title: A new metabolite of diclofenac sodium in human plasma.
abstract: 1. Among the phenolic metabolites of diclofenac in human plasma, an unknown compound (metabolite VI) was detected by h.p.l.c. and g.c. methods. This was also found in baboon plasma. 2. Metabolite VI was identified as 3'-hydroxy-4'-methoxy diclofenac by mass and n.m.r. spectroscopic analysis. Comparison with synthetic reference compound confirmed its structure. 3. In plasma, metabolite VI persists much longer than do unchanged diclofenac and the other phenolic metabolites. In urine, metabolite VI and its conjugates are excreted in trace amounts only. 4. A synthetic sample of metabolite VI was shown to be virtually inactive in animal models of inflammation and pain.
authors.affiliation: Research and Development Department, Ciba-Geigy Ltd., Basle, Switzerland.
authors.forename: J W
authors.initials: JW
authors.lastname: Faigle
authors.forename: I
authors.initials: I
authors.lastname: Böttcher
authors.forename: J
authors.initials: J
authors.lastname: Godbillon
authors.forename: H P
authors.initials: HP
authors.lastname: Kriemler
authors.forename: E
authors.initials: E
authors.lastname: Schlumpf
authors.forename: W
authors.initials: W
authors.lastname: Schneider
authors.forename: A
authors.initials: A
authors.lastname: Schweizer
authors.forename: H
authors.initials: H
authors.lastname: Stierlin
authors.forename: T
authors.initials: T
authors.lastname: Winkler
mesh_terms: D000328:Adult; D000818:Animals; D001711:Biotransformation; D002417:Cattle; D055598:Chemical Phenomena; D002621:Chemistry; D004008:Diclofenac / Q000031:analogs & derivatives* / Q000493:pharmacokinetics* / Q000494:pharmacology; D008401:Gas Chromatography-Mass Spectrometry; D006801:Humans; D007249:Inflammation / Q000188:drug therapy; D008297:Male; D010146:Pain / Q000188:drug therapy; D010215:Papio; D011453:Prostaglandins / Q000096:biosynthesis; D051381:Rats; D011917:Rats, Inbred Lew
chemical_list: D011453:Prostaglandins; C058953:3'-hydroxy-4'-methoxydiclofenac; D004008:Diclofenac