Piperacetazine
(Synonyms: 乙酰哌普嗪) 目录号 : GC33670
A typical antipsychotic
Cas No.:3819-00-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Piperacetazine is a typical antipsychotic.1 It inhibits spontaneous motor activity and responding for food in rats, as well as potentiates hexobarbital-induced narcosis in mice. It also inhibits lysosome acidification, as well as viral entry (IC50 = <8.5 ?M), in Ebola-infected Huh7 cells.2 Formulations containing piperacetazine have been used in the treatment of schizophrenia.
1.Pitman-MoorePiperacetazine (Quide tablets)Clin. Pharmacol. Ther.10(5)749-754(1969) 2.Dyall, J., Nelson, E.A., DeWald, L.E., et al.Identification of combinations of approved drugs with synergistic activity against Ebola virus in cell culturesJ. Infect. Dis.218(Suppl 5)S672-S678(2018)
| Cas No. | 3819-00-9 | SDF | |
| 别名 | 乙酰哌普嗪 | ||
| Canonical SMILES | CC(C(C=C1N2CCCN3CCC(CCO)CC3)=CC=C1SC4=C2C=CC=C4)=O | ||
| 分子式 | C24H30N2O2S | 分子量 | 410.57 |
| 溶解度 | DMSO : ≥ 6 mg/mL (14.61 mM) | 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 | 2.4356 mL | 12.1782 mL | 24.3564 mL |
| 5 mM | 0.4871 mL | 2.4356 mL | 4.8713 mL |
| 10 mM | 0.2436 mL | 1.2178 mL | 2.4356 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。
Chlorpromazine versus Piperacetazine for schizophrenia
Cochrane Database Syst Rev 2018 Oct 31;10(10):CD011709.PMID:30378678DOI:10.1002/14651858.CD011709.pub2.
Background: Schizophrenia is a severe mental disorder with a prevalence of about 1% among the general population. It is listed among the top 10 causes of disability-adjusted life years (DALYs) worldwide. Antipsychotics are the mainstay treatment. Piperacetazine has been reported to be as clinically effective as chlorpromazine, a well established 'benchmark' antipsychotic, for people with schizophrenia. However, the side effect profiles of these antipsychotics differ and it is important that an evidence base is available comparing the benefits, and potential harms of these two antipsychotics. Objectives: To assess the clinical and side effects of chlorpromazine for people with schizophrenia and schizophrenia-like psychoses in comparison with Piperacetazine. Search methods: We searched the Cochrane Schizophrenia Group's Trials Register (6 June 2015 and 8 October 2018) which is based on regular searches of CINAHL, CENTRAL, BIOSIS, AMED, Embase, PubMed, MEDLINE, PsycINFO and registries of clinical trials. There are no language, date, document type, or publication status limitations for inclusion of records in the register. Selection criteria: We included randomised controlled trials (RCTs) focusing on chlorpromazine versus Piperacetazine for people with schizophrenia, reporting useable data. Data collection and analysis: We extracted data independently. For binary outcomes, we calculated risk ratio (RR) and its 95% confidence interval (CI), on an intention-to-treat basis. For continuous data, we estimated the mean difference (MD) between groups and its 95% CI. We employed a fixed-effect model for analyses. We assessed risk of bias for included studies and created 'Summary of findings' tables using GRADE. Main results: We found 12 records referring to six trials. We included five trials, all from the 1970s, randomising 343 participants. We excluded one trial. The overall methodology and data reporting by the trials was poor. Only short-term data were available.Results from the included trials found that, in terms of global state improvement, when rated by a psychiatrist, there was no clear difference between chlorpromazine and Piperacetazine (RR 0.90, 95% CI 0.80 to 1.02; participants = 208; studies = 2; very low-quality evidence). One trial reported change scores on the mental state scale Brief Psychiatric Rating Scale (BPRS); no clear difference was observed (MD -0.40, 95% CI -1.41 to 0.61; participants = 182; studies = 1; very low-quality evidence). Chlorpromazine appears no worse or better than Piperacetazine regarding adverse effects. In both treatment groups, around 60% of participants experienced some sort of adverse effect (RR 1.00, 95% CI 0.75 to 1.33; participants = 74; studies = 3; very low-quality evidence), with approximately 40% of these participants experiencing some parkinsonism-type movement disorder (RR 0.95, CI 0.61 to 1.49; participants = 106; studies = 3; very low-quality evidence). No clear difference in numbers of participants leaving the study early for any reason was observed (RR 0.50, 95% CI 0.10 to 2.56; participants = 256; studies = 4; very low-quality evidence). No trial reported data for change in negative symptoms or economic costs. Authors' conclusions: The results of this review show chlorpromazine and Piperacetazine may have similar clinical efficacy, but data are based on very small numbers of participants and the evidence is very low quality. We can not make firm conclusions based on such data. Currently, should clinicians and people with schizophrenia need to choose between chlorpromazine and Piperacetazine they should be aware there is no good quality evidence to base decisions. More high quality research is needed.
Piperacetazine versus thioridazine in the treatment of organic brain disease: a controlled double-blind study
J Am Geriatr Soc 1976 Aug;24(8):355-8.PMID:7588DOI:10.1111/j.1532-5415.1976.tb03311.x.
In a double-blind cross-over study, 50 geriatric patients with organic brain disease were divided into two groups. One group first received Piperacetazine for 15 days and then thioridazine for 15 days. For the other group the sequence was reversed. Piperacetazine proved to be at least as effective as thioridazine and seemed to be more effective against certain target symptoms; side effects were less common and less severe.
High dosage Piperacetazine (Quide) in ambulatory schizophrenic patients--therapeutic efficacy and toxicity
Dis Nerv Syst 1974 May;35(5):231-6.PMID:17894106doi
Indications for high dosage neuroleptics have become increasingly more debatable with recent emphasis on outpatient community management of the severely ill schizophrenic patient. Early studies suggest that high dose neuroleptics have greater effectiveness with some schizophrenic patients while remaining low in toxicity. As part of a rater blind study, 16 patients with the diagnosis of either chronic undifferentiated or chronic paranoid schizophrenia were placed on standard dose Piperacetazine following a washout period. The dosage was then gradually increased until the patient achieved maximal effect with a minimum of side effects. Eight patients required standard dose (25-160 mg/day) while the remaining eight required high dose (160-400 mg/day). The two clinical groups are compared for therapeutic efficacy and toxicity. High dose Piperacetazine was found to be effective in seven patients refractory to low dosage. Although the incidence of side effects was higher with the high dose patients, toxicity (liver, blood, renal) was not increased in patients requiring high dose medication. Indications for high dose neuroleptics are briefly discussed.
Drug Repurposing Screen for Compounds Inhibiting the Cytopathic Effect of SARS-CoV-2
bioRxiv 2020 Aug 18;2020.08.18.255877.PMID:32839771DOI:10.1101/2020.08.18.255877.
Drug repurposing is a rapid approach to identifying therapeutics for the treatment of emerging infectious diseases such as COVID-19. To address the urgent need for treatment options, we carried out a quantitative high-throughput screen using a SARS-CoV-2 cytopathic assay with a compound collection of 8,810 approved and investigational drugs, mechanism-based bioactive compounds, and natural products. Three hundred and nineteen compounds with anti-SARS-CoV-2 activities were identified and confirmed, including 91 approved drug and 49 investigational drugs. Among these confirmed compounds, the anti-SARS-CoV-2 activities of 230 compounds, including 38 approved drugs, have not been previously reported. Chlorprothixene, methotrimeprazine, and Piperacetazine were the three most potent FDA approved drugs with anti-SARS-CoV-2 activities. These three compounds have not been previously reported to have anti-SARS-CoV-2 activities, although their antiviral activities against SARS-CoV and Ebola virus have been reported. These results demonstrate that this comprehensive data set of drug repurposing screen for SARS-CoV-2 is useful for drug repurposing efforts including design of new drug combinations for clinical trials.
Drug Repurposing Screen for Compounds Inhibiting the Cytopathic Effect of SARS-CoV-2
Front Pharmacol 2021 Jan 25;11:592737.PMID:33708112DOI:10.3389/fphar.2020.592737.
Drug repurposing is a rapid approach to identify therapeutics for the treatment of emerging infectious diseases such as COVID-19. To address the urgent need for treatment options, we carried out a quantitative high-throughput screen using a SARS-CoV-2 cytopathic assay with a compound collection of 8,810 approved and investigational drugs, mechanism-based bioactive compounds, and natural products. Three hundred and nineteen compounds with anti-SARS-CoV-2 activities were identified and confirmed, including 91 approved drugs and 49 investigational drugs. The anti-SARS-CoV-2 activities of 230 of these confirmed compounds, of which 38 are approved drugs, have not been previously reported. Chlorprothixene, methotrimeprazine, and Piperacetazine were the three most potent FDA-approved drugs with anti-SARS-CoV-2 activities. These three compounds have not been previously reported to have anti-SARS-CoV-2 activities, although their antiviral activities against SARS-CoV and Ebola virus have been reported. These results demonstrate that this comprehensive data set is a useful resource for drug repurposing efforts, including design of new drug combinations for clinical trials for SARS-CoV-2.