title: Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx).
abstract: Metabolites of the COX-2 inhibitor rofecoxib (MK-0966, Vioxx) were prepared by synthetic or biosynthetic methods. Metabolites include products of oxidation, glucuronidation, reduction and hydrolytic ring opening. Based on an in vitro whole blood assay, none of the known human metabolites of rofecoxib inhibits COX-1 nor contributes significantly to the inhibition of COX-2.
authors: Merck Frosst Centre for Therapeutic Research, Pointe-Claire-Dorval, Québec, Canada. deborah_nicoll_griffith@merck.com
authors: D A
authors: DA
authors: Nicoll-Griffith
authors: J A
authors: JA
authors: Yergey
authors: L A
authors: LA
authors: Trimble
authors: J M
authors: JM
authors: Silva
authors: C
authors: C
authors: Li
authors: N
authors: N
authors: Chauret
authors: J Y
authors: JY
authors: Gauthier
authors: E
authors: E
authors: Grimm
authors: S
authors: S
authors: Léger
authors: P
authors: P
authors: Roy
authors: M
authors: M
authors: Thérien
authors: Z
authors: Z
authors: Wang
authors: P
authors: P
authors: Prasit
authors: R
authors: R
authors: Zamboni
authors: R N
authors: RN
authors: Young
authors: C
authors: C
authors: Brideau
authors: C C
authors: CC
authors: Chan
authors: J
authors: J
authors: Mancini
authors: D
authors: D
authors: Riendeau
mesh_terms: D000818:Animals; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007527:Isoenzymes / Q000097:blood; D007783:Lactones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008565:Membrane Proteins; D011451:Prostaglandin-Endoperoxide Synthases / Q000097:blood; D051381:Rats; D013450:Sulfones
chemical_list: D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D007783:Lactones; D008565:Membrane Proteins; D013450:Sulfones; C116926:rofecoxib; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; C496511:PTGS1 protein, human; C496540:PTGS2 protein, human; D011451:Prostaglandin-Endoperoxide Synthases; C496513:Ptgs1 protein, rat