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

Spiperone hydrochloride  (Synonyms: Spiroperidol hydrochloride)

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

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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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)

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)

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].

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].

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.
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)

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
10 mM 0.2315 mL 1.1576 mL 2.3152 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.10%

References
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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.

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Spiperone hydrochloride
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