For research use only. Not for therapeutic Use.
ADL-5859 hydrochloride (compound 20) 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 hydrochloride also shows inhibitory activity to hERG channel with an IC50 value of 78 μM. ADL-5859 hydrochloride can be used for the research of pain[1][2].
ADL-5859 (0-10 μM) hydrochloride 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) hydrochloride exhibits inhibitory activity to hERG channel with an IC50 value of 78 μM[1].
ADL-5859 (0-100 μM) hydrochloride inhibits activity of the drug metabolizing enzyme cytochrome P450 2D6 (CYP2D6) in vitro with an IC50 value of 43 μM[2].
ADL-5859 (0.3-10 mg/kg; p.o. once) hydrochloride reverses hyperalgesia in inflamed paw of rats and shows robust antidepressant-like activity[1].
1.19
Pharmacokinetic Properties of ADL-5859 in Rats and Dogs[1].
RatsIV 0.25 mg/kg and PO 3 mg/kg
DogsIV 1 mg/kg and PO 3 mg/kg
CLs (L/h/kg)
1.8±0.5
0.4±0.1
Vdss (L/kg)
10.7±1.9
2.5±0.5
t1/2 (oral, h)
5.3±0.7
4.7±0.2
F (%)
33.4±3.2
66.5±6.8
| Catalog Number | I001223 |
| CAS Number | 850173-95-4 |
| Synonyms | N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4′-piperidine]-4-yl)benzamide;hydrochloride |
| Molecular Formula | C24H29ClN2O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H28N2O3.ClH/c1-3-26(4-2)23(28)18-10-8-17(9-11-18)19-16-24(12-14-25-15-13-24)29-21-7-5-6-20(27)22(19)21;/h5-11,16,25,27H,3-4,12-15H2,1-2H3;1H |
| InChIKey | ZFNLSWREIULTDO-UHFFFAOYSA-N |
| SMILES | CCN(CC)C(=O)C1=CC=C(C=C1)C2=CC3(CCNCC3)OC4=CC=CC(=C42)O.Cl |
| Reference | [1]. 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. [2]. 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. |
