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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- CAS No.: 87151-85-7
- 화학식: C22H30Cl2N2O2
- 분자량:425.39
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Biological Activity
제품 설명
IC50 & Target
Ki: 8.6 nM (κ-opioid receptor in guinea pig), 252 nM (μ-receptor) and 9400 nM (δ-receptor)[2]
In Vitro
Using the patch-clamp method in isolated rat cardiac myocytes, indicated that Spiradoline (15 to 500 μM) produces its antiarrythmic effect via blockade of sodium channels (and at the higher doses also of potassium currents) in myocardial tissue. Thus, Spiradoline reduces the peak sodium current, increased the decay rate of the transient outward potassium current, and reduced the sustained plateau potassium amplitude[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Juvenile, adolescent and adult Sprague-Dawley male and female rats exposured to repeated restraint[1]
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Dosage:0.1 mg/kg, 0.2 mg/kg, 0.3 mg/kg, and 0.4 mg/kg
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Administration:Subcutaneous injection; once
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Result:Dose-dependently reduced social behaviors in non-stressed adults, producing social avoidance at the highest dose tested.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 87151-85-7
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분자량 425.39
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화학식 C22H30Cl2N2O2
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SMILES
ClC1=CC(CC(N([C@H]([C@H](C2)N3CCCC3)CC[C@]42CCCO4)C)=O)=CC=C1Cl
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Synonyms
U-62066
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Spiradoline Related Classifications
HY-106756 Related Classifications
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