title: In vitro and in vivo evaluation of O-alkyl derivatives of tramadol.
abstract: Tramadol is a centrally acting opioid analgesic structurally related to codeine and morphine. O-Alkyl, N-desmethyl, and non-phenol containing derivatives of tramadol were synthesized to probe their effect on metabolic stability and both in vitro and in vivo potency.
authors.affiliation: Sepracor Inc., Medicinal Chemistry, 84 Waterford Drive, Marlborough, MA 01752, USA. Liming.shao@sepracor.com
authors.forename: Liming
authors.initials: L
authors.lastname: Shao
authors.forename: Michael
authors.initials: M
authors.lastname: Hewitt
authors.forename: Thomas P
authors.initials: TP
authors.lastname: Jerussi
authors.forename: Frank
authors.initials: F
authors.lastname: Wu
authors.forename: Scott
authors.initials: S
authors.lastname: Malcolm
authors.forename: Paul
authors.initials: P
authors.lastname: Grover
authors.forename: Kevin
authors.initials: K
authors.lastname: Fang
authors.forename: Patrick
authors.initials: P
authors.lastname: Koch
authors.forename: Chris
authors.initials: C
authors.lastname: Senanayake
authors.forename: Nandkumar
authors.initials: N
authors.lastname: Bhongle
authors.forename: Seth
authors.initials: S
authors.lastname: Ribe
authors.forename: Roger
authors.initials: R
authors.lastname: Bakale
authors.forename: Mark
authors.initials: M
authors.lastname: Currie
mesh_terms: D000701:Analgesics, Opioid / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D006801:Humans; D008862:Microsomes, Liver / Q000187:drug effects / Q000378:metabolism; D015394:Molecular Structure; D010146:Pain / Q000188:drug therapy; D011485:Protein Binding; D051381:Rats; D013329:Structure-Activity Relationship; D014147:Tramadol / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D000701:Analgesics, Opioid; D014147:Tramadol