Derivatives of tramadol for increased duration of effect.

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Shao L, Abolin C, Hewitt MC, Koch P, Varney M

Derivatives of tramadol for increased duration of effect.

Bioorg Med Chem Lett. 2006 Feb;16(3):691-4. Epub 2005 Oct 27.

PubMed ID
16257206 [ View in PubMed
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Abstract

Tramadol is a centrally acting opioid analgesic structurally related to codeine and morphine. Analogs of tramadol with deuterium-for-hydrogen replacement at metabolically active sites were prepared and evaluated in vitro and in vivo.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
TramadolMu-type opioid receptorIC 50 (nM)>10000N/AN/ADetails
TramadolMu-type opioid receptorIC 50 (nM)5300N/AN/ADetails
TramadolMu-type opioid receptorIC 50 (nM)7600N/AN/ADetails
TramadolSodium-dependent noradrenaline transporterIC 50 (nM)790N/AN/ADetails
TramadolSodium-dependent noradrenaline transporterIC 50 (nM)3600N/AN/ADetails
TramadolSodium-dependent noradrenaline transporterIC 50 (nM)2000N/AN/ADetails
TramadolSodium-dependent noradrenaline transporterIC 50 (nM)3200N/AN/ADetails
TramadolSodium-dependent serotonin transporterIC 50 (nM)4300N/AN/ADetails
TramadolSodium-dependent serotonin transporterIC 50 (nM)1900N/AN/ADetails
TramadolSodium-dependent serotonin transporterIC 50 (nM)3100N/AN/ADetails
TramadolSodium-dependent serotonin transporterIC 50 (nM)1100N/AN/ADetails