中文名 | ARM390 HCl |
英文名 | N,N-Diethyl-4-(phenyl-4-piperidinylidenemethyl)benzamide Hydrochloride |
别名 | 化合物AR-M 1000390 HYDROCHLORIDE N,N-二乙基-4-(苯基(哌啶-4-亚基)甲基)苯甲酰胺盐酸盐 |
英文别名 | ARM390 ARM-390 ARM 390 ARM-390HCl ARM390 HCl ARM390 Hydrochloride AR-M 1000390 hydrochloride N,N-Diethyl-4-(phenyl-4-piperidinylideneMethyl)benzaMide Hydrochloride N,N-Diethyl-4-(phenyl-4-piperidinylidenemethyl)benzamide Hydrochloride N,N-Diethyl-4-(phenyl(piperidin-4-ylidene)methyl)benzamide hydrochloride |
CAS | 209808-47-9 |
化学式 | C23H29ClN2O |
分子量 | 384.94216 |
溶解度 | DMSO,H2O |
存储条件 | under inert gas (nitrogen or Argon) at 2-8°C |
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. |
参考资料 展开查看 | 1. Wei ZY, 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 Oct 19;43(21):3895-905.2. Otieno MA, et al. Mechanistic investigation of N,N-diethyl-4-(phenyl-piperidin-4-ylidenemethyl)-benzamide-inducedinsulin depletion in the rat and RINm5F cells. Toxicol Sci. 2008 Sep;105(1):221-9. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.598 ml | 12.989 ml | 25.978 ml |
5 mM | 0.52 ml | 2.598 ml | 5.196 ml |
10 mM | 0.26 ml | 1.299 ml | 2.598 ml |
5 mM | 0.052 ml | 0.26 ml | 0.52 ml |
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