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Spiperone hydrochloride

CAS No. : 2022-29-9

MCE 站：Spiperone hydrochloride

产品活性：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 K_i 值分别为 0.06 nM，0.6 nM，0.08 nM，~350 nM，~3500 nM) 和 5-HT_2A/5-HT_1A 受体 (K_i 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。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Membrane Transporter/Ion Channel

作用靶点：Dopamine Receptor  |  5-HT Receptor  |  Adrenergic Receptor  |  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.
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.

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.

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