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
- 储存条件 :Store at RT
- 溶解度 :Soluble to 100 mM in DMSO
- 形态 :Powder
- 颜色 :White to off-white
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。
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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
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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.
- 公司名称:TOCRIS-US
- 联系电话:--
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- 国家:英国
- 产品数:5726
- 优势度:77