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U-62066

Cat. No. M8834
U-62066 Structure
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Biological Activity

Highly selective κ opioid receptor agonist; antitussive.

Chemical Information
Molecular Weight 521.5
Formula C22H30Cl2N2O2 · CH3SO3H
CAS Number 87151-85-7
Solubility (25°C) Water: 14 mg/mL
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] Marthe M Vandeputte, et al. Characterization of recent non-fentanyl synthetic opioids via three different in vitro µ-opioid receptor activation assays

[2] Elena I Varlinskaya, et al. Stress alters social behavior and sensitivity to pharmacological activation of kappa opioid receptors in an age-specific manner in Sprague Dawley rats

[3] Y B Lishmanov, et al. Participation of central and peripheral kappa 1 and kappa 2 opioid receptors in arrhythmogenesis

[4] H Sershen, et al. Effect of ibogaine on cocaine-induced efflux of [3H] dopamine and [3H] serotonin from mouse striatum

[5] M F Piercey, et al. Spinal analgesic actions of kappa receptor agonists, U-50488H and spiradoline (U-62066)

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