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AR-M 1000390 hydrochloride

Catalog No.
B5558
Delta-opioid receptor agonist,low-internalizing
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$163.00
Ship with 10-15 days
5mg
$149.00
Ship with 10-15 days
10mg
$255.00
Ship with 10-15 days
50mg
$885.00
Ship with 10-15 days
100mg
$1,493.00
Ship with 10-15 days

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Email: [email protected]

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Background

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.

Chemical Properties

Physical AppearanceWhite solid
StorageStore at -20°C
M.Wt384.94
Cas No.209808-47-9
FormulaC23H28N2O·HCl
Solubility<38.49mg/ml in DMSO; <38.49mg/ml in H2O
Chemical NameN,N-diethyl-4-(phenyl(piperidin-4-ylidene)methyl)benzamide hydrochloride
SDFDownload SDF
Canonical SMILESO=C(C1=CC=C(C=C1)/C(C2=CC=CC=C2)=C3CCNCC/3)N(CC)CC.Cl
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

AR-M 1000390 hydrochloride