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.
- CAS No.: 80456-81-1
- Formula: C15H23NO2
- Molecular Weight:249.35
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Opioid Receptor Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
120 nM
Compound: Des-methyltramadol
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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
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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] |
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.
Chemical Information
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CAS No. 80456-81-1
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Molecular Weight 249.35
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Formula C15H23NO2
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SMILES
O[C@@](CCCC1)(C2=CC(O)=CC=C2)[C@H]1CN(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Lee J, et al. Population pharmacokinetic analysis of tramadol and O-desmethyltramadol with genetic polymorphism of CYP2D6. Drug Des Devel Ther. 2019;13:1751-1761. [Content Brief]
[2]. Liu HC, et al. Transportation of the enantiomers of trans tramadol and O-demethyltramadol across blood-brain barrier. Yao Xue Xue Bao. 2001 Sep;36(9):644-7. Chinese. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)