Benperidol
(Synonyms: 苯哌利多) 目录号 : GC64702
Benperidol 是一种比较古老的抗精神病药物。Benperidol 是一种苯丁酮类抗精神病药，在阻断 D2 受体方面具有最高的安定药效。
Cas No.:2062-84-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Benperidol is a relatively old antipsychotic drug. Benperidol is a butyrophenone antipsychotic, with the highest neuroleptic potency in terms of D2 receptor blockade[1].
[1]. Leucht S, et al. Benperidol for schizophrenia. Cochrane Database Syst Rev. 2005;2005(2):CD003083.
| Cas No. | 2062-84-2 | SDF | Download SDF |
| 别名 | 苯哌利多 | ||
| 分子式 | C22H24FN3O2 | 分子量 | 381.44 |
| 溶解度 | DMSO : 100 mg/mL (262.16 mM; Need ultrasonic) | 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 | 2.6216 mL | 13.1082 mL | 26.2164 mL |
| 5 mM | 0.5243 mL | 2.6216 mL | 5.2433 mL |
| 10 mM | 0.2622 mL | 1.3108 mL | 2.6216 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。
Benperidol for schizophrenia
Cochrane Database Syst Rev 2002;(1):CD003083.PMID:11869652DOI:10.1002/14651858.CD003083.
Background: Benperidol is a relatively old antipsychotic drug, marketed since 1966, used in Germany for 30 years, but also available in Belgium, Greece, Italy, the Netherlands and the UK. Benperidol is a butyrophenone antipsychotic, with the highest neuroleptic potency in terms of D2 receptor blockade. Those taking it are, therefore, reputed to be at high risk of extrapyramidal side effects, but Benperidol's unusual profile may render it of value to subgroups of people with schizophrenia. Objectives: To examine the clinical effects and safety of Benperidol for those with schizophrenia and schizophrenia-like psychoses. Search strategy: The reviewers searched the Cochrane Schizophrenia Group's register (January 2001) which includes relevant randomised controlled trials from the bibliographic databases Biological Abstracts, CINAHL, The Cochrane Library, EMBASE, MEDLINE, PsycLIT, LILACS, PSYNDEX, Sociological Abstracts and Sociofile. We also searched the references of all included studies and contacted pharmaceutical companies and authors of included studies in order to identify further trials. Selection criteria: Randomised controlled trials that compared Benperidol with other treatments for people with schizophrenia and/or schizophrenia-like psychoses. Data collection and analysis: Citations and, where possible, abstracts were independently inspected by two reviewers and papers were ordered, re-inspected and quality assessed. We independently extracted data but excluded data if loss to follow up was greater than 50%. For homogeneous dichotomous data, we calculated the relative risk (RR), the 95% confidence interval (CI) and, where appropriate, the number needed to treat/harm (NNT/H), on an intention-to-treat basis. Main results: We identified only one unpublished poorly randomised controlled trial (N=40, duration 30 days, comparison perphenazine). Although Benperidol was inferior to perphenazine (1 RCT, N=40, global state no better or worse RR 8.0 CI 2.1 to 30, NNH 1.4 CI 1 to 2) poor reporting suggests that an overestimate of effect is likely. It was not possible to report other outcomes. Reviewer's conclusions: Currently, there are insufficient data from randomised trials to assess the clinical effects of Benperidol. This interesting compound merits further research.
Benperidol for schizophrenia
Cochrane Database Syst Rev 2005 Apr 18;2005(2):CD003083.PMID:15846648DOI:10.1002/14651858.CD003083.pub2.
Background: Benperidol is a relatively old antipsychotic drug that has been marketed since 1966. It has been used in Germany for 30 years, but is also available in Belgium, Greece, Italy, the Netherlands and the UK. Benperidol is a butyrophenone antipsychotic, with the highest neuroleptic potency in terms of D2 receptor blockade. Those taking it are therefore reputed to be at high risk of extrapyramidal side effects, but Benperidol's unusual profile may render it valuable to subgroups of people with schizophrenia. Objectives: To examine the clinical effects and safety of Benperidol for those with schizophrenia and schizophrenia-like psychoses. Search strategy: We searched the Cochrane Schizophrenia Group's register (November 2004) for this update. Selection criteria: We included all randomised controlled trials that compared Benperidol with other treatments for people with schizophrenia, or schizophrenia-like psychoses. Data collection and analysis: We reliably selected studies, quality rated them and extracted data. We independently extracted data but excluded data if loss to follow up was greater than 50%. For dichotomous data, we estimated relative risks (RR), with the 95% confidence intervals (CI). Where possible, we calculated the number needed to treat/harm statistic (NNT/H) and used intention-to-treat analysis. Main results: The update yielded no further studies for inclusion in the review. We identified only one unpublished poorly randomised controlled trial (N=40, duration 30 days, comparison perphenazine). Although Benperidol was inferior to perphenazine (1 RCT, N=40, global state no better or worse RR 8.0 CI 2.1 to 30, NNH 1.4 CI 1 to 2) poor reporting suggests that an overestimate of effect is likely. It was not possible to report other outcomes. Authors' conclusions: Currently, there are insufficient data from randomised trials to assess the clinical effects of Benperidol. This compound merits further research interest.
Influence of intravenous administration of the antipsychotic drug Benperidol on the QT interval
Neuropsychiatr 2017 Dec;31(4):172-175.PMID:28791627DOI:10.1007/s40211-017-0230-5.
A group effect is generally assumed regarding the prolongation of the QT interval through butyrophenone antipsychotics like haloperidol. Consequently intravenous administration of Benperidol is seen critically notwithstanding sparse evidence; thus Benperidol and haloperidol were compared regarding their cardiac risk of prolonging the QT interval when administered intravenously for acute sedation of psychotic patients. The QT interval was measured by a 12-lead ECG. For the correction of QT values Bazett's formula was used. The resulting QTc intervals of the Benperidol and the haloperidol group were compared using Mann-Whitney U-test. Our data provide statistical evidence for Benperidol being less prone to cause QTc prolongation than haloperidol (p = 0.049). The results of our study indicate a more favourable risk profile of Benperidol compared to haloperidol regarding QTc prolongation when administered intravenously.
Determination of Benperidol and its reduced metabolite in human plasma by high-performance liquid chromatography and electrochemical detection
J Chromatogr 1991 Apr 19;565(1-2):363-73.PMID:1874880DOI:10.1016/0378-4347(91)80397-u.
An isocratic high-performance liquid chromatographic method with electrochemical detection for the quantification of Benperidol and its suggested reduced metabolite TVX Q 5402 in human plasma is described. The method included a two-step solid-phase extraction on reversed-phase and cation-exchange material, followed by separation on a cyanopropyl silica gel column (5 microns; 250 mm x 4.6 mm I.D.). The eluent was 0.15 M acetate buffer (pH 4.7) containing 25% acetonitrile (w/w). Spiperone served as internal standard. The inclusion of the cation-exchange step provided sample purity higher than those achieved with other methods. After extraction of 1 ml of plasma, concentrations as low as 0.5 ng/ml were detectable for both Benperidol and the metabolite. In plasma samples collected from a schizophrenic patient treated with a single oral dose of 6 mg of Benperidol, plasma levels of Benperidol and of the metabolite could be measured from 20 min to at least 12 h after administration.
Electrochemical detection of Benperidol in serum for drug monitoring in humans
Ther Drug Monit 1987 Sep;9(3):343-6.PMID:3672579DOI:10.1097/00007691-198709000-00015.
A high-pressure liquid chromatographic (HPLC) method for the serum assay of Benperidol is described. One ml of serum is required for a single estimation. The method involves a simple and rapid extraction step (BondElut columns), HPLC separation (C8 10-mu column), and electrochemical detection (+0.65 V). Haloperidol is used as internal standard. On the basis of this procedure, recovery (93-97%) and reproducibility (intra-assay and inter-assay coefficients of variation less than 9%) are satisfactory. The detection limit is 0.2 ng/ml of serum. After therapeutic doses, trough serum levels ranged from 3.8 to 12 ng/ml in five patients.