedings of the National Academy of Sciences of the United States of America·M K O'BanionD A Young
May 8, 1991·Biochimica Et Biophysica Acta·D L DeWitt
Sep 1, 1991·Prostaglandins, Leukotrienes, and Essential Fatty Acids·L A Salamonsen
Mar 1, 1988·Proceedings of the National Academy of Sciences of the United States of America·D L DeWitt, W L Smith
Dec 1, 1985·Circulation·C PatronoL Forni
Jun 1, 1982·The Journal of Clinical Investigation·P PatrignaniC Patrono
Nov 8, 1994·Proceedings of the National Academy of Sciences of the United States of America·R A CopelandJ M Trzaskos
Jan 20, 1994·Nature·J Vane
Apr 12, 1994·Proceedings of the National Academy of Sciences of the United States of America·J L MasferrerK Seibert
Dec 15, 1993·Proceedings of the National Academy of Sciences of the United States of America·J A MitchellJ R Vane

❮ Previous
Next ❯

Citations

Jun 1, 1996·Journal of Clinical Pharmacology·A CarabazaD Mauleón
Jun 1, 1996·Journal of Clinical Pharmacology·G Geisslinger, H G Schaible
Oct 25, 2002·Journal of Cellular Biochemistry·Taketoshi KushidaNader G Abraham
Feb 13, 1999·European Journal of Pharmacology·P MontuschiG Ciabattoni
Apr 20, 2001·European Journal of Medicinal Chemistry·G Dannhardt, W Kiefer
Jan 6, 1999·Proceedings of the National Academy of Sciences of the United States of America·B F McAdamG A FitzGerald
Apr 27, 2001·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·C García-CabanesA Orts
May 20, 1999·The Journal of Clinical Investigation·B RoccaG A FitzGerald
Mar 1, 1997·Expert Opinion on Investigational Drugs·M Schattenkirchner
Jul 23, 2014·Knee Surgery, Sports Traumatology, Arthroscopy : Official Journal of the ESSKA·Sevtap Hekimoglu SahinNecdet Sut
Feb 13, 2014·Journal of Enzyme Inhibition and Medicinal Chemistry·J Alberto Guevara-SalazarJosé Trujillo-Ferrara
Jul 30, 2009·British Journal of Cancer·G A DohertyD J Fitzgerald
Dec 31, 1997·Arteriosclerosis, Thrombosis, and Vascular Biology·C Patrono, G A FitzGerald
Jul 15, 1998·Clinical Pharmacology and Therapeutics·M R PanaraP Patrignani
Jan 24, 2002·The Journal of Pharmacology and Experimental Therapeutics·Elizabeth ConnollyOrina Belton
Feb 1, 1997·Alimentary Pharmacology & Therapeutics·N M DaviesJ L Wallace
Jul 4, 2015·British Journal of Pharmacology·Luigia Di FrancescoPaola Patrignani
Nov 28, 1996·European Journal of Pharmacology·G SantiniP Patrignani

❮ Previous
Next ❯

Related Concepts

Related Feeds

Blood Clotting Disorders

Thrombophilia includes conditions with increased tendency for excessive blood clotting. Blood clotting occurs when the body has insufficient amounts of specialized proteins that make blood clot and stop bleeding. Here is the latest research on blood clotting disorders.