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Preclinical pharmacology of lumiracoxib: a novel selective inhibitor of cyclooxygenase‐2
1 This manuscript presents the preclinical profile of lumiracoxib, a novel cyclooxygenase‐2 (COX‐2) selective inhibitor. 2 Lumiracoxib inhibited purified COX‐1 and COX‐2 with Ki values of 3 and 0.06Expand
Preclinical pharmacology of robenacoxib: a novel selective inhibitor of cyclooxygenase-2.
This manuscript reports the results of preclinical studies in the rat with robenacoxib, a novel selective cyclooxygenase (COX)-2 inhibitor. Robenacoxib selectively inhibited COX-2 in vitro asExpand
Selective functional inhibition of JAK-3 is sufficient for efficacy in collagen-induced arthritis in mice.
OBJECTIVE All gamma-chain cytokines signal through JAK-3 and JAK-1 acting in tandem. We undertook this study to determine whether the JAK-3 selective inhibitor WYE-151650 would be sufficient toExpand
Novel C5a receptor antagonists regulate neutrophil functions in vitro and in vivo.
Novel recombinant human C5a receptor antagonists were discovered through modification of the C terminus of C5a. The C5a1-71T1M,C27S,Q71C monomer, (C5aRAM; CGS 27913), was a pure and potent functionalExpand
Effects of diclofenac sodium on arachidonic acid metabolism.
Characterization of CGS 8515 as a selective 5-lipoxygenase inhibitor using in vitro and in vivo models.
CGS 8515 inhibited 5-hydroxyeicosatetraenoic acid (5-HETE) and leukotriene B4 synthesis in guinea pig leukocytes (IC50 = 0.1 microM). The compound did not appreciably affect cyclooxygenase (sheepExpand
The effects of diclofenac sodium on arachidonic acid metabolism.
Evidence has been presented that inhibition by diclofenac sodium of the production of leukotrienes by cells participating in the inflammatory process is due to a decreased availability ofExpand
CGS 15435A, a thromboxane synthetase inhibitor with an extended duration of action: a comparison with dazoxiben.
CGS 15435A, a novel thromboxane (Tx) synthetase inhibitor (5-chloro-1-methyl-2-(3-pyridyl)-3-indolhexanoic acid HCl), had a selectivity for Tx synthetase 100,000-fold greater than that forExpand
Characterization of CGS 8515 as a selective 5-lipoxygenase (5-LO) inhibitor.
1. CGS 8515 selectively inhibited 5-LO (IC50 = 0.1 microM) with negligible effect on CO, 12-LO, 15-LO and TxS at concentrations up to 100 microM. 2. CGS 8515 selectively inhibited A23187-inducedExpand
Novel pyrrolidine ureas as C-C chemokine receptor 1 (CCR1) antagonists.
Monocyte infiltration is implicated in a variety of diseases including multiple myeloma, rheumatoid arthritis, and multiple sclerosis. C-C chemokine receptor 1 (CCR1) is a chemokine receptor thatExpand