Pipamperone
(Synonyms: 酰胺哌啶酮,Floropipamide; McN-JR 3345; R 3345) 目录号 : GC36924
Pipamperone (Floropipamide; McN-JR 3345; R 3345) 是 5-HT2A 受体 (pKi=8.2) 和 D4 受体 (pKi=8.0) 的高亲和力拮抗剂。Pipamperone (Floropipamide; McN-JR 3345; R 3345) 是 D2 受体 (pKi=6.7) 的低亲和力拮抗剂。
Cas No.:1893-33-0
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
Pipamperone (Floropipamide; McN-JR 3345; R 3345) is a high-affinity antagonist of 5-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0) and a low-affinity antagonist of D2 receptor (pKi=6.7)[1]. 5-HT2A Receptor|8.2 (pKi)|5-HT2C Receptor|6.9 (pKi)|5-HT1 Receptor|5.7 (pKi)|D4 receptor|8.0 (pKi)|D2 receptor|6.7 (pKi)|α1 receptor|7.2 (pKi)
[1]. Erik Buntinx, MD, et al. Selective Serotonergic Properties of Low-Dose Pipamperone May Enhance Antidepressant Effect: Preclinical Evidence.
| Cas No. | 1893-33-0 | SDF | |
| 别名 | 酰胺哌啶酮,Floropipamide; McN-JR 3345; R 3345 | ||
| Canonical SMILES | O=C(C1(N2CCCCC2)CCN(CCCC(C3=CC=C(F)C=C3)=O)CC1)N | ||
| 分子式 | C21H30FN3O2 | 分子量 | 375.48 |
| 溶解度 | 0.1 M HCL: 25 mg/mL (66.58 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 | 2.6633 mL | 13.3163 mL | 26.6326 mL |
| 5 mM | 0.5327 mL | 2.6633 mL | 5.3265 mL |
| 10 mM | 0.2663 mL | 1.3316 mL | 2.6633 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。
Pipamperone Population Pharmacokinetics Related to Effectiveness and Side Effects in Children and Adolescents
Clin Pharmacokinet 2020 Nov;59(11):1393-1405.PMID:32394297DOI:10.1007/s40262-020-00894-y.
Background: Pipamperone is a frequently prescribed antipsychotic in children and adolescents in the Netherlands, Belgium, and Germany. However, pediatric pharmacokinetics and the relationship with side effects and efficacy are unknown. Currently, divergent pediatric dosing recommendations exist. Objectives: The objective of this study was to describe the population pharmacokinetics of Pipamperone in children and adolescents; to correlate measured and predicted Pipamperone trough concentrations and predicted 24-h area under the curves with effectiveness, extrapyramidal symptoms, and sedation; and to propose dose recommendations based on simulations. Methods: Pipamperone concentrations were collected from Dutch pediatric patients in a prospective naturalistic trial (n = 8), and German pediatric patients in a therapeutic drug monitoring service (n = 22). A total of 70 Pipamperone concentrations were used to develop a population pharmacokinetic model with non-linear mixed-effects modeling (NONMEM®). Additionally, an additional random sample of 21 German patients with 33 Pipamperone concentrations from the same therapeutic drug monitoring service was used for external validation. Pharmacokinetic parameters were related to clinical improvement, sedation, and extrapyramidal symptoms. Simulations were performed to determine optimal dosages. Results: In a one-compartment model, the apparent volume of distribution was 416 L/70 kg and the apparent clearance was 22.1 L/h/70 kg. Allometric scaling was used to correct for differences in bodyweight. The model was successfully externally validated. The median [25th-75th percentile] measured Pipamperone trough concentrations were numerically higher in responders (98.0 µg/L [56.0-180.5 µg/L]) than in non-responders (58.0 µg/L [14.9-105.5 µg/L]), although non-significant (p = 0.14). A twice-daily 0.6-mg/kg dosage was better than a fixed dosage to attain the concentration range observed in responders. Conclusions: Our findings suggest that Pipamperone therapeutic reference ranges may be lower for children with behavioral problems than recommended for adults with psychotic symptoms (100-400 µg/L). When dosing Pipamperone in children and adolescents, bodyweight should be taken into account.
Pipamperone and delirium: a preliminary evaluation of its effectiveness in the management of delirium and its subtypes
Swiss Med Wkly 2017 Jul 24;147:w14471.PMID:28750419DOI:10.4414/smw.2017.14471.
Introduction: Delirium has been recognised as an underdiagnosed and undermanaged syndrome with substantial prevalence rates and potentially deleterious consequences in the medically ill population. Despite its frequent administration in the management of delirium, the effectiveness of Pipamperone has not yet been evaluated. Methods: In this retrospective, descriptive cohort study of 192 patients, Pipamperone as monotherapy and as an adjunct to haloperidol, haloperidol alone, or atypical antipsychotics were compared with respect to their effectiveness in the management of delirium and its subtypes over the course of 20 days. Results: In this elderly patient population, Pipamperone alone and as an adjunct to haloperidol was as effective as haloperidol or atypical antipsychotics in the management of delirium. Management with low-dose Pipamperone monotherapy achieved delirium resolution in 70% of patients, over a mean of 6.4 (2-20) days. With Pipamperone as an adjunct to haloperidol, delirium resolved in 59% of patients, over a mean of 7.4 (2-20) days. When haloperidol or atypical antipsychotics (risperidone, olanzapine or quetiapine) were used, the delirium resolution rates were 72 and 67%, over a mean of 5.2 (2-11) and 6.4 (2-20) days, respectively. The addition of Pipamperone to haloperidol decreased the requirement for lorazepam. Pipamperone proved to be equally effective in all delirium subtypes - hypoactive, hyperactive and mixed. Nonetheless, potential bias could not be excluded in this observational design. Conclusion: From these initial results, low-dose Pipamperone was as effective as haloperidol or atypical antipsychotics in the management of delirium and its subtypes, and was benzodiazepine-sparing when used as an adjunct to haloperidol.
[Overdosing of Pipamperone from a squeeze bottle]
Ned Tijdschr Geneeskd 2018;162:D2160.PMID:29543144doi
Background: Medication is not always delivered in a safe dosing format. Up to 33% of medication errors can be attributed to confusing packaging or labelling. Case description: A 6-year-old boy with ADHD, for which he was being treated with methylphenidate and Pipamperone drops, was brought to the A&E department with signs of severe encephalopathy. He had apparently been given Pipamperone in streams rather than in drops in the previous months. The Pipamperone level in his blood was raised to toxic levels. The Pipamperone drops were delivered in a plastic squeeze bottle (LDPE bottle), which makes correct dosing almost impossible. The treating psychiatrist and the prescribing GP had not noticed this medication error. The incident was reported to the Netherlands Pharmacovigilance Centre Lareb, the Netherlands Medicines Evaluation Board and the Portal for Patient Safety. A warning was also added to the Netherlands paediatric medication prescription website about Pipamperone in a squeeze bottle. Conclusion: Drug packaging can be a cause of intoxication. The treatment provider should be aware of this in cases of drug intoxication.
Pipamperone (Dipiperon, R3345) in troublesome mental retardates: a double-blind placebo controlled cross-over study with long-term follow-up
Acta Psychiatr Scand 1975 Oct;52(4):237-45.PMID:1103575DOI:10.1111/j.1600-0447.1975.tb00039.x.
A 6-week double-blind cross-over study comparing Pipamperone with placebo was conducted in 20 female mental retardates with behavioural disorders. The ages of the patients ranged between 22 and 42 years. After a 2-week washout period, patients were randomly allocated to either Pipamperone or placebo treatment. The initial dosage of Pipamperone was 40 mg b.i.d., which was gradually increased to 80 mg b.i.d. within 5 days. Patients were assessed using a ten-item rating scale before and after each week of treatment. For six of the ten items, patients showed a better response during the Pipamperone than during the placebo period. When pre-trial scores were compared with those at the end of the trial, seven items had significantly improved with Pipamperone. The nursing staff considered the patients more alert and amenable during Pipamperone treatment.
[Pipamperone and the treatment of impulsive aggressive behaviour]
Tijdschr Psychiatr 2008;50(3):179-83.PMID:18324605doi
Background: Pipamperone is prescribed to prevent impulsive aggressive behaviour in patients with intermittent explosive disorder, personality disorders or mental retardation. Aim: To investigate the scientific basis of this treatment. Method: Various databases were searched using the terms 'pipamperon', 'Pipamperone' and 'Dipiperon'. Located articles were reviewed in order to discover whether they dealt with the relationship between the drug and impulsiveness and aggression. results Six publications were found, all dating from before 1979. Conclusion: In view of the limited amount of research on the subject and the adverse side effects it is concluded that Pipamperone is not the drug of first choice considering the treatment of impulsive aggressive behaviour.