ADL5859 HCl是一种δ-opioid receptor激动剂，K_i为0.8 nM，选择性作用于opioid receptor κ，μ，对hERG通道具有微弱的抑制活性。在32nM和37nM K_i 条件下ADL5859独立刺激δ-阿片类受体的特异选择性比µ-或者κ-阿片类受体高1000倍。在78uM IC50条件下，ADL5859表现出对hERG通道的弱的抑制效应。ADL5859对δ-阿片类受体的EC50值是20nM 。

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

ADL5859 HCl

Ethanol ：1 mg/mL (2.33 mM)

DMSO ：80 mg/mL (186.5 mM)

Water ：5 mg/mL (11.65 mM)

δ-opioid receptor,μ-opioid receptor,κ-opioid receptor

ADL5859 agonizes δ-opioid receptor with a 1000-fold selectivity than µ- or κ-opioid receptor with Ki of 32 nM and 37 nM, respectively.ADL5859 displays weak inhibitory activity at the hERG channel with an IC50 of 78 μM. The EC50 of ADL5859 against δ opioid receptor is 20 nM.

At the screening dose of 3 mg/kg p.o., ADL5859 produces 100% reversal of hyperalgesia in the inflamed paw. The oral ED50 of ADL5859 in the FCA mechanical hyperalgesia assay is 1.4 mg/kg. The antihyperalgesia produced by ADL5859 (3 mg/kg, p.o.) is reversed by pretreatment with the δ opioid antagonist naltrindole (0.3 mg/kg s.c.), thus demonstrating a δ receptor mediated effect.In the rat forced swim assay, ADL5859 (3 mg/kg p.o.) produces robust antidepressant-like activity, as evidenced by a significant decrease in the time spent immobile and a significant increase in the time spent swimming. The bioavailability of ADL5859 (3 mg/kg p.o.) in rats and dogs is 33% and 66%, respectively.ADL5859 efficiently reduces inflammatory and neuropathic pain mainly by recruiting δ-opioid receptors expressed by peripheral Nav1.8-expressing neurons.

δ-Opioid mechanisms for ADL5747 and ADL5859 effects in mice: analgesia, locomotion, and receptor internalization.
Nozaki C,et al. J Pharmacol Exp Ther. 2012 Sep;342(3):799-807. PMID: