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Fluphenazine dihydrochloride
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。
Fluphenazine dihydrochloride图片
CAS NO:146-56-5
包装与价格:
包装价格(元)
100mg电议
500mg电议

产品介绍
Fluphenazine dihydrochloride 是吩噻嗪类 D1DR 和 D2DR 抑制剂;在探索这种常用多巴胺拮抗剂的作用和代谢命运的研究中,用于将氟奋乃静输送到生物系统。
Cas No.146-56-5
别名盐酸氟奋乃静
化学名2-(4-(3-(2-(trifluoromethyl)-10H-phenothiazin-10-yl)propyl)piperazin-1-yl)ethanol dihydrochloride
Canonical SMILESFC(F)(F)C1=CC(N(C2=CC=CC=C2S3)CCCN4CCN(CCO)CC4)=C3C=C1.Cl.Cl
分子式C22H28Cl2F3N3OS
分子量510.44
溶解度DMF: 30 mg/ml,DMSO: 20 mg/ml,Ethanol: 5 mg/ml
储存条件Store at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

EC50: 1.24 μM

Fluphenazine is a dopamine D1 and D2 receptor inhibitor.

Dopamine D1 and D2 receptor immunohistochemistry has been used to study the structure of the adult rat arcuate-median eminence complex, particularly in relation to the tubero-infundibular dopamine neurons.

In vitro: Previous study showed that both phenothiazines of fluphenazine and perphenazine induced concentration-dependent loss in cell viability with EC50s to be 1.24 and 2.76 μM for fluphenazine and perphenazine, respectively. Moreover, fluphenazine at 1.0 μM and perphenazine at 1.0 and 3.0 μM could inhibit melanogenesis and decrease the content of microphthalmia-associated transcription factor. In addition, both fluphenazine and perphenazine at higher concentrations caused depletion of melanocytes antioxidant status, indicating oxidative stress induction [1].

In vivo: Systemic fluphenazine could effectively attenuate mechanical allodynia in rat neuropathic pain models at 0.03-0.3 mg/kg doses, which approximated those used in rodent models of psychosis. For antiallodynic effect, fluphenazine was able to effectively suppress the ectopic discharges in injured afferent fibers without affecting the propagation of action potentials in an ex-vivo DRG-nerve preparation from CCI rats [2].

Clinical trial: Fluphenazine, which is sold under the brand names Prolixin, is clinically used as an antipsychotic medication in the treatment of chronic psychoses such as schizophrenia. In addition, fluphenazine is about equal in effectiveness to low-potency antipsychotics (https://en.wikipedia.org/wiki/Fluphenazine).

References:
[1] Otreba M et al.  Fluphenazine and perphenazine impact on melanogenesis and antioxidant enzymes activity in normal human melanocytes. Acta Poloniae Pharmaceutica-Drug Research, July-August 2016, 73(4):903-911.
[2] Dong XW,Jia Y,Lu SX,Zhou X,Cohen-Williams M,Hodgson R,Li H,Priestley T.  The antipsychotic drug, fluphenazine, effectively reverses mechanical allodynia in rat models of neuropathic pain. Psychopharmacology (Berl). 2008 Jan;195(4):559-68.