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Merck
CN

F100

Sigma-Aldrich

氟司必林

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别名:
8-[4,4-双(p-氟苯)丁基]-1-苯基-1,3,8-三氮杂螺[4.5]癸-4-酮, R 6218
经验公式(希尔记法):
C29H31F2N3O
CAS号:
分子量:
475.57
EC 号:
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

检测方案

≥98% (HPLC)

形式

solid

颜色

white

溶解性

DMSO: ≥20 mg/mL
H2O: insoluble
ethanol: soluble

创始人

Johnson & Johnson

储存温度

room temp

SMILES字符串

Fc1ccc(cc1)C(CCCN2CCC3(CC2)N(CNC3=O)c4ccccc4)c5ccc(F)cc5

InChI

1S/C29H31F2N3O/c30-24-12-8-22(9-13-24)27(23-10-14-25(31)15-11-23)7-4-18-33-19-16-29(17-20-33)28(35)32-21-34(29)26-5-2-1-3-6-26/h1-3,5-6,8-15,27H,4,7,16-21H2,(H,32,35)

InChI key

QOYHHIBFXOOADH-UHFFFAOYSA-N

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应用

氟司必林已用于研究其作为神经安定药物对人ether-a-go-go相关基因(HERG)的影响。
氟司必林已用于研究其对恶性神经胶质瘤的细胞毒性作用。

生化/生理作用

氟司必林(Fluspirilene)是一种多巴胺受体拮抗剂。也可充当钙通道阻断剂。氟司必林是一种抗精神病药物,具有精神安定作用。对胶质母细胞瘤和精神分裂症有治疗作用。
氟司必林可抑制周期蛋白依赖性激酶2(CDK2)的活性。可作为抗癌药有效治疗人肝细胞癌。

特点和优势

该化合物由 Johnson & Johnson 开发。浏览其他由制药公司开发的化合物以及批准药物/候选药物清单, 请单击此处

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

Eyeshields, Gloves, type N95 (US)


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Inhibition of P-type and N-type calcium channels by dopamine receptor antagonists.
Sah, DW and Bean, Bruce P
Molecular Pharmacology, 45(1), 84-92 (1994)
Qin Cao et al.
Nature chemistry (2018-10-10)
Inhibiting the interaction between amyloid-β (Aβ) and a neuronal cell surface receptor, LilrB2, has been suggested as a potential route for treating Alzheimer's disease. Supporting this approach, Alzheimer's-like symptoms are reduced in mouse models following genetic depletion of the LilrB2
Identification of antipsychotic drug fluspirilene as a potential anti-glioma stem cell drug
Dong Y, et al.
Oncotarget, 8(67), 111728-111728 (2017)
In silico identification and in vitro and in vivo validation of anti-psychotic drug fluspirilene as a potential CDK2 inhibitor and a candidate anti-cancer drug
Shi XN, et al.
PLoS ONE, 10(7), e1753-e1753 (2015)
D W Sah et al.
Molecular pharmacology, 45(1), 84-92 (1994-01-01)
P-type Ca2+ channels in cerebellar Purkinje neurons and N-type Ca2+ channels in sympathetic neurons were found to be inhibited by D2 dopamine receptor antagonists with diverse structures, including phenothiazines (chlorpromazine and thioridazine), diphenylbutylpiperidines (fluspirilene and pimozide), butyrophenones (haloperidol and spiperone)

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