螺哌隆盐酸盐

螺哌隆盐酸盐

中文名称螺哌隆盐酸盐
中文同义词螺哌隆盐酸盐;盐酸螺哌隆;化合物 T23381
英文名称Spiroperidol Hydrochloride
英文同义词Spiroperidol Hydrochloride
CAS号2022-29-9
分子式C23H27ClFN3O2
分子量431.94
EINECS号
相关类别
Mol文件2022-29-9.mol
结构式螺哌隆盐酸盐 结构式

螺哌隆盐酸盐 性质

储存条件Store at RT
溶解度在 DMSO 中溶解度为 100 mM
形态粉末

螺哌隆盐酸盐 用途与合成方法

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)

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

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.

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.

安全信息

MSDS信息

螺哌隆盐酸盐 上下游产品信息

"螺哌隆盐酸盐"相关产品信息
氟司哌隆 8-[4-(4-fluorophenyl)-4-oxobutyl]-1-(2,3,4,5,6-pentadeuteriophenyl)-1,3,8-triazaspiro[4.5]decan-4-one
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