In vitro and in vivo evaluation of O-alkyl derivatives of tramadol.

Article Details

Citation

Shao L, Hewitt M, Jerussi TP, Wu F, Malcolm S, Grover P, Fang K, Koch P, Senanayake C, Bhongle N, Ribe S, Bakale R, Currie M

In vitro and in vivo evaluation of O-alkyl derivatives of tramadol.

Bioorg Med Chem Lett. 2008 Mar 1;18(5):1674-80. doi: 10.1016/j.bmcl.2008.01.051. Epub 2008 Jan 18.

PubMed ID
18242987 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
TramadolMu-type opioid receptorIC 50 (nM)7600N/AN/ADetails
TramadolSodium-dependent noradrenaline transporterIC 50 (nM)3861N/AN/ADetails
TramadolSodium-dependent serotonin transporterIC 50 (nM)1493N/AN/ADetails