Fluphenazine dimaleate

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CAS NO:

3093-66-1

氟奋乃静马来酸氢盐

Fluphenazine dimaleate 是一种有效且具有口服活性的吩噻嗪类多巴胺受体 (dopamine receptor)拮抗剂。Fluphenazine dimaleate 阻断神经元电压门控的钠离子通道 (sodium channels)。Fluphenazine dimaleate 主要通过拮抗中边缘、黑质纹状体和下颌结节神经通路的突触后多巴胺-2 受体来发挥作用。Fluphenazine dimaleate 可拮抗苯甲酸甲酯诱导的小鼠刻板咬伤，抑制小鼠攀爬行为。Fluphenazine dimaleate 可用于研究精神病以及与糖尿病相关的疼痛性周围神经病变，并有抑制SARS-CoV-2的潜力。

生物活性

Fluphenazine dimaleate is a potent, orally active phenothiazine-baseddopamine receptorantagonist. Fluphenazine dimaleate blocks neuronal voltage-gatedsodium channels. Fluphenazine dimaleate acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dimaleate can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dimaleate can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibitSARS-CoV-2^[1]^[2]^[3]^[4]^[6].

IC₅₀& Target

Dopamine receptor, Sodium channels, SARS-CoV-2^[1]^[2]

体内研究
(In Vivo)

Fluphenazine (1 mg/kg; IG, treated from day 6 to day 15 of gestation) causes malformations in pregnant mice^[5].
Fluphenazine (0.125-1 mg/kg; IP, single dosage) antagonizes Methylphenidate-induced stereotyped gnawing; inhibits significantly climbing behaviour^[6].

Animal Model:	Mature female Swiss-Webster mice^[5]
Dosage:	1 mg/kg
Administration:	IG, treated from day 6 to day 15 of gestation
Result:	Significantly reduced fetal weight and length, increased the incidence of incomplete ossification of sternebrae and skull bones.

Animal Model:	Mice (injected with 60 mg/kg Methylphenidate)^[6]
Dosage:	0.125, 0.25, 0.5, and 1 mg/kg
Administration:	IP, single dosage
Result:	Antagonized Methylphenidate-induced stereotyped gnawing; inhibited significantly climbing behaviour in mice at 0.0625-0.5 mg/kg, and at the dose of 1 mg/kg abolished this effect completely.

Clinical Trial

分子量

669.67

Formula

C₃₀H₃₄F₃N₃O₉S

CAS 号

3093-66-1

中文名称

氟奋乃静马来酸氢盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.