ARM390 explained
| Drug Name: | AR-M 1000390 |
| Width: | 250px |
| Cas Number: | 209808-01-5 |
| Cas Supplemental: | 209808-47-9 (HCl) |
| Pubchem: | 9841259 |
| Iuphar Ligand: | 9005 |
| Chemspiderid: | 8016974 |
| Synonyms: | ARM-390 |
| C: | 23 |
| H: | 28 |
| N: | 2 |
| O: | 1 |
| Smiles: | CCN(CC)C(=O)C1=CC=C(C=C1)C(=C2CCNCC2)C3=CC=CC=C3 |
| Stdinchi: | 1S/C23H28N2O/c1-3-25(4-2)23(26)21-12-10-19(11-13-21)22(18-8-6-5-7-9-18)20-14-16-24-17-15-20/h5-13,24H,3-4,14-17H2,1-2H3 |
| Stdinchikey: | SMUGAZNLKPFBSB-UHFFFAOYSA-N |
ARM-390 is an opioid-analgesic compound selective for the delta opioid receptor.[1] [2] [3]
It is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.
In contrast to the delta-opioid selective agonist SNC-80, ARM390 was not found to produce receptor desensitization following multiple administrations. Although behavioral desensitization formed to the analgesic effect of ARM390 through a receptor internalization-independent mechanism, anxiolytic effects persisted during long-term treatment.[4] ARM390 has been dubbed a "low-internalizing agonist" of delta opioid receptors.
Notes and References
- Wei ZY, Brown W, Takasaki B, Plobeck N, Delorme D, Zhou F, Yang H, Jones P, Gawell L, Gagnon H, Schmidt R, Yue SY, Walpole C, Payza K, St-Onge S, Labarre M, Godbout C, Jakob A, Butterworth J, Kamassah A, Morin PE, Projean D, Ducharme J, Roberts E . N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues . Journal of Medicinal Chemistry . 43 . 21 . 3895–3905 . October 2000 . 11052794 . 10.1021/jm000229p .
- Marie N, Landemore G, Debout C, Jauzac P, Allouche S . Pharmacological characterization of AR-M1000390 at human delta opioid receptors . Life Sciences . 73 . 13 . 1691–1704 . August 2003 . 12875901 . 10.1016/s0024-3205(03)00489-2 .
- Pradhan AA, Walwyn W, Nozaki C, Filliol D, Erbs E, Matifas A, Evans C, Kieffer BL . Ligand-directed trafficking of the δ-opioid receptor in vivo: two paths toward analgesic tolerance . The Journal of Neuroscience. 30 . 49 . 16459–16468 . December 2010 . 21147985 . 3086517 . 10.1523/JNEUROSCI.3748-10.2010 .
- Pradhan AA, Befort K, Nozaki C, Gavériaux-Ruff C, Kieffer BL . The delta opioid receptor: an evolving target for the treatment of brain disorders . Trends in Pharmacological Sciences . 32 . 10 . 581–590 . October 2011 . 21925742 . 3197801 . 10.1016/j.tips.2011.06.008 .
