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ARM390

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Opioid-analgesic compound
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Find sources: "ARM390" – news ·newspapers ·books ·scholar ·JSTOR
(November 2024)

Pharmaceutical compound
AR-M 1000390
Clinical data
Other namesARM-390
Identifiers
CAS Number
PubChemCID
IUPHAR/BPS
ChemSpider
Chemical and physical data
FormulaC23H28N2O
Molar mass348.490 g·mol−1
3D model (JSmol)
  • CCN(CC)C(=O)C1=CC=C(C=C1)C(=C2CCNCC2)C3=CC=CC=C3
  • InChI=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
  • Key:SMUGAZNLKPFBSB-UHFFFAOYSA-N

ARM-390 is anopioid-analgesic compoundselective for thedelta opioid receptor.[1][2][3]

It is an exceptionally selective, potent δopioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.[1]

In contrast to the delta-opioid selective agonistSNC-80, ARM390 was not found to produce receptordesensitization 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.[4]

References

[edit]
  1. ^abWei ZY, Brown W, Takasaki B, Plobeck N, Delorme D, Zhou F, et al. (October 2000). "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.doi:10.1021/jm000229p.PMID 11052794.
  2. ^Marie N, Landemore G, Debout C, Jauzac P, Allouche S (August 2003). "Pharmacological characterization of AR-M1000390 at human delta opioid receptors".Life Sciences.73 (13):1691–1704.doi:10.1016/s0024-3205(03)00489-2.PMID 12875901.
  3. ^Pradhan AA, Walwyn W, Nozaki C, Filliol D, Erbs E, Matifas A, et al. (December 2010)."Ligand-directed trafficking of the δ-opioid receptor in vivo: two paths toward analgesic tolerance".The Journal of Neuroscience.30 (49):16459–16468.doi:10.1523/JNEUROSCI.3748-10.2010.PMC 3086517.PMID 21147985.
  4. ^abPradhan AA, Befort K, Nozaki C, Gavériaux-Ruff C, Kieffer BL (October 2011)."The delta opioid receptor: an evolving target for the treatment of brain disorders".Trends in Pharmacological Sciences.32 (10):581–590.doi:10.1016/j.tips.2011.06.008.PMC 3197801.PMID 21925742.
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