生物活性 靶点 体外研究 体内研究
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螺哌隆盐酸盐

螺哌隆盐酸盐,2022-29-9,结构式
螺哌隆盐酸盐
  • CAS号:2022-29-9
  • 英文名:Spiroperidol Hydrochloride
  • 中文名:螺哌隆盐酸盐
  • CBNumber:CB33110644
  • 分子式:C23H27ClFN3O2
  • 分子量:431.94
  • MOL File:2022-29-9.mol
螺哌隆盐酸盐化学性质
  • 储存条件 :Store at RT
  • 溶解度 :Soluble to 100 mM in DMSO
  • 形态 :Powder

螺哌隆盐酸盐性质、用途与生产工艺

  • 生物活性 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 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。
  • 靶点

    D 2 Receptor

    0.06 nM (Ki)

    D 1 Receptor

    ~350 nM (Ki)

    D 3 Receptor

    0.6 nM (Ki)

    D 4 Receptor

    0.08 nM (Ki)

    D 5 Receptor

    ~3500 nM (Ki)

    5-HT 2A Receptor

    1 nM (Ki)

    5-HT 1A Receptor

    49 nM (Ki)

    α1B-adrenoceptor

    Calcium-activated chloride channel

  • 体外研究

    Spiperone is a potent intracellular Ca 2+ enhancer (EC 50 =9.3 μM) and stimulates intracellular Ca 2+ 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.

  • 体内研究

    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.

    Animal Model: C57Bl/6 mice (7-8-week-old) induced pulmonary fibrosis by Bleomycin
    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.
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