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Enadoline

Cat. No. M28027
Enadoline Structure
Synonym:

CI-977

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Quality Control & Documentation
Biological Activity

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

Chemical Information
Molecular Weight 396.52
Formula C24H32N2O3
CAS Number 124378-77-4
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] S L Walsh, et al. Psychopharmacology (Berl). Enadoline, a selective kappa opioid agonist: comparison with butorphanol and hydromorphone in humans

[2] S L Walsh, et al. J Pharmacol Exp Ther. Enadoline and butorphanol: evaluation of kappa-agonists on cocaine pharmacodynamics and cocaine self-administration in humans

[3] G J Carey, et al. J Pharmacol Exp Ther. Enadoline discrimination in squirrel monkeys: effects of opioid agonists and antagonists

[4] M J Field, et al. Pain. Enadoline, a selective kappa-opioid receptor agonist shows potent antihyperalgesic and antiallodynic actions in a rat model of surgical pain

[5] A C Pande, et al. Clin Neuropharmacol. Analgesic efficacy of the kappa-receptor agonist, enadoline, in dental surgery pain

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Keywords: Enadoline, CI-977 supplier, Opioid Receptor, inhibitors, activators


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