ADL-5859 (hydrochloride)

ADL-5859 hydrochloride (compound 20) is a selective and orally active δ opioid receptor (DOR) agonist with an K_i 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]. IC50 & Target:IC50: 78 μM (hERG channel), 43 μM (CYP2D6)^[1][2] In Vitro:ADL-5859 (0-10 μM) hydrochloride shows activities to δ opioid receptor with an K_i 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]. In Vivo: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].
Pharmacokinetic Properties of ADL-5859 in Rats and Dogs^[1].

	Rats IV 0.25 mg/kg and PO 3 mg/kg	Dogs IV 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