F100
氟司必林
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
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关于此项目
经验公式（希尔记法）:
C29H31F2N3O
化学文摘社编号:
分子量:
475.57
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
EC Number:
217-418-6
MDL number:
InChI key
QOYHHIBFXOOADH-UHFFFAOYSA-N
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)
SMILES string
Fc1ccc(cc1)C(CCCN2CCC3(CC2)N(CNC3=O)c4ccccc4)c5ccc(F)cc5
assay
≥98% (HPLC)
form
solid
color
white
solubility
DMSO: ≥20 mg/mL
H2O: insoluble
ethanol: soluble
originator
Johnson & Johnson
storage temp.
room temp
Quality Level
Gene Information
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)
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Application
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。
Biochem/physiol Actions
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。
Features and Benefits
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。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
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)
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)
J P Galizzi et al.
Proceedings of the National Academy of Sciences of the United States of America, 83(19), 7513-7517 (1986-10-01)
[3H]Fluspirilene, a neuroleptic molecule of the diphenylbutylpiperidine series, binds to skeletal muscle transverse tubule membranes with a high affinity corresponding to a Kd of 0.11 +/- 0.04 nM, A 1:1 stoichiometry was found between [3H]fluspirilene binding and the binding of
The pharmacology of fluspirilene (R 6218), a potent, long-acting and injectable neuroleptic drug.
P A Janssen et al.
Arzneimittel-Forschung, 20(11), 1689-1698 (1970-11-01)
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)
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