Spiradoline (Synonyms: U-62066)

Cat. No.: HY-106756: FAQs
Data Sheet Handling Instructions

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Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a K_i of 8.6 nM in guinea pig. The K_i 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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Spiradoline Chemical Structure

CAS No. : 87151-85-7

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Other Forms of Spiradoline:

Spiradoline mesylate Get quote

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•Related Small Molecules:

•Related Proteins:

View All Opioid Receptor Isoform Specific Products:

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

Biological Activity
Purity & Documentation
References
Customer Review

Description

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

Spiradoline (U-62066; 0.1-0.4 mg/kg; subcutaneous injection; once; Sprague-Dawley rats) treatment dose-dependently reduces social behaviors in non-stressed adults, producing social avoidance at the highest dose tested, while younger animals displays reduced sensitivity to this socially suppressing effect of Spiradoline. In stressed animals, the socially suppressing effects of the Spiradoline are blunted at all ages, with juveniles and adolescents exhibiting increased social preference in response to certain doses of U-62066^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Juvenile, adolescent and adult Sprague-Dawley male and female rats exposured to repeated restraint^[1]
Dosage:	0.1 mg/kg, 0.2 mg/kg, 0.3 mg/kg, and 0.4 mg/kg
Administration:	Subcutaneous injection; once
Result:	Dose-dependently reduced social behaviors in non-stressed adults, producing social avoidance at the highest dose tested.

Molecular Weight

425.39

Formula

C₂₂H₃₀Cl₂N₂O₂

CAS No.

87151-85-7

SMILES

ClC1=CC(CC(N([C@H]([C@H](C2)N3CCCC3)CC[C@]42CCCO4)C)=O)=CC=C1Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (117.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.88 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Handling Instructions (2659 KB)

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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3508 mL	11.7539 mL	23.5078 mL	58.7696 mL
	5 mM	0.4702 mL	2.3508 mL	4.7016 mL	11.7539 mL
	10 mM	0.2351 mL	1.1754 mL	2.3508 mL	5.8770 mL
	15 mM	0.1567 mL	0.7836 mL	1.5672 mL	3.9180 mL
	20 mM	0.1175 mL	0.5877 mL	1.1754 mL	2.9385 mL
	25 mM	0.0940 mL	0.4702 mL	0.9403 mL	2.3508 mL
	30 mM	0.0784 mL	0.3918 mL	0.7836 mL	1.9590 mL
	40 mM	0.0588 mL	0.2938 mL	0.5877 mL	1.4692 mL
	50 mM	0.0470 mL	0.2351 mL	0.4702 mL	1.1754 mL
	60 mM	0.0392 mL	0.1959 mL	0.3918 mL	0.9795 mL
	80 mM	0.0294 mL	0.1469 mL	0.2938 mL	0.7346 mL
	100 mM	0.0235 mL	0.1175 mL	0.2351 mL	0.5877 mL

Spiradoline Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Spiradoline87151-85-7U-62066U62066U 62066Opioid ReceptorKORκ-opioidarylacetamideanalgesicdiureticantiarrythmicneuroprotectiveBBBantitussiveInhibitorinhibitorinhibit

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