ADL5859
Based on 1 publication(s) in Google Scholar
ADL-5859 is a selective and orally active δ opioid receptor (DOR) agonist with an Ki and an EC50 value of 0.84 and 20 nM, respectively. ADL-5859 also shows inhibitory activity to hERG channel with an IC50 value of 78 μM. ADL-5859 can be used for the research of pain.
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- CAS No.: 850305-06-5
- Formule: C24H28N2O3
- Masse moléculaire:392.49
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) ADL5859
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Cell Proliferation/Viability Assay
Voir tous les produits spécifiques à Isoform Opioid Receptor
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Activité biologique
IC50: 78 μM (hERG channel), 43 μM (CYP2D6)[1][2]
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
20 nM
Compound: 20, ADL5859
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Agonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS binding
Agonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS binding
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[PMID: 18788723] |
| HEK293 | IC50 |
78 μM
Compound: 20, ADL5859
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Inhibition of human ERG channel in HEK293 cells by voltage-clamp method
Inhibition of human ERG channel in HEK293 cells by voltage-clamp method
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[PMID: 18788723] |
ADL-5859 (0-10 μM) shows activities to δ opioid receptor with an Ki and an EC50 value of 0.84 and 20 nM, and inhibits 32% and 37% activities to µ and κ opioid receptor, respectively[1]. ADL-5859 (0-100 μM) exhibits inhibitory activity to hERG channel with an IC50 value of 78 μM[1]. ADL-5859 (0-100 μM) inhibits activity of the drug metabolizing enzyme cytochrome P450 2D6 (CYP2D6) in vitro with an IC50 value of 43 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 850305-06-5
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Masse moléculaire 392.49
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Formule C24H28N2O3
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SMILES
O=C(N(CC)CC)C1=CC=C(C2=CC3(CCNCC3)OC4=C2C(O)=CC=C4)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Eur J Pharmacol
Synergistic antidepressant-like effects between a kappa opioid antagonist (LY2444296) and a delta opioid agonist (ADL5859) in the mouse forced swim test. [Abstract]2016 Jun 15:781:53-9. PMID: 27044434
ADL5859 purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2016 Jun 15:781:53-9. [Abstract]
The DOR agonist ADL5859 shows antidepressant-like effects in the FST in C57BL/6J mice.
Pureté et documentation
Références
[2]. Le Bourdonnec B, et al. Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859). J Med Chem. 2008 Oct 9;51(19):5893-6. [Content Brief]
[3]. Le Bourdonnec B, et al. Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747).J Med Chem. 2009 Sep 24;52(18):5685-702. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ADL5859 Related Classifications
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