ARM-390HCL

中文名称:

ARM-390HCL

中文同义词:

化合物AR-M 1000390 HYDROCHLORIDE

英文名称:

AR-M 1000390 hydrochloride

英文同义词:

AR-M 1000390 hydrochloride;N,N-Diethyl-4-(phenyl-4-piperidinylideneMethyl)benzaMide Hydrochloride;ARM-390HCl;ARM-390;ARM 390;ARM-390;ARM390;N,N-Diethyl-4-[phenyl(4-piperidinylidene)methyl]benzamide hydroch loride (1:1);N,N-Diethyl-4-(phenyl(piperidin-4-ylidene)methyl)benzamide hydrochloride;ARM390 Hydrochloride

CAS号:

209808-47-9

分子式:

C23H29ClN2O

分子量:

384.94216

EINECS号:

相关类别:

API;Aromatics, Heterocycles, Pharmaceuticals, Intermediates Fine Chemicals

Mol文件:

209808-47-9.mol

储存条件 

Inert atmosphere,2-8°C

生物活性

AR-M 1000390 hydrochloride 是一种有效的选择性 δ 阿片受体激动剂，EC50 为 7.2±0.9 nM。

靶点

EC50: 7.2±0.9 nM (δ opioid receptor)

体外研究

AR-M 1000390 (Compound 6a) exhibits the binding affinities (IC 50 ) of 0.87±0.23 nM for the δ opioid receptor and extremely high selectivity over the µ receptor (IC 50 =3800±172 nM) and the κ receptor (IC 50 =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).

体内研究

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.