AR-M 1000390 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AR-M 1000390（盐酸盐），也称为 ARM-390，是一种低内化性非肽类 δ-选择性阿片受体激动剂； SNC 80 的衍生品。

AR-M 1000390 (hydrochloride), also known as ARM-390, is a low-internalizing nonpeptidic δ-selective opioid receptor agonist; derivative of SNC 80. Does not trigger acute desensitization of the analgesic response; reduces CFA-induced hyperalgesia. Brain penetrant following systemic administration.

AR-M 1000390 (Compound 6a) exhibits the binding affinities (IC50) of 0.87±0.23 nM for the δ opioid receptor and extremely high selectivity over the μ receptor (IC50=3800±172 nM) and the κ receptor (IC50=7470±606 nM). RINm5F cells are treated with AR-M 1000390 (AR-M100390) and Cyclizine for 16-24 h before measurement of intracellular and secreted insulin levels. AR-M 1000390 mediates a dose-dependent decrease in insulin content with a maximal inhibition of ~90% at the highest concentration tested (10 μM).

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.

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Others

Other Targets

δ-opioid receptor

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209808-47-9

384.94

C23H29ClN2O

>98% (HPLC)

DMSO : ≥ 150 mg/mL; 389.67 mM

Cl.CCN(CC)C(=O)c1ccc(cc1)\C(=C2/CCNCC2)c3ccccc3

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(-20℃)

With Ice Pack

≥ 2 years