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AR-M 1000390 hydrochloride is a potent and selective agonist of δ-opioid receptor with IC50 value of 0.87 nM [1].

Opioid receptor is a G protein-coupled receptor with opioids as ligands. δ-opioid receptor is a opioid receptor with enkephalins as its endogenous ligands and activation of δ-opioid receptor causes analgesia.

AR-M 1000390 hydrochloride is a potent and selective δ-opioid receptor agonist with IC50 values of 0.87 nM, 3.8 and 7.47 μM for δ-opioid receptor, μ-opioid receptor and κ-opioid receptor, respectively [1]. In the SK-N-BE neuroblastoma cell line, AR-M 1000390 inhibited forskolin-stimulated cAMP accumulation with Ki and EC50 values of 106 and 111 nM, respectively. Sustained activation of opioid receptors by AR-M1000390 produced a strong desensitization [2].

In DOR-eGFP mice, ARM390 (10 mg/kg) significantly reduced CFA-induced heat hyperalgesia at day 1 and induced complete tolerance at day 5. In ARM390-tolerant mice, δ-opioid receptor uncoupled to Ca2+ channels in dorsal root ganglia [3].

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