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SR16835

Cat. No. M41884
SR16835 Structure
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Biological Activity

SR16835 has high affinity for both NOPr and MOPr, with full agonist activity for NOPr and partial agonist activity for MOPr.

Chemical Information
Molecular Weight 386.53
Formula C26H30N2O
CAS Number 1207195-45-6
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] Stephen R Morairty et al. Proc Natl Acad Sci U S A. Activation of the nociceptin/orphanin-FQ receptor promotes NREM sleep and EEG slow wave activity

[2] Thomas Günther et al. Br J Pharmacol. Targeting multiple opioid receptors - improved analgesics with reduced side effects?

[3] Taline V Khroyan et al. J Pharmacol Exp Ther. Differential effects of nociceptin/orphanin FQ (NOP) receptor agonists in acute versus chronic pain: studies with bifunctional NOP/μ receptor agonists in the sciatic nerve ligation chronic pain model in mice

[4] Lawrence Toll et al. J Pharmacol Exp Ther. Comparison of the antinociceptive and antirewarding profiles of novel bifunctional nociceptin receptor/mu-opioid receptor ligands: implications for therapeutic applications

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