1. Metabolic Enzyme/Protease Neuronal Signaling GPCR/G Protein
  2. Drug Metabolite Opioid Receptor
  3. O-Desmethyltramadol

O-Desmethyltramadol is the main active metabolite of tramadol (Tramadol) and can cross the blood-brain barrier. O-Desmethyltramadol mainly exerts its analgesic effect by activating the µ-opioid receptor (µ-OR).

For research use only. We do not sell to patients.

O-Desmethyltramadol

O-Desmethyltramadol Chemical Structure

CAS No. : 80456-81-1

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Description

O-Desmethyltramadol is the main active metabolite of tramadol (Tramadol) and can cross the blood-brain barrier. O-Desmethyltramadol mainly exerts its analgesic effect by activating the µ-opioid receptor (µ-OR)[1][2].

Cellular Effect
Cell Line Type Value Description References
CHO EC50
120 nM
Compound: Des-methyltramadol
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay
[PMID: 24900459]
CHO EC50
240 nM
Compound: 5; (+/-)-M1
Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay
Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay
[PMID: 27096047]
In Vitro

O-Desmethyltramadol can be metabolized from Tramadol through the cytochrome P450 (CYP) 2D6 enzyme[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

249.35

Formula

C15H23NO2

CAS No.
SMILES

O[C@@](CCCC1)(C2=CC(O)=CC=C2)[C@H]1CN(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
O-Desmethyltramadol
Cat. No.:
HY-109054
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