Art. -Nr.: HY-B1371A

Spiperone hydrochloride

(Synonyms: Spiroperidol hydrochloride)

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D₂ receptor (K_i values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D₂, D₃, D₄, D₁ and D₅ receptors, respectively) and 5-HT_2A/5-HT_1A receptor (K_is of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities.

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Reinheit: 99.0%
CAS. Nr.: 2022-29-9
Formel: C₂₃H₂₇ClFN₃O₂
Molecular Weight:431.93

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Spiperone hydrochloride Chemical Structure

CAS. Nr.: 2022-29-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]^[4]

D₂ Receptor

0.06 nM (Ki)

D₃ Receptor

D₄ Receptor

5-HT_2A Receptor

1 nM (Ki)

5-HT_1A Receptor

49 nM (Ki)

α1B-adrenoceptor

Calcium-activated chloride channel

D₁ Receptor

~350 nM (Ki)

D₃ Receptor

0.6 nM (Ki)

D₄ Receptor

0.08 nM (Ki)

D₅ Receptor

~3500 nM (Ki)

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen :

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	0.31 μM Compound: Spiperone HCl	Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis	[PMID: 32631561]

In Vitro

Spiperone is a potent intracellular Ca²⁺ enhancer (EC₅₀=9.3 μM) and stimulates intracellular Ca²⁺ through a protein tyrosine kinase-coupled phospholipase C-dependent pathway, which results in increased secretion of Cl^- in Calu-3 and CFBE41o^- cell monolayers^[2].
Spiperone significantly decreases the production of nitric oxide in lipopolysaccharide-stimulated BV-2 microglia cells, primary microglia and primary astrocyte cultures. Spiperone also significantly inhibits nitric oxide production in ATP-stimulated primary microglia cultures. Spiperone markedly decreases the production of TNF-α in BV-2 microglia cells. Spiperone attenuates the expression of inducible nitric oxide synthase and proinflammatory cytokines such as IL-1β and TNF-α at mRNA levels in BV-2 microglia cells^[3].

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

In Vivo

Spiperone (1.5 mg/kg; intraperitoneal injection; on days 1, 3, 6, 7, and 13-21; C57Bl/6 mice) treatment reduces infiltration of the alveolar interstitium and alveolar ducts with inflammatory cells and prevents the growth of the connective tissue in the parenchyma of Bleomycin lungs^[6].

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

Animal Model:

C57Bl/6 mice (7-8-week-old) induced pulmonary fibrosis by Bleomycin^[6]
Dosage:

1.5 mg/kg
Administration:

Intraperitoneal injection; on days 1, 3, 6, 7, and 13-21
Result:

Reduced infiltration of the alveolar interstitium and alveolar ducts with inflammatory cells and prevented the growth of the connective tissue in the parenchyma of bleomycin lungs.

Chemical Information

CAS. Nr. 2022-29-9
Appearance Solid
Molecular Weight 431.93
Formel C₂₃H₂₇ClFN₃O₂
Color White to off-white
SMILES

O=C1NCN(C2=CC=CC=C2)C13CCN(CCCC(C4=CC=C(F)C=C4)=O)CC3.[H]Cl
Synonyms

Spiroperidol hydrochloride
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (231.52 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

2.3152 mL

11.5759 mL

23.1519 mL

5 mM

0.4630 mL

2.3152 mL

4.6304 mL

10 mM

0.2315 mL

1.1576 mL

2.3152 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 2.08 mg/mL (4.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (4.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)

Verweise

[1]. P Seeman, et al. Dopamine receptor pharmacology. Trends Pharmacol Sci. 1994 Jul;15(7):264-70. [Content Brief]

[2]. Lihua Liang, et al. Spiperone, identified through compound screening, activates calcium-dependent chloride secretion in the airway. Am J Physiol Cell Physiol. 2009 Jan;296(1):C131-41. [Content Brief]

[3]. Long Tai Zheng, et al. The antipsychotic spiperone attenuates inflammatory response in cultured microglia via the reduction of proinflammatory cytokine expression and nitric oxide production. J Neurochem. 2008 Dec;107(5):1225-35. [Content Brief]

[4]. Richard A Glennon, et al. Ketanserin and spiperone as templates for novel serotonin 5-HT(2A) antagonists. Curr Top Med Chem. 2002 Jun;2(6):539-58. [Content Brief]

[5]. Andrea E Errasti, et al. Human umbilical vein vasoconstriction induced by epinephrine acting on alpha1B-adrenoceptor subtype. Am J Obstet Gynecol. 2003 Nov;189(5):1472-80. [Content Brief]

[6]. E G Skurikhin, et al. Effect of spiperone on mesenchymal multipotent stromal and hemopoietic stem cells under conditions of pulmonary fibrosis. Bull Exp Biol Med. 2014 May;157(1):132-7. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3152 mL	11.5760 mL	23.1519 mL	57.8798 mL
	5 mM	0.4630 mL	2.3152 mL	4.6304 mL	11.5760 mL
	10 mM	0.2315 mL	1.1576 mL	2.3152 mL	5.7880 mL
	15 mM	0.1543 mL	0.7717 mL	1.5435 mL	3.8587 mL
	20 mM	0.1158 mL	0.5788 mL	1.1576 mL	2.8940 mL
	25 mM	0.0926 mL	0.4630 mL	0.9261 mL	2.3152 mL
	30 mM	0.0772 mL	0.3859 mL	0.7717 mL	1.9293 mL
	40 mM	0.0579 mL	0.2894 mL	0.5788 mL	1.4470 mL
	50 mM	0.0463 mL	0.2315 mL	0.4630 mL	1.1576 mL
	60 mM	0.0386 mL	0.1929 mL	0.3859 mL	0.9647 mL
	80 mM	0.0289 mL	0.1447 mL	0.2894 mL	0.7235 mL
	100 mM	0.0232 mL	0.1158 mL	0.2315 mL	0.5788 mL

Keywords

Spiperone hydrochloride

3 Cited Publications

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Spiperone hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Spiperone hydrochloride

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Spiperone hydrochloride Related Classifications

HY-B1371A Related Classifications