209808-47-9

Usage

Uses

Used in Pharmaceutical Industry:
AR-M 1000390 hydrochloride is used as an analgesic agent for the treatment of pain. Its effectiveness in alleviating pain is attributed to its ability to interact with specific receptors in the body, thereby reducing the sensation of pain and providing relief to patients.

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.