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ARM390

Cat. No. M8776
ARM390 Structure
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Biological Activity

ARM390 in a δ-selective opioid receptor agonist derivative of SNC80. ARM390 leads to very low levels of receptor internalization, and does not induce acute desensitization of analgesic response compared to SNC80. ARM390 preferentially recruits arrestin 3 to the delta opioid receptor in mice.

Chemical Information
Molecular Weight 348.48
Formula C23H28N2O
CAS Number 209808-01-5
Solubility (25°C) DMSO: 2 mg/mL (warmed)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jesse J DiCello, et al. Agonist-dependent development of delta opioid receptor tolerance in the colon

[2] Ana Vicente-Sanchez, et al. Tolerance to high-internalizing δ opioid receptor agonist is critically mediated by arrestin 2

[3] Amynah A Pradhan, et al. Agonist-Specific Recruitment of Arrestin Isoforms Differentially Modify Delta Opioid Receptor Function

[4] S Stevens Negus, et al. Effects of the δ opioid receptor agonist SNC80 on pain-related depression of intracranial self-stimulation (ICSS) in rats

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