ADL5859 HCl (CAS 850173-95-4)
Application:
ADL5859 HCl is a selective receptor agonist for the δ-opioid receptor
CAS Number:
850173-95-4
Molecular Weight:
428.95
Molecular Formula:
C24H28N2O3•HCl
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
ADL5859 HCl is a selective δ-opioid receptor agonist (Ki=0.84 nM, EC50=20 nM) with Ki values for µ and κ receptors being 32 nM and 37 nM respectively. It also displayed weak inhibitory activity at the hERG channel (IC50= 78 µM).
ADL5859 HCl (CAS 850173-95-4) References
- 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). | Le Bourdonnec, B., et al. 2009. J Med Chem. 52: 5685-702. PMID: 19694468
- Δ-Opioid mechanisms for ADL5747 and ADL5859 effects in mice: analgesia, locomotion, and receptor internalization. | Nozaki, C., et al. 2012. J Pharmacol Exp Ther. 342: 799-807. PMID: 22700431
- Novel screening assay for the selective detection of G-protein-coupled receptor heteromer signaling. | van Rijn, RM., et al. 2013. J Pharmacol Exp Ther. 344: 179-88. PMID: 23097213
- Opiate-induced analgesia: contributions from mu, delta and kappa opioid receptors mouse mutants. | Gavériaux-Ruff, C. 2013. Curr Pharm Des. 19: 7373-81. PMID: 23448470
- In vivo properties of KNT-127, a novel Δ opioid receptor agonist: receptor internalization, antihyperalgesia and antidepressant effects in mice. | Nozaki, C., et al. 2014. Br J Pharmacol. 171: 5376-86. PMID: 25048778
- Delta opioid receptors expressed in forebrain GABAergic neurons are responsible for SNC80-induced seizures. | Chung, PC., et al. 2015. Behav Brain Res. 278: 429-34. PMID: 25447299
- β-Arrestin 2 dependence of Δ opioid receptor agonists is correlated with alcohol intake. | Chiang, T., et al. 2016. Br J Pharmacol. 173: 332-43. PMID: 26507558
- Synergistic antidepressant-like effects between a kappa opioid antagonist (LY2444296) and a delta opioid agonist (ADL5859) in the mouse forced swim test. | Huang, P., et al. 2016. Eur J Pharmacol. 781: 53-9. PMID: 27044434
- In silico design of novel probes for the atypical opioid receptor MRGPRX2. | Lansu, K., et al. 2017. Nat Chem Biol. 13: 529-536. PMID: 28288109
- Agonist-induced phosphorylation bar code and differential post-activation signaling of the delta opioid receptor revealed by phosphosite-specific antibodies. | Mann, A., et al. 2020. Sci Rep. 10: 8585. PMID: 32444688
- Opportunities and Challenges for In Silico Drug Discovery at Delta Opioid Receptors. | Meqbil, YJ. and van Rijn, RM. 2022. Pharmaceuticals (Basel). 15: PMID: 35890173
- To probe the activation mechanism of the Delta opioid receptor by an agonist ADL5859 started from inactive conformation using molecular dynamic simulations. | Dean, E., et al. 2022. J Biomol Struct Dyn. 1-18. PMID: 35938617
- Exploration of beta-arrestin isoform signaling pathways in delta opioid receptor agonist-induced convulsions. | Blaine, AT., et al. 2022. Front Pharmacol. 13: 914651. PMID: 36059958
- Development of a novel cell-based, In-Cell Western/ERK assay system for the high-throughput screening of agonists acting on the delta-opioid receptor. | Asghar, J., et al. 2022. Front Pharmacol. 13: 933356. PMID: 36225576
Inhibitor of:
DOR-1, and neurexin II.Activator of:
DOR, KOR-1, and MOR.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
ADL5859 HCl, 5 mg | sc-364396 | 5 mg | $255.00 | |||
ADL5859 HCl, 50 mg | sc-364396A | 50 mg | $1455.00 |