| Bioactivity | 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[1][2]. |
| Target | IC50: 78 μM (hERG channel), 43 μM (CYP2D6) |
| Invitro | 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> ADL5859 相关抗体: |
| In Vivo | ADL-5859 (0.3-10 mg/kg; p.o. once) reverses hyperalgesia in inflamed paw of rats and shows robust antidepressant-like activity[1].1.19Pharmacokinetic Properties of ADL-5859 in Rats and Dogs[1]. |
| CAS | 850305-06-5 |
| Formula | C24H28N2O3 |
| Molar Mass | 392.49 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. 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, 51 (19), pp 5893-5896 [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. [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. |