Fluphenazine dihydrochloride
(Synonyms: 盐酸氟奋乃静) 目录号 : GC14559
A dopamine D1 and D2 receptor antagonist
Cas No.:146-56-5
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 146-56-5 | SDF | |
| 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 SMILES | FC(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 tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9591 mL | 9.7955 mL | 19.5909 mL |
| 5 mM | 0.3918 mL | 1.9591 mL | 3.9182 mL |
| 10 mM | 0.1959 mL | 0.9795 mL | 1.9591 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet