Cat. No.: HY-B1371

Spiperone

(Synonyms: Spiroperidol)

3 Cited Publications

Customer Review

Based on 3 publication(s) in Google Scholar

Spiperone (Spiroperidol) is a potent dopamine D2, serotonin 5-HT_1A, and serotonin 5-HT_2A antagonist. Spiperone is also a labelled ligand for neuroleptic receptors. Spiperone enhances intracellular calcium level and inhibits the Wnt signaling pathway. Spiperone has the potential for the research of neurology diseases.

For research use only. We do not sell to patients.

Purity: 99.00%
CAS No.: 749-02-0
Formula: C₂₃H₂₆FN₃O₂
Molecular Weight:395.47

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Spiperone Chemical Structure

CAS No.: 749-02-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

5-HT_1A Receptor

5-HT_2A Receptor

All Dopamine Receptor Isoforms :

All 5-HT Receptor Isoforms :

All Wnt Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.25 nM Compound: Spiperone	Displacement of [3H]Spiperone from human recombinant dopamine D2S receptor expressed in CHO cells after 2 hrs Displacement of [3H]Spiperone from human recombinant dopamine D2S receptor expressed in CHO cells after 2 hrs	[PMID: 23403082]
CHO	IC₅₀	0.36 nM Compound: Spiperone	Displacement of [3H]Spiperone from human recombinant dopamine D3 receptor expressed in CHO cells after 2 hrs Displacement of [3H]Spiperone from human recombinant dopamine D3 receptor expressed in CHO cells after 2 hrs	[PMID: 23403082]
CHO-K1	IC₅₀	0.5 nM Compound: Spiperone	Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs	[PMID: 23403082]
CHO-K1	IC₅₀	97 nM Compound: Spiperone	Antagonist activity at dopamine D3 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 assessed as inhibition of agonist-induced response incubated for 60 mins in incubator followed by 15 mins at room temperature by FLIPR assay Antagonist activity at dopamine D3 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 assessed as inhibition of agonist-induced response incubated for 60 mins in incubator followed by 15 mins at room temperature by FLIPR assay	[PMID: 23675993]
H4	EC₅₀	>50 μM Compound: 12f	Induction of autophagy in human H4 cells expressing LC3 using DAPI staining after 4 hrs by fluorescence microscopic analysis Induction of autophagy in human H4 cells expressing LC3 using DAPI staining after 4 hrs by fluorescence microscopic analysis	[PMID: 21126871]
HEK293	IC₅₀	1.27 nM Compound: Spiperone	Displacement of [3H]Spiprone from human dopamine D2 receptor expressed in HEK293 cells Displacement of [3H]Spiprone from human dopamine D2 receptor expressed in HEK293 cells	[PMID: 22748706]

In Vitro

Spiperone (5 μM, 24 h) specifically inhibits Wnt signaling by targeting the Wnt/LRP complex in HEK293 cells^[4].
Spiperone (1-10 μM, 275-470 s) induces a rise in intracellular calcium levels in HEK293 cells^[4].

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

Chemical Information

CAS No. 749-02-0
Appearance Solid
Molecular Weight 395.47
Formula C₂₃H₂₆FN₃O₂
Color Off-white to light yellow
SMILES

O=C1NCN(C2=CC=CC=C2)C13CCN(CCCC(C4=CC=C(F)C=C4)=O)CC3
Synonyms

Spiroperidol
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

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Journal Impact Factor

Insect Biochem Mol Biol

Molecular and pharmacological characterization of the dopamine receptors in the oriental fruit fly, Bactrocera dorsalis. [Abstract]

2025 May:180:104312. PMID: 40245998
J Ocul Pharmacol Ther

Survey of Dopamine Receptor D2 Antagonists as Retinal Antifibrotics. [Abstract]

2024 Oct;40(8):536-542. PMID: 39206555
bioRxiv

2026 Apr 1.

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (84.28 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5286 mL

12.6432 mL

25.2864 mL

5 mM

0.5057 mL

2.5286 mL

5.0573 mL

10 mM

0.2529 mL

1.2643 mL

2.5286 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

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

Stock Solution Working Solution

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: ≥ 4.55 mg/mL (11.51 mM); Clear solution

This protocol yields a clear solution of ≥ 4.55 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.5 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Metwally KA, et al. Spiperone: influence of spiro ring substituents on 5-HT2A serotonin receptor binding. J Med Chem. 1998;41(25):5084-5093. [Content Brief]

[2]. Palacios JM, et al. [3H]Spiperone binding sites in brain: autoradiographic localization of multiple receptors. Brain Res. 1981 Jun 1;213(2):277-89. [Content Brief]

[3]. Leysen JE, et al. Spiperone: a ligand of choice for neuroleptic receptors. 1. Kinetics and characteristics of in vitro binding. Biochem Pharmacol. 1978 Feb 1;27(3):307-16. [Content Brief]

[4]. Lu D, et al. Spiperone enhances intracellular calcium level and inhibits the Wnt signaling pathway. BMC Pharmacol. 2009 Nov 30;9:13. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5286 mL	12.6432 mL	25.2864 mL	63.2159 mL
	5 mM	0.5057 mL	2.5286 mL	5.0573 mL	12.6432 mL
	10 mM	0.2529 mL	1.2643 mL	2.5286 mL	6.3216 mL
	15 mM	0.1686 mL	0.8429 mL	1.6858 mL	4.2144 mL
	20 mM	0.1264 mL	0.6322 mL	1.2643 mL	3.1608 mL
	25 mM	0.1011 mL	0.5057 mL	1.0115 mL	2.5286 mL
	30 mM	0.0843 mL	0.4214 mL	0.8429 mL	2.1072 mL
	40 mM	0.0632 mL	0.3161 mL	0.6322 mL	1.5804 mL
	50 mM	0.0506 mL	0.2529 mL	0.5057 mL	1.2643 mL
	60 mM	0.0421 mL	0.2107 mL	0.4214 mL	1.0536 mL
	80 mM	0.0316 mL	0.1580 mL	0.3161 mL	0.7902 mL

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Spiperone

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Neuronal Signaling Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

FDA-Approved Drug Library

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Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Spiperone

All Dopamine Receptor Isoforms

All 5-HT Receptor Isoforms

All Wnt Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Spiperone Related Classifications

HY-B1371 Related Classifications