AR-M 1000390 hydrochloride |
Catalog No.GC12219 |
El clorhidrato de AR-M 1000390 es un agonista del receptor opioide δ excepcionalmente selectivo y potente con una EC50 de 7,2 ± 0,9 nM para la potencia del agonista δ.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 209808-47-9
Sample solution is provided at 25 µL, 10mM.
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.
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