209808-47-9
209808-47-9 structure
- Name: AR-M 1000390 hydrochloride
- Chemical Name: N,N-Diethyl-4-[phenyl(4-piperidinylidene)methyl]benzamide hydroch loride (1:1)
- CAS Number: 209808-47-9
- Molecular Formula: C23H29ClN2O
- Molecular Weight: 384.942
- Catalog: Signaling Pathways GPCR/G Protein Opioid Receptor
- Create Date: 2016-01-03 08:43:40
- Modify Date: 2024-01-03 14:58:37
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AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.
| Name | N,N-Diethyl-4-[phenyl(4-piperidinylidene)methyl]benzamide hydroch loride (1:1) |
|---|---|
| Synonyms |
Benzamide, N,N-diethyl-4-(phenyl-4-piperidinylidenemethyl)-, hydrochloride (1:1)
N,N-Diethyl-4-[phenyl(4-piperidinylidene)methyl]benzamide hydrochloride (1:1) ARM390 Hydrochloride N,N-Diethyl-4-(phenyl-4-piperidinylidenemethyl)benzamide Hydrochloride AR-M 1000390 (hydrochloride) |
| Description | AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency. |
|---|---|
| Related Catalog | |
| Target |
EC50: 7.2±0.9 nM (δ opioid receptor)[1] |
| In Vitro | 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)[1]. 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)[2]. |
| In Vivo | 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[2]. |
| Cell Assay | RINm5F cells are seeded in 24-well plates and treated with vehicle (DMSO), 10 μM AR-M 1000390 (AR-M100390), and 10 μM Cyclizine in serum-free medium; cells are rinsed with phosphate-buffered saline and stored at -80°C until analysis. RNA is isolated with the RNeasy purification system with DNAse treatment[2]. |
| Animal Admin | Rats[2] Han Wistar rats (six per treatment group) are treated with vehicle (saline) or 5, 100, and 600 μmol/kg/day of AR-M 1000390 (AR-M100390) for 7 days. A separate group of rats are treated with 600 μmol/kg/day for 7 days followed by a 14-day recovery period. Another group is treated with 600 μmol/kg/day for 3 days. Blood sampling for glucose, lipids, and insulin measurements are taken on days 2, 4, 8, and 22. Blood sampling for AR-M 1000390 concentration measurements are collected on days 4 and 8. The animals are euthanized with CO2 on days 4, 8, and 22 and the pancreas isolated and processed for histopathology, insulin immunohistochemistry, and insulin mRNA analyses[2]. |
| References |
| Molecular Formula | C23H29ClN2O |
|---|---|
| Molecular Weight | 384.942 |
| Exact Mass | 384.196838 |
| PSA | 32.34000 |
| LogP | 5.48470 |
| Storage condition | 2-8℃ |