Azaphen
(Synonyms: 阿扎吩,Azafen; Pipofezin hydrochloride; Pipofezine hydrochloride) 目录号 : GC35443
Pipofezine(Azafen,Azaphen)是5-羟色胺重吸收抑制剂。
Cas No.:24853-80-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Pipofezine(Azafen or Azaphen) is a potent inhibitor of the reuptake of serotonin. IC50 Value: Target: SSRIsPipofezine is a tricyclic antidepressant (TCA) approved in Russia for the treatment of depression. In addition to its antidepressant action, pipofezine has sedative effects as well, indicating antihistamine activity.
[1]. Domestic antidepressants. 1. Azaphen By Andreeva, N. I.; Asnina, V. V.; Liberman, S. S. From Pharmaceutical Chemistry Journal (Translation of Khimiko-Farmatsevticheskii Zhurnal) (2000), 34(5), 237-241. [2]. Shinaev NN, Akzhigitov RG. Azaphen: a return to clinical practice.Zh Nevrol Psikhiatr Im S S Korsakova. 2005;105(10):55-6. [3]. Ignatowicz L, Ignatowicz R, Wdowiak MW, Jaremko A. Azaphen in the treatment of enuresis in children.Psychiatr Pol. 1977 Jan-Feb;11(1):29-33. [4]. Liberman SS, Sharova SA. A comparison of the effect of the tricyclic antidepressants azaphen and imizin on the gastrointestinal tracts of experimental animals.Farmakol Toksikol. 1975 Jan-Feb;38(1):29-32. [5]. Misurec J, NÁhunek K, KamenickÁ V, Chmelar M. Proceedings: Influence of azaphen, a new antidepressive drug, on the human EEG. Act Nerv Super (Praha). 1974;16(4):245-6.
| Cas No. | 24853-80-3 | SDF | |
| 别名 | 阿扎吩,Azafen; Pipofezin hydrochloride; Pipofezine hydrochloride | ||
| Canonical SMILES | [H]Cl.[H]Cl.CN1C2=CC=CC=C2OC3=C1C=C(N4CCN(C)CC4)N=N3 | ||
| 分子式 | C16H21Cl2N5O | 分子量 | 370.28 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| 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 | 2.7007 mL | 13.5033 mL | 27.0066 mL |
| 5 mM | 0.5401 mL | 2.7007 mL | 5.4013 mL |
| 10 mM | 0.2701 mL | 1.3503 mL | 2.7007 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。
[A new approach to overcoming the drug resistance of the causative agents of malaria]
Med Parazitol (Mosk) 1990 Sep-Oct;(5):18-21.PMID:2266896doi
Progressively expanding area of multiresistant falciparum malaria and the profile of its resistance to drugs successively implemented into practice necessitate the elaboration of approaches to the "revival" of the drugs used. As with neoplastic cells, a correlation between plasmodium multiresistance with increased "outflow" of specific drugs from the cell is suggested, which is blocked by inhibition of Ca2+ transport. Reversion of resistance to chloroquine by a combination with Ca2+ channel blockers verapamil, tricyclic antidepressants (desipramine, protritreline, etc.), tricyclic antihistamine drugs (cyproheptadine), and reversion of resistance to sulfadoxine in combination with the antihistamine drug ketodiphene have been shown in vivo and in vitro. The function of Ca2+ channels is directly related to Ca2(+)-, Mg2(+)-dependent ATPase. Ph-metric techniques elaborated in the USSR make it possible to evaluate its activity, determine the inhibitors, differentiate them according to the effect. The authors have established reversion of P. berghei resistance to chloroquine, with the tricyclic antidepressants Azaphen, aminazin, triftazin correlating with the degree of Ca2+, Mg2(+)-ATPase inhibition and to praziquantel, whose effect might be associated with the increased permeability of the cellular membrane to Ca2+. The inhibitors of Ca2+ transport have various parasitocidal activities which might be accounted for by the deficiency of this cation necessary for plasmodium development. The task is to elaborate safe optimum antimalarial drug/modulator of Ca2+ transport combinations. Multiresistance (genetically predetermined multifactorial cellular changes) may be associated with enhanced synthesis of transmembrane glycoprotein with varying molecular mass depending on the direction of resistance.
[Differential psychopharmacotherapy of heart rhythm disorders]
Kardiologiia 1987 May;27(5):48-52.PMID:3656892doi
Antiarrhythmic activity of psychotropic agents, such as phenibut, eglonyl, Azaphen, grandaxin, fali-lepsin, is demonstrated for the first time ever in patients with paroxysmal supraventricular tachycardia, atrial fibrillation and ventricular extrasystole. It is dependent on the nature of the underlying heart disease, the psychopathologic syndrome and vegetative cardiac rhythm regulation type. Different trends of cardiac and hemodynamic change are produced by different psychopharmacologic agents. Differential long-term intermittent psychopharmacotherapy is proposed for the control of heart rhythm disorders.
[Atypical antidepressants: effect on synaptosomal uptake of serotonin and GABA]
Biull Eksp Biol Med 1981 Nov;92(11):564-6.PMID:7198493doi
Effect of the antidepressants of different chemical groups--imipramine, desmethylimipramine, chlorimipramine, befuralin, trazodon, pyrazidol, inkasan and azaphen--on the uptake of 3H-serotonin and 3H-GABA by the crude synaptosomal fraction of the rat brain was studied. The Cm values for the uptake of serotonin and GABA were 0.195 and 30 micro M, respectively. Inkasan and Azaphen were the most potent inhibitors of the 3H-serotonin uptake (65-70% inhibition at a concentration of 50 micro M. Azaphen and chlorimipramine were the only ones to inhibit the uptake of 3H-GABA at a concentration of 50 micro M. The majority of the antidepressants studied inhibited the GABA uptake only at high concentrations.
5-Hydroxytryptamine activates a 5-HT/c-Myc/SLC6A4 signaling loop in non-small cell lung cancer
Biochim Biophys Acta Gen Subj 2022 Apr;1866(4):130093.PMID:35066124DOI:10.1016/j.bbagen.2022.130093.
Purpose: Psychological stress is a crucial driver of tumorigenesis and cancer metastasis. The impact of the stress-associated neurotransmitter 5-hydroxytryptamine (5-HT) on tumor progression is poorly understood. We aimed to identify the role of 5-HT in the pathogenesis of non-small cell lung cancer (NSCLC) and to identify innovative therapeutic strategies. Methods: The expression of 5-HT and related signaling molecules was assessed by immunohistochemistry and ELISA in tumor tissues from 30 NSCLC patients. The tumorigenic potential and migrative properties of NSCLC A549 cells were examined by colony-formation and Transwell assays. Western blotting and immunofluorescence staining to evaluate protein expression in NSCLC cells and tumor tissues were performed. Patient survival information was downloaded from the Cancer Genome Atlas (TCGA) database to assess the impact of c-Myc/SLC6A4/5-HT signaling on NSCLC development. Results: Patients with metastatic NSCLC had increased 5-HT expression in NSCLC tissues. In vitro 5-HT pretreatment significantly strengthened the tumorigenic and metastatic potential of A549 cells. Mechanistically, 5-HT promoted the activity of the transcription factor c-Myc in a tribbles pseudokinase 3 (TRIB3)-dependent manner, and c-Myc upregulated the expression of the 5-HT transporter SCL6A4, thereby promoting 5-HT uptake in A549 cells and forming a 5-HT/c-Myc/SLC6A4/5-HT feedback loop. Azaphen dihydrochloride monohydrate-induced suppression of 5-HT uptake decreased the tumorigenic potential and suppressed distant metastasis of NSCLC cells in vivo. Conclusions: 5-HT signaling is essential for NSCLC development, and 5-HT uptake inhibitors potentially have therapeutic value in the treatment of NSCLC patients.
[Anticalcium activity of several antidepressive agents]
Biull Eksp Biol Med 1992 May;113(5):502-4.PMID:1421269doi
In experiments in white mice and rats the antidepressants pyrazidol (pirlindole), moclobemide and especially tetrindole possess anticalcium activity in tests of calcium chloride-induced lethality in mice and arrhythmia in rats. Tetrindole is as active as verapamil. Imipramine, Azaphen and incazane were not active in these experiments. In vitro on isolated intestinal segments of guinea-pigs tetrindole exerts anticalcium action, but in less degree than verapamil. In all probability the anticalcium activity of tetrindole may play some role in the mechanism of action of this compound on the central nervous system.