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氟司必林

氟司必林用途

Fluspirilene是L型钙通道的非竞争性拮抗剂,IC50为0.03 μM。Fluspirileneis是一种用于精神分裂症的长效可注射抗精神病药物。

氟司必林名称

[ CAS 号 ]:
1841-19-6

[ 中文名 ]:
帕罗西汀杂质C

[ 英文名 ]:
fluspirilene

[中文别名 ]:

[英文别名 ]:

fluspirilene

氟司必林生物活性

[ 描述 ]:

Fluspirilene是L型钙通道的非竞争性拮抗剂,IC50为0.03 μM。Fluspirileneis是一种用于精神分裂症的长效可注射抗精神病药物。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

研究领域 >> 神经疾病

[ 靶点 ]

IC50: 0.03 μM (L-type calcium channel)[1]

[体外研究]

Fluspirilene,在非竞争性改变二氢吡啶结合的浓度下,选择性地拮抗钙通道激活剂的作用[1]。 Fluspirilene以剂量依赖性方式降低活力并抑制胶质瘤干细胞系的球形成。 Fluspirilene在1.25,2.5和5μM时显示抑制T98,U87和所有GSC系的增殖,而在2.5和5μM时抑制U251和SNB19的增殖[2]。

[体内研究]

用fluspirilene治疗的小鼠显示出肿瘤大小的显着减少。 Fluspirilene显着延长了TGS04小鼠模型的存活[2]。

[细胞实验]

为了研究fluspirilene对细胞增殖的影响，用1.25,2.5和5μM的fluspirilene处理细胞。使用细胞计数试剂盒-8 [2]评估GSC活力。

[动物实验]

小鼠[2]将小鼠随机分成两组，用fluspirilene（n = 5）或用DMSO作为对照组（n = 5）治疗。所有小鼠肌内注射200μLDMSO或溶于DMSO的氟苯吡胺，剂量为1 mg / kg体重4次[2]。

[参考文献]

[1]. Kenny BA, et al. Selective antagonism of calcium channel activators by fluspirilene. Br J Pharmacol. 1990 Jun;100(2):211-6.

[2]. Dong Y, et al. Identification of antipsychotic drug fluspirilene as a potential anti-glioma stem cell drug. Oncotarget. 2017 Dec 4;8(67):111728-111741.

[相关活性小分子]

氟司必林物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
668.9±55.0 °C at 760 mmHg

[ 熔点 ]:
187.5-190°

[ 分子式 ]:
C₂₉H₃₁F₂N₃O

[ 分子量 ]:
475.573

[ 闪点 ]:
358.3±31.5 °C

[ 精确质量 ]:
475.243530

[ PSA ]:
35.58000

[ LogP ]:
3.89

[ 外观性状 ]:
amorphous solid | white to yellow

[ 蒸汽压 ]:
0.0±2.0 mmHg at 25°C

[ 折射率 ]:
1.632

[ 储存条件 ]:
room temp

[ 水溶解性 ]:
DMSO: soluble

氟司必林MSDS

氟司必林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XX8750000

CHEMICAL NAME :: 1,3,8-Triazaspiro(4.5)decan-4-one, 8-(4,4-bis(p-fluorophenyl)butyl)-1-phenyl-

CAS REGISTRY NUMBER :: 1841-19-6

BEILSTEIN REFERENCE NO. :: 0633853

LAST UPDATED :: 199612

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C29-H31-F2-N3-O

MOLECULAR WEIGHT :: 475.63

WISWESSER LINE NOTATION :: T6N DXTJ A3YR DF&R DF& D-& CT5MVXN EHJ DR

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 183 ug/kg

TOXIC EFFECTS :: Skin and Appendages - corrosive (after topical exposure)

REFERENCE :: BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 1,523,1979

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >146 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 20,1689,1970

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 106 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity)

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 20,1689,1970

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >37 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 20,1689,1970

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: >80 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 20,1689,1970

氟司必林安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
UN 3249

[ WGK德国 ]:
3

[ RTECS号 ]:
XX8750000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2933990090

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氟司必林海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

氟司必林文献

Small molecule regulators of autophagy identified by an image-based high-throughput screen.

Proc. Natl. Acad. Sci. U. S. A. 104 , 19023-8, (2007)

Autophagy is a lysosome-dependent cellular catabolic mechanism mediating the turnover of intracellular organelles and long-lived proteins. Reduction of autophagy activity has been shown to lead to the...

Determination of fluspirilene in human plasma by liquid chromatography-tandem mass spectrometry with electrospray ionisation.

J. Chromatogr. A. 828(1-2) , 219-27, (1998)

An ultra-sensitive method for the determination of fluspirilene in plasma was established, using high-performance liquid chromatographic separation with tandem mass spectrometric detection. The sample...

Test therapy in the treatment of generalized anxiety disorders with low dose fluspirilene.

Prog. Neuropsychopharmacol. Biol. Psychiatry 19(6) , 1049-60, (1995)

1. The present double-blind study was designed to determine under three different conditions (0.5 mg, 1.0 mg, 1.5 mg per week) whether response or non-response within a two-week test-therapy predicts ...

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