Spiperone

SKU:BHB21902689
Research Validated
Overview
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Spiperone (CAS 749-02-0) is an antagonist supplied as a solid. Reported to act on 5-HT 1A Receptor, 5-HT 2A Receptor. Relevant to GPCR/G Protein and Neuronal Signaling research. Molecular formula C23H26FN3O2, molecular weight 395.47 g/mol.
Purity 99.58%
CAS Number 749-02-0
Molecular Weight 395.47 g/mol
Form Solid
Target 5-HT 1A Receptor, 5-HT 2A Receptor
Storage Powder -20°C; in solvent -80°C
Options selector
Catalog no. Size
HY-B1371-5MG 5 mg
HY-B1371-10MG 10 mg
HY-B1371-25MG 25 mg
HY-B1371-50MG 50 mg
HY-B1371-100MG 100 mg
HY-B1371-200MG 200 mg
HY-B1371-500MG 500 mg
HY-B1371-1MLX10MM 1 mL x 10 mM (in DMSO)
Available Options

Select the variant that best fits your experiment. Availability and lead time may vary by option.

  • Options: Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 mL x 10 mM (in DMSO)
  • Lead time: varies by selected option.
  • Storage: Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
  • Shipping: Room temperature in continental US; may vary elsewhere.
  • Upon receipt: transfer to -20°C as soon as possible.
Field Specification
Target 5-HT 1A Receptor, 5-HT 2A Receptor
Alternative names Spiroperidol
CAS no. 749-02-0
Applications
  • Functional Assay (In Vitro)
Molecular weight 395.47
Molecular formula C23H26FN3O2
Purity 99.58%
SMILES O=C1NCN(C2=CC=CC=C2)C13CCN(CCCC(C4=CC=C(F)C=C4)=O)CC3
Form Solid
Storage Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
Shipping Room temperature in continental US; may vary elsewhere.
Catalog no. (Mfr.) HY-B1371
Main SKU BHB21902689
Antagonists

Compound Overview

Spiperone, also known as Spiroperidol, is a potent antagonist of dopamine D2, serotonin 5-HT1A, and serotonin 5-HT2A receptors, and it also serves as a labelled ligand for neuroleptic receptors. It enhances intracellular calcium levels and inhibits the Wnt signaling pathway, giving it potential for neurology disease research[1][2][3][4]. It is supplied as an off-white to light yellow solid (C23H26FN3O2, MW 395.47) at 99.58% purity.

Physical & Chemical Properties

CAS Number 749-02-0
Molecular Formula C23H26FN3O2
Molecular Weight 395.47 g/mol
Purity 99.58%
Appearance Solid
Color Off-white to light yellow
SMILES O=C1NCN(C2=CC=CC=C2)C13CCN(CCCC(C4=CC=C(F)C=C4)=O)CC3
Target 5-HT 1A Receptor, 5-HT 2A Receptor
Signaling Pathway GPCR/G Protein; Neuronal Signaling; Stem Cell/Wnt
Solubility In Vitro: DMSO: 33.33 mg/mL (84.28 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Storage Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
Shipping Room temperature in continental US; may vary elsewhere.

Literature Cited

Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under 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.

[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.

[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.

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

Safety

For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.

In Vitro

SolventSolubilityNotes
DMSO33.33 mg/mL (84.28 mM)requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility)

Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.

In Vivo

Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.

Protocol 1

Composition10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline
Result≥ 4.55 mg/mL (11.51 mM); clear solution
How to prepareGives a clear solution at ≥ 4.55 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (45.5 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL.

Protocol 2

Composition10% DMSO + 90% Corn Oil
Result≥ 2.5 mg/mL (6.32 mM); clear solution
How to prepareGives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil.

Data provided by the manufacturer.

In Vitro

In HEK293 cells, Spiperone (5 μM, 24 h) selectively blocks Wnt signaling by acting on the Wnt/LRP complex[4]. Spiperone (1-10 μM, 275-470 s) raises intracellular calcium levels in HEK293 cells[4].

Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.

Q.Why is there no price on some sizes?
A.Availability and lead time for those sizes are confirmed on inquiry. Send us the size you need and we will come back with price and lead time.
Q.Can this be used in humans or for diagnostics?
A.No. This product is supplied For Research Use Only. It is not for diagnostic or therapeutic procedures and not for human or veterinary use.

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Molecular and pharmacological characterization of the dopamine receptors in the oriental fruit fly, Bactrocera dorsalis. Insect Biochem Mol Biol 2025 May:180:104312. PMID: 40245998

Survey of Dopamine Receptor D2 Antagonists as Retinal Antifibrotics. J Ocul Pharmacol Ther 2024 Oct;40(8):536-542. PMID: 39206555

bioRxiv. 2026 Apr 1.

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