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Enadoline

Chemical Structure : Enadoline

CAS No.: 124378-77-4

Enadoline (CI 977;PD 129290)

Catalog No.: PC-62107Not For Human Use, Lab Use Only.

Enadoline (CI 977.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Enadoline (CI 977;PD 129290) is a potent, selective κ-opioid receptor (KOR) agonist with Ki of 0.11 nM, binding with high affinity to [3H]-U69593-labelled kappa-sites; produces a potent inhibition of the electrically-evoked contractions of the guinea-pig ileum and rabbit vas deferens with IC50 values of 0.087 nM and 3.3 nM, respectively; is effective in reducing infarction in a model of focal cerebral ischaemia.

Pain

Phase 2 Discontinued

Physicochemical Properties

M.Wt 396.531
Formula C24H32N2O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(1-benzofuran-4-yl)-N-methyl-N-[(5R,7S,8S)-7-pyrrolidin-1-yl-1-oxaspiro[4.5]decan-8-yl]acetamide

References

1. Hunter JC, et al. Br J Pharmacol. 1990 Sep;101(1):183-9.

2. Singh L, et al. Eur J Pharmacol. 1990 Dec 4;191(3):477-80.

3. Kusumoto K, et al. Brain Res. 1992 Mar 27;576(1):147-51.

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