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
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.

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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].

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].

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.

2022-29-9

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

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

SpiperoneSpiroperidolDopamine Receptor5-HT ReceptorAdrenergic ReceptorChloride ChannelSerotonin Receptor5-hydroxytryptamine ReceptorBeta ReceptorCl− Channels5-HT2AantipsychoticD2-receptorα1B-adrenoceptorcalciumanti-inflammatoryneuroprotectivefibrosisInhibitorinhibitorinhibit

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Spiperone hydrochloride
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