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Etoricoxib (MK-0663): preclinical profile and comparison with other agents that selectively inhibit cyclooxygenase-2.
TLDR
Etoricoxib represents a novel agent that selectively inhibits COX-2 with 106-fold selectivity in human whole blood assays in vitro and with the lowest potency of inhibition ofCOX-1 compared with other reported selective agents. Expand
Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX‐2 inhibitor
TLDR
The time‐dependent inhibition by DFU was decreased by co‐incubation with arachidonic acid under non‐turnover conditions, consistent with reversible competitive inhibition at the COX active site. Expand
Cloning, Expression, and Up-regulation of Inducible Rat Prostaglandin E Synthase during Lipopolysaccharide-induced Pyresis and Adjuvant-induced Arthritis*
TLDR
The results demonstrate that PGE synthase is up-regulated in vivo after LPS or adjuvant administration and suggest that this is a key enzyme involved in the formation of PGE2in COX-2-mediated inflammatory and pyretic responses. Expand
Arachidonyl trifluoromethyl ketone, a potent inhibitor of 85-kDa phospholipase A2, blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets.
TLDR
The results suggest that the cPLA2 plays an important role in the generation of free AA for 12-HETE biosynthesis in platelets and affects the cyclooxygenase pathway in addition to AA release. Expand
Characterization of rofecoxib as a cyclooxygenase‐2 isoform inhibitor and demonstration of analgesia in the dental pain model
TLDR
Nonsteroidal anti‐inflammatory drugs such as aspirin, ibuprofen, and indomethacin (INN, indometacin) inhibit both the constitutive and inducible isoforms of cyclooxygenase, leading to the hypothesis that COX‐2 inhibition primarily accounts for the therapeutic properties of NSAIDs. Expand
Comparison of the cyclooxygenase-1 inhibitory properties of nonsteroidal anti-inflammatory drugs (NSAIDs) and selective COX-2 inhibitors, using sensitive microsomal and platelet assays.
TLDR
The microsomal assay was more sensitive to inhibition than cell-based assays and allowed the detection of inhibitory effects on COX-1 for all NSAIDs and selective COx-2 inhibitors examined with discrimination of their potency under conditions of limited availability of arachidonic acid. Expand
Deletion of Microsomal Prostaglandin E2 (PGE2) Synthase-1 Reduces Inducible and Basal PGE2 Production and Alters the Gastric Prostanoid Profile*
TLDR
A dual role for mPGES-1 in both inflammatory and COX-1-mediated PGE2 production is demonstrated for the first time and an interdependence of prostanoid production with tissue-specific alterations of prostaglandin levels in the absence of mPGes-1 is suggested. Expand
Mechanism of selective inhibition of human prostaglandin G/H synthase-1 and -2 in intact cells.
TLDR
Cell-based screening ofPGHS inhibitors demonstrated that the selectivities and potencies of PGHS inhibitors determined using intact cells are affected by substrate concentration and differ from that determined in cell-free microsomal or purified enzyme preparations of PG HS isozymes. Expand
Carrageenan-induced Paw Edema in Rat Elicits a Predominant Prostaglandin E2 (PGE2) Response in the Central Nervous System Associated with the Induction of Microsomal PGE2 Synthase-1*
TLDR
The results show that the carrageenan-induced edema in the paw elicits an early phase of COX-2 induction in the CNS leading to an increase synthesis in PGD2, 6-keto-PGF1α, and TXB2 in addition to the major PGE2 response. Expand
MF63 [2-(6-Chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-isophthalonitrile], a Selective Microsomal Prostaglandin E Synthase-1 Inhibitor, Relieves Pyresis and Pain in Preclinical Models of Inflammation
TLDR
It is demonstrated that mPGES-1 inhibition leads to effective relief of both pyresis and inflammatory pain in preclinical models of inflammation and may be a useful approach for treating inflammatory diseases. Expand
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