2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  3. Dopamine Receptor 5-HT Receptor Adrenergic Receptor Chloride Channel
  4. Spiperone hydrochloride

Spiperone hydrochloride  (Synonyms: Spiroperidol hydrochloride)

Cat. No.: HY-B1371A Purity: ≥99.0%
SDS COA Handling Instructions

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Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D2 receptor (Ki 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-HT2A/5-HT1A receptor (Kis 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.

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

Spiperone hydrochloride Chemical Structure

Spiperone hydrochloride Chemical Structure

CAS No. : 2022-29-9

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Other Forms of Spiperone hydrochloride:

Spiperone hydrochloride Related Antibodies

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Description

Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D2 receptor (Ki 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-HT2A/5-HT1A receptor (Kis 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[1][2][3][4][5].

IC50 & Target[1][2][4]

D2 Receptor

0.06 nM (Ki)

D3 Receptor

 

D4 Receptor

 

5-HT2A Receptor

1 nM (Ki)

5-HT1A 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)

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.

Spiperone hydrochloride Related Antibodies
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.
Molecular Weight

431.93

Formula

C23H27ClFN3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (289.40 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 2.3152 mL 11.5759 mL 23.1519 mL
5 mM 0.4630 mL 2.3152 mL 4.6304 mL
View the Complete Stock Solution Preparation Table

* 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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.08 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.

    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: ≥ 2.08 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.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).

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

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

Purity: 99.10%

SDS (252 KB)

COA (250 KB) HNMR (284 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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
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Spiperone hydrochloride Related Classifications

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  • 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:

Spiperone2022-29-9SpiroperidolDopamine Receptor5-HT ReceptorAdrenergic ReceptorChloride ChannelSerotonin Receptor5-hydroxytryptamine ReceptorBeta ReceptorCl− Channels5-HT2AantipsychoticD2-receptorα1B-adrenoceptorcalciumanti-inflammatoryneuroprotectivefibrosisInhibitorinhibitorinhibit

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