Biological Activity
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].
References
[1]. wei zy, brown w, takasaki b, et al. n,n-diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues. j med chem, 2000, 43(21): 3895-3905.
[2]. marie n, landemore g, debout c, et al. pharmacological characterization of ar-m1000390 at human delta opioid receptors. life sci, 2003, 73(13): 1691-1704.
[3]. pradhan aa, walwyn w, nozaki c, et al. ligand-directed trafficking of the -opioid receptor in vivo: two paths toward analgesic tolerance. j neurosci, 2010, 30(49): 16459-16468.
