ADL5859 Hydrochloride

ADL5859 Hydrochloride is a novel δ-opioid agonists that shows good oral bioavailability and analgesic and antidepressive effects in the rat and represent potential drugs for chronic pain treatment. ADL5859 HCl significantly reduced inflammatory and neuropathic pain. The antiallodynic effects of ADL5859 was abolished in constitutive δ-receptor KO mice and strongly diminished in δ-receptor cKO mice. ADL5859 Hydrochloride did not induce either hyperlocomotion or receptor internalization in vivo. ADL5859 also displayed weak inhibitory activity at the hERG channel (IC50 = 78 µM). ADL5859 HCl efficiently reduces inflammatory and neuropathic pain mainly by recruiting δ-opioid receptors expressed by peripheral Nav1.8-expressing neurons.