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Bifeprunox
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Bifeprunox图片
CAS NO:350992-10-8
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
Bifeprunox 是有效的多巴胺D25-HT1A受体部分激动剂,对皮质 5-HT1A 和纹状体 D2 的pKi分别为 7.19 和 8.83,对海马 5-HT1A 的pEC50为 6.37。Bifeprunox 作为一种抗精神病剂,可用于精神分裂症的研究。
生物活性

Bifeprunox is a potentdopamine D2-like and5-HT1A receptorpartial agonist withpKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and apEC50of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox is an antipsychotic for the research of schizophrenia[1][2].

IC50& Target[2]

5-HT1AReceptor

7.19 (pKi, cortex)

D2Receptor

8.83 (pKi, striatum)

5-HT1AReceptor

6.37 (pEC50, hippocampus)

体外研究
(In Vitro)

Bifeprunox has a pKiof 8 at h5-HT1A receptors, with an Emaxof 70%[1].

体内研究
(In Vivo)

Bifeprunox (0.001-2.5 mg/kg) reduces marble burying in mice[2].
Bifeprunox (4-250 μg/kg) influences nicotine-seeking behaviour in response to drug-associated stimuli in rats[3].

Animal Model:Male NMRI mice (weighing 20-22 g)[2]
Dosage:0.001, 0.0025, 0.01, 0.04, 0.16, 0.63, and 2.5 mg/kg
Administration:I.p.
Result:Reduced marble burying. Potently active from 0.0025 mg/kg.
Animal Model:Naive male Wistar rats (weighing 250-275 g)[3]
Dosage:4, 16, 64 and 250 μg/kg
Administration:Injected s.c. 30 minutes before testing
Result:4-16 μg/kg dose-dependently attenuated the responsereinstating effects of nicotine-associated cues. Higher doses (64-250 μg/kg, s.c.) reduced spontaneous locomotor activity and suppressed operant responding induced by sucrose-associated cues and by the primary reinforcing properties of nicotine or sucrose.
Clinical Trial
分子量

385.46

Formula

C24H23N3O2

CAS 号

350992-10-8

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.