Drug intelligence / Profile preview

o-demethyl-tramadol + tramadol

Development stage
Preclinical
Lead developer
Syntrix Pharmaceuticals
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

This is a combination of two substances: - **Tramadol** is a centrally acting synthetic analgesic used for the relief of moderate to severe pain. It acts as an agonist at μ-opioid receptors and also inhibits the reuptake of serotonin and norepinephrine, providing dual mechanisms for analgesia. Tramadol is metabolized in the liver primarily by CYP2D6 to its active metabolite O-desmethyltramadol (also known as M1), which has significantly higher affinity for μ-opioid receptors and greater analgesic potency than the parent compound[2][3][4][5]. - **O-demethyl-tramadol** (also called O-desmethyltramadol or M1) is the primary active metabolite of tramadol, produced via CYP2D6-mediated O-demethylation. It exhibits much stronger binding to μ-opioid receptors—up to 300-fold higher than tramadol—and contributes substantially to overall analgesic effect[3][5]. The combination may be considered in research or investigational settings where both parent drug and active metabolite are administered together, potentially bypassing metabolic variability due to CYP2D6 polymorphisms that affect conversion from tramadol to its active form[1]. Both components act synergistically on opioid receptors and monoaminergic pathways.

Other names
O-desmethyltramadol + tramadolO-dT + tramadolM1 + tramadol
02

Targets

NET (Norepinephrine Transporter)M1 (Muscarinic acetylcholine receptor M1)SERT (Sodium-dependent serotonin transporter)MOR (Mu opioid receptor)

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