87151-85-7
Chemical Structure
Spiradoline
Synonym(s): U-62066
- CAS No.: 87151-85-7
- Formula:C22H30Cl2N2O2
- Molecular Weight:425.39
IUPAC Name: 2-(3,4-dichlorophenyl)-N-methyl-N-((5R,7S,8S)-7-(pyrrolidin-1-yl)-1-oxaspiro[4.5]decan-8-yl)acetamide
InChIKey: NYKCGQQJNVPOLU-ONTIZHBOSA-N
SMILES: ClC1=CC(CC(N([C@H]([C@H](C2)N3CCCC3)CC[C@]42CCCO4)C)=O)=CC=C1Cl
Biological Activity: Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier[1][2].
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Spiradoline | Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier. | |||||||||||||||||||||
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References
- [1]. Elena I Varlinskaya, et al. Stress alters social behavior and sensitivity to pharmacological activation of kappa opioid receptors in an age-specific manner in Sprague Dawley rats. Neurobiol Stress. 2018 Sep 11;9:124-132. [Content Brief]
- [2]. M-L G Wadenberg. A review of the properties of spiradoline: a potent and selective kappa-opioid receptor agonist. CNS Drug Rev. Summer 2003;9(2):187-98. [Content Brief]
