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.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-03, Vol.18 (5), p.1674-1680
Hauptverfasser:	Shao, Liming, Hewitt, Michael, Jerussi, Thomas P., Wu, Frank, Malcolm, Scott, Grover, Paul, Fang, Kevin, Koch, Patrick, Senanayake, Chris, Bhongle, Nandkumar, Ribe, Seth, Bakale, Roger, Currie, Mark
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesics, Opioid - chemistry Analgesics, Opioid - metabolism Analgesics, Opioid - pharmacology Animals Humans Metabolic stability Microsomes, Liver - drug effects Microsomes, Liver - metabolism Molecular Structure Opioids Pain - drug therapy Protein Binding Rats Structure-Activity Relationship Tramadol Tramadol - analogs & derivatives Tramadol - chemistry Tramadol - metabolism Tramadol - pharmacology
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Beschreibung
Zusammenfassung:	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.
ISSN:	0960-894X 0968-0896 1464-3405 1464-3391
DOI:	10.1016/j.bmcl.2008.01.051