| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
Ki: 8.6 nM (κ-opioid receptor in guinea pig), 252 nM (μ-receptor) and 9400 nM (δ-receptor)[2]
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| ln Vitro |
Employing the patch-clamp technique on isolated rat heart myocytes, it was found that spirol (15–500 μM) inhibits potassium currents and sodium channels in cardiac tissue to create its antiarrhythmic activity. At higher concentrations, it also blocks potassium channels. Consequently, spiradoline decreases the sustained plateau potassium amplitude, increases the decay rate of the transient outward potassium current, and decreases the peak sodium current[2].
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| ln Vivo |
In non-stressed adults, Spiradoline (U-62066; 0.1-0.4 mg/kg; subcutaneous injection; once; Sprague-Dawley rats) treatment dose-dependently decreases social behaviors, resulting in social avoidance at the highest dose tested. However, in younger animals, Spiradoline's socially suppressive effect is less pronounced. The Spiradoline's socially suppressive effects are attenuated in stressed animals at all ages, with juveniles and adolescents responding to specific dosages of U-62066 with greater social preference[1].
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| Animal Protocol |
Animal/Disease Models: Juvenile, adolescent and adult SD (Sprague-Dawley) male and female rats exposed to repeated restraint[1]
Doses: 0.1 mg/kg, 0.2 mg/kg, 0.3 mg/kg, and 0.4 mg/kg Route of Administration: subcutaneous (sc) injection; once Experimental Results: Dose -dependently decreased social behaviors in non-stressed adults, producing social avoidance at the highest dose tested. |
| 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.
[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. |
| Molecular Formula |
C22H30CL2N2O2
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|---|---|
| Molecular Weight |
425.39
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| CAS # |
87151-85-7
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| Related CAS # |
Spiradoline mesylate;87173-97-5
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| SMILES |
N([C@H]1CC[C@]2(OCCC2)C[C@@H]1N1CCCC1)(C)C(=O)CC1C=CC(Cl)=C(Cl)C=1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 50 mg/mL (117.54 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.88 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3508 mL | 11.7539 mL | 23.5078 mL | |
| 5 mM | 0.4702 mL | 2.3508 mL | 4.7016 mL | |
| 10 mM | 0.2351 mL | 1.1754 mL | 2.3508 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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