螺哌隆盐酸盐
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- CAS号:
- 2022-29-9
- 英文名:
- Spiroperidol Hydrochloride
- 英文别名:
- Spiroperidol Hydrochloride
- 中文名:
- 螺哌隆盐酸盐
- 中文别名:
- 盐酸螺哌隆;螺哌隆盐酸盐;化合物 T23381
- CBNumber:
- CB33110644
- 分子式:
- C23H27ClFN3O2
- 分子量:
- 431.94
- MOL File:
- 2022-29-9.mol
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螺哌隆盐酸盐化学性质
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储存条件:
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Store at RT
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溶解度:
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Soluble to 100 mM in DMSO
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形态:
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Powder
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螺哌隆盐酸盐性质、用途与生产工艺
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。
D
2
Receptor
0.06 nM (Ki)
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D
1
Receptor
~350 nM (Ki)
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D
3
Receptor
0.6 nM (Ki)
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D
4
Receptor
0.08 nM (Ki)
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D
5
Receptor
~3500 nM (Ki)
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5-HT
2A
Receptor
1 nM (Ki)
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5-HT
1A
Receptor
49 nM (Ki)
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α1B-adrenoceptor
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Calcium-activated chloride channel
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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
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in Calu-3 and CFBE41o
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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.
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:
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C57Bl/6 mice (7-8-week-old) induced pulmonary fibrosis by Bleomycin
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Dosage:
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1.5 mg/kg
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Administration:
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Intraperitoneal injection; on days 1, 3, 6, 7, and 13-21
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Result:
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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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螺哌隆盐酸盐
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2022-29-9, 螺哌隆盐酸盐 相关搜索:
- 药靶配体
- 化合物 T23381
- 盐酸螺哌隆
- 螺哌隆盐酸盐
- 2022-29-9
- Spiroperidol Hydrochloride