In vitro and in vivo evaluation of O-alkyl derivatives of tramadol.
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.
Shao
Liming
L
Sepracor Inc., Medicinal Chemistry, 84 Waterford Drive, Marlborough, MA 01752, USA. Liming.shao@sepracor.com
Hewitt
Michael
M
Jerussi
Thomas P
TP
Wu
Frank
F
Malcolm
Scott
S
Grover
Paul
P
Fang
Kevin
K
Koch
Patrick
P
Senanayake
Chris
C
Bhongle
Nandkumar
N
Ribe
Seth
S
Bakale
Roger
R
Currie
Mark
M
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*
D000701:Analgesics, Opioid; D014147:Tramadol