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)

目录号: HY-B1371A

Spiperone hydrochloride (Spiroperidol hydrochloride) 是一种选择性的多巴胺 D2 受体 (D2,D3,D4,D1 和 D5 受体的 Ki 值分别为 0.06 nM,0.6 nM,0.08 nM,~350 nM,~3500 nM) 和 5-HT2A/5-HT1A 受体 (Ki 为1 nM/49 nM) 拮抗剂。Spiperone hydrochloride 也是一种选择性的 α1B-肾上腺素受体 (α1B-adrenoceptor) 拮抗剂。Spiperone hydrochloride 激活钙激活的氯离子通道 (CaCC)。抗精神病和抗炎作用。

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Spiperone hydrochloride Chemical Structure

Spiperone hydrochloride Chemical Structure

CAS No. : 2022-29-9

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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[1][2][3][4][5].

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

D2 Receptor

0.06 nM (Ki)

D1 Receptor

~350 nM (Ki)

D3 Receptor

0.6 nM (Ki)

D4 Receptor

0.08 nM (Ki)

D5 Receptor

~3500 nM (Ki)

5-HT2A Receptor

1 nM (Ki)

5-HT1A Receptor

49 nM (Ki)



Calcium-activated chloride channel


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











Room temperature in continental US; may vary elsewhere.


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

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


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Spiperone hydrochloride