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U-69593

Cat. No. M8832
U-69593 Structure
Synonym:

U69593

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Biological Activity

U-69593 is a selective κ opioid receptor agonist. U-69593 is known to inhibit cocaine sensitization in meso-limbic dopamine neurons by normalizing basal overflow of dopamine.

Chemical Information
Molecular Weight 356.5
Formula C22H32N2O2
CAS Number 96744-75-1
Solubility (25°C) 45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 10 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] Philemon Kipkemoi Towett, et al. Activation of micro, delta or kappa opioid receptors by DAMGO, DPDPE, U-50488 or U-69593 respectively causes antinociception in the formalin test in the naked mole-rat (Heterocephalus glaber)

[2] Elena Zakharova, et al. Depletion of serotonin decreases the effects of the kappa-opioid receptor agonist U-69593 on cocaine-stimulated activity

[3] Anabel Puig-Ramos, et al. U-69593, a kappa opioid receptor agonist, decreases cocaine-induced behavioral sensitization in female rats

[4] R A Lahti, et al. [3H]U-69593 a highly selective ligand for the opioid kappa receptor

[5] B Nock, et al. [3H]U-69593 labels a subtype of kappa opiate receptor with characteristics different from that labeled by [3H]ethylketocyclazocine

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