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ICI 199441 

Cat. No. M27855
ICI 199441  Structure
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Biological Activity

ICI 199441 is a potent and selective κ-opioid receptor agonist. ICI 199441 can improve heart resistance to ischemia/reperfusion.

Chemical Information
Molecular Weight 427.8
Formula C21H25Cl3N2O
CAS Number 115199-84-3
Form Solid
Solubility (25°C) DMSO 250 mg/mL (ultrasonic)
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] Yi-Min Tao, et al. Eur J Pharmacol. LPK-26, a novel kappa-opioid receptor agonist with potent antinociceptive effects and low dependence potential

[2] Amanda J Page, et al. Am J Physiol Gastrointest Liver Physiol. Opioid modulation of ferret vagal afferent mechanosensitivity

[3] Jolan M Terner, et al. Behav Pharmacol. Effects of the long-lasting kappa opioid 2-(3,4-dichlorophenyl)-N-methyl-N-[(1S)-1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl) ethyl] acetamide in a drυg discrimination and warm water tail-withdrawal procedure

[4] Tomohisa Mori, et al. Life Sci. Differential properties between TRK-820 and U-50,488H on the discriminative stimulus effects in rats

[5] T Endoh, et al. Eur J Pharmacol. Characterization of the antinociceptive effects of TRK-820 in the rat

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Keywords: ICI 199441  supplier, Opioid Receptor, inhibitors, activators


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