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Enadoline hydrochloride

Cat. No. M28028
Enadoline hydrochloride Structure
Synonym:

CI-977 hydrochloride

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Biological Activity

Enadoline (CI-977) hydrochloride is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects.

Chemical Information
Molecular Weight 432.98
Formula C24H33ClN2O3
CAS Number 124439-07-2
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Gabriela Trevisan, et al. Neuropharmacology. A novel, potent, oral active and safe antinociceptive pyrazole targeting kappa opioid receptors

[2] Charles W Schindler, et al. Eur J Pharmacol. Effects of kappa opioid agonists alone and in combination with cocaine on heart rate and blood pressure in conscious squirrel monkeys

[3] Ichiro Takasaki, et al. J Pharmacol Exp Ther. Suppression of acute herpetic pain-related responses by the kappa-opioid receptor agonist (-)-17-cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-epoxy-beta-[n-methyl-3-trans-3-(3-furyl) acrylamido] morphinan hydrochloride (TRK-820) in mice

[4] C P France, et al. J Pharmacol Exp Ther. Behavioral effects of 6-methylene naltrexone (nalmefene) in rhesus monkeys

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