| Identification | Back Directory | [Name]
AR-M 1000390 hydrochloride | [CAS]
209808-47-9 | [Synonyms]
ARM-390
ARM-390HCl
AR-M1000390 HCl
ARM390 Hydrochloride
ARM 390;ARM-390;ARM390
AR-M 1000390 hydrochloride
N,N-Diethyl-4-(phenyl-4-piperidinylideneMethyl)benzaMide Hydrochloride
N,N-Diethyl-4-(phenyl(piperidin-4-ylidene)methyl)benzamide hydrochloride
Benzamide,N,N-diethyl-4-(phenyl-4-piperidinylidenemethyl)-,monohydrochloride
N,N-Diethyl-4-[phenyl(4-piperidinylidene)methyl]benzamide hydroch loride (1:1) | [Molecular Formula]
C23H29ClN2O | [MDL Number]
MFCD20926357 | [MOL File]
209808-47-9.mol | [Molecular Weight]
384.942 |
| Hazard Information | Back Directory | [Uses]
N,N-Diethyl-4-(phenyl-4-piperidinylidenemethyl)benzamide Hydrochloride is a (arylheteroaryl)methylene]piperidine derivatives with analgesic effect. | [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]. | [in vivo]
Rats are treated with 5, 100, and 600 μmol/kg of AR-M 1000390 (AR-M100390) for 3 and/or 7 days; another group of rats treated with 600 μmol/kg of compound are allowed to recover for 14 days. AR-M 1000390 (600 μmol/kg) causes vacuolation in the β-cell of the rat pancreas that is associated with depletion of insulin and hyperglycemia after 7 days of dosing. Treatment of rats with 600 μmol/kg of AR-M 1000390 results in vacuolation of the β-cell of the rat pancreas that is similar to that reported for cyclizine and cyproheptadine[2]. | [IC 50]
δ Opioid Receptor/DOR | [storage]
Store at -20°C | [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. |
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BOC Sciences
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