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O-Desmethyltramadol (O-DSMT) is an opioid analgesic and the main active metabolite of tramadol. (+)-O-Desmethyltramadol is the most important metabolite of tramadol produced in the liver after tramadol is consumed.
Application: A metabolite of tramadol
CAS Number:73986-53-5
Purity:≥98%
Molecular Weight:285.81
Molecular Formula:C15H23NO2•HCl
Desmetramadol is a G-protein biase μ-opioid receptor full agonist.[4] It shows comparatively far lower affinity for the δ- and κ-opioid receptors.[5]
The two enantiomers of desmetramadol show quite distinct pharmacological profiles;[6] both (+) and (−)-desmetramadol are inactive as serotonin reuptake inhibitors,[7] but (−)-desmetramadol retains activity as a norepinephrine reuptake inhibitor,[8] and so the mix of both the parent compound and metabolites contributes significantly to the complex pharmacological profile of tramadol
Buy O-desmethyltramadol (O-DSMT) Online
Desmetramadol (INN), also known as O-desmethyltramadol (O-DSMT), is an opioid analgesic and the main active metabolite of tramadol.[2] Tramadol is demethylated by the liver enzyme CYP2D6[3] in the same way as codeine, and so similarly to the variation in effects seen with codeine, individuals who have a less active form of CYP2D6 (“poor metabolizers”) will tend to get reduced analgesic effects from tramadol. This also results in a ceiling effect (dependent on CYP2D6 availability) which limits tramadol’s range of therapeutic benefits to the treatment of moderate pain.
Desmetramadol is a G-protein biase μ-opioid receptor full agonist.[4] It shows comparatively far lower affinity for the δ- and κ-opioid receptors.[5]
The two enantiomers of desmetramadol show quite distinct pharmacological profiles;[6] both (+) and (−)-desmetramadol are inactive as serotonin reuptake inhibitors,[7] but (−)-desmetramadol retains activity as a norepinephrine reuptake inhibitor,[8] and so the mix of both the parent compound and metabolites contributes significantly to the complex pharmacological profile of tramadol
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