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

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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

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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

Drug	Target	Property	Measurement	pH	Temperature (°C)
Tramadol	Mu-type opioid receptor	IC 50 (nM)	7600	N/A	N/A	Details
Tramadol	Sodium-dependent noradrenaline transporter	IC 50 (nM)	3861	N/A	N/A	Details
Tramadol	Sodium-dependent serotonin transporter	IC 50 (nM)	1493	N/A	N/A	Details