Melperone
(Synonyms: 美哌隆) 目录号 : GC36581
An atypical antipsychotic
Cas No.:3575-80-2
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
Melperone is an atypical antipsychotic.1 It binds to α1- and α2-adrenergic and dopamine D2 receptors (Kds = 180, 150, and 180 nM, respectively), as well as the serotonin (5-HT) receptor subtype 5-HT2A (Kd = 102 nM). It is selective for these receptors over histamine H1, muscarinic, 5-HT1A, 5-HT1D, and 5-HT2C receptors (Kds = 580, >10,000, 2,200, 3,400, and 2,100 nM, respectively). Melperone (2 mg/kg per day) increases basal, but not amphetamine-induced, extracellular dopamine levels in the rat nucleus accumbens.2
1.Richelson, E., and Souder, T.Binding of antipsychotic drugs to human brain receptors: Focus on newer generation compoundsLife Sci.68(1)29-39(2000) 2.Ichikawa, J., and Meltzer, H.Y.The effect of chronic atypical antipsychotic drugs and haloperidol on amphetamine-induced dopamine release in vivoBrain Res.574(1-2)98-104(1992)
| Cas No. | 3575-80-2 | SDF | |
| 别名 | 美哌隆 | ||
| Canonical SMILES | O=C(C1=CC=C(F)C=C1)CCCN2CCC(C)CC2 | ||
| 分子式 | C16H22FNO | 分子量 | 263.35 |
| 溶解度 | DMSO: 41.67 mg/mL (158.23 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 | 3.7972 mL | 18.9861 mL | 37.9723 mL |
| 5 mM | 0.7594 mL | 3.7972 mL | 7.5945 mL |
| 10 mM | 0.3797 mL | 1.8986 mL | 3.7972 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。
Interpretation of Melperone intoxication: post-mortem concentration distribution and interpretation of intoxication data
Drug Metab Pers Ther 2021 Mar 29;36(3):233-237.PMID:34412172DOI:10.1515/dmpt-2020-0181.
Objectives: Since Melperone abuse with lethal intoxication is common, expert opinions based on therapeutical and lethal concentration ranges can be considered as important. Because there is a lack of information about fatalities caused by Melperone mono-intoxications and data on tissue samples with concentration distribution, the aim of this work is the examination of lethal concentration ranges of Melperone and drug quantification in different matrices. Methods: An LC-MS/MS method was applied for analyses performed in blood and tissue samples. Quantification based on standard addition and sample preparation on liquid-liquid extraction with 1-chlorobutane. An appropriate tissue homogenization was performed ahead of extraction with an IKA Ultra-Turrax-Tube-Drive®. A Luna 5 µm C18 (2) 100 Å, 150 × 2 mm analytical column was used for chromatographic separation and the elution was performed with two mobile phases consisted of A (H2O/methanol = 95/5, v/v) and B (H2O/methanol = 3/97, v/v) both with 10 mM ammonium acetate and 0.1% acetic acid. Results: A multi-drug LC-MS/MS analytical method developed was applied successfully for Melperone quantification in different post-mortem matrices. No analytical problems could be identified during method development and analyses of real samples. The Melperone lethal concentration calculated in femoral blood of the drug mono-intoxication investigated was 10 mg/L. Melperone concentration distribution was presented for the first time. Conclusions: The lethal reference concentration of Melperone in femoral blood of 17.1 mg/L pointed out in different reference lists should be used with caution. Instead, a lower lethal Melperone concentration should be considered. The post-mortem concentration distribution of the drug presented could be helpful in the interpretation of cases where no blood samples are available.
Interpretation of Melperone intoxication: post-mortem concentration distribution and interpretation of intoxication data
Drug Metab Pers Ther 2021 Mar 26.PMID:33770824DOI:10.1515/dmdi-2020-0181.
Objectives: Since Melperone abuse with lethal intoxication is common, expert opinions based on therapeutical and lethal concentration ranges can be considered as important. Because there is a lack of information about fatalities caused by Melperone mono-intoxications and data on tissue samples with concentration distribution, the aim of this work is the examination of lethal concentration ranges of Melperone and drug quantification in different matrices. Methods: An LC-MS/MS method was applied for analyses performed in blood and tissue samples. Quantification based on standard addition and sample preparation on liquid-liquid extraction with 1-chlorobutane. An appropriate tissue homogenization was performed ahead of extraction with an IKA Ultra-Turrax-Tube-Drive®. A Luna 5 µm C18 (2) 100 Å, 150 × 2 mm analytical column was used for chromatographic separation and the elution was performed with two mobile phases consisted of A (H2O/methanol = 95/5, v/v) and B (H2O/methanol = 3/97, v/v) both with 10 mM ammonium acetate and 0.1% acetic acid. Results: A multi-drug LC-MS/MS analytical method developed was applied successfully for Melperone quantification in different post-mortem matrices. No analytical problems could be identified during method development and analyses of real samples. The Melperone lethal concentration calculated in femoral blood of the drug mono-intoxication investigated was 10 mg/L. Melperone concentration distribution was presented for the first time. Conclusions: The lethal reference concentration of Melperone in femoral blood of 17.1 mg/L pointed out in different reference lists should be used with caution. Instead, a lower lethal Melperone concentration should be considered. The post-mortem concentration distribution of the drug presented could be helpful in the interpretation of cases where no blood samples are available.
Melperone is an inhibitor of the CYP2D6 catalyzed O-demethylation of venlafaxine
Pharmacopsychiatry 2003 Jan;36(1):3-6.PMID:12649767DOI:10.1055/s-2003-38084.
Introduction: Melperone, a butyrophenone neuroleptic, is frequently used for its sleep-inducing properties. Despite its common use for more than 30 years, it is not yet characterized regarding its effects on cytochrome P450 s (CYPs). In an open pilot study, effects of Melperone on the steady-state blood levels of venlafaxine, a recently introduced serotonin- and noradrenaline reuptake inhibiting antidepressant, were assessed. Methods: The dose-corrected serum concentrations of venlafaxine and O-desmethylvenlafaxine were analyzed retrospectively in a therapeutic drug-monitoring (TDM) database comprising 94 patients. In addition, three patients received venlafaxine and Melperone concomitantly and the serum concentrations of venlafaxine and O-desmethylvenlafaxine were analyzed before, during, and after Melperone co-medication. The effect of Melperone on CYP2D6 was further assessed in seven patients by means of the dextromethorphan O-demethylation, which serves as a CYP2D6 probe reaction. Results: Patients treated concomitantly with venlafaxine and Melperone had significantly higher (mean +/- SD) venlafaxine (3.27 +/- 2.9 vs. 0.97 +/- 0.99 ng/ml per mg/d; p < 0.05) and lower O-desmethylvenlafaxine serum concentrations (0.69 +/- 0.35 vs. 1.51 +/- 0.9 ng/ml per mg/d; p < 0.01) compared to patients without Melperone comedication. In the three patients, venlafaxine serum concentrations increased, on average by 52 % during Melperone co-medication, whereas O-desmethylvenlafaxine was decreased, on average by 29 %. Administration of Melperone over three days elevated the ratio of dextromethorphan to dextrorphan from 0.044 +/- 0.04 to 0.09 +/- 0.083 (p < 0.05). Discussion: This study pointed to an inhibitory effect of Melperone on the O-demethylation of venlafaxine. Because the O-demethylation of venlafaxine is almost exclusively catalyzed by CYP2D6 it is concluded that Melperone is an inhibitor of CYP2D6. The hypothesis was further corroborated by the inhibitory effect of Melperone on the dextromethorphan O-demethylation.
Melperone in treatment-refractory schizophrenia: a case series
Ther Adv Psychopharmacol 2011 Feb;1(1):19-23.PMID:23983923DOI:10.1177/2045125311399800.
Objective: Clozapine is the treatment of choice in refractory schizophrenia, but a substantial proportion of patients experience inadequate response or tolerate the drug poorly. Melperone has been suggested as a possible alternative in such patients. This case series examines the efficacy of Melperone in refractory schizophrenia. Method: All patients prescribed Melperone at the South London and Maudsley NHS Foundation Trust were identified using a pharmacy database. The main outcome was to determine the proportion of patients discharged on Melperone. Results: Three of 21 patients were discharged on Melperone. The primary reason for discontinuation was lack of efficacy. Conclusion: Melperone may be an option in a very few patients with refractory schizophrenia, but it should not be considered as an alternative to clozapine.
Melperone, an aytpical antipsychotic drug with clozapine-like effect on plasma prolactin: contrast with typical neuroleptics
Hum Psychopharmacol 2009 Jul;24(5):415-22.PMID:19551763DOI:10.1002/hup.1036.
Objective: To evaluate the effect of Melperone, a butyrophenone with atypical antipsychotic properties, on plasma prolactin (PRL) concentrations compared with clozapine and typical neuroleptics. Methods: Analysis of pre- and post-treatment PRL levels collected prospectively per protocol in a non-randomized study of 26 melperone-, 76 clozapine-, and 66 neuroleptic-treated patients with schizophrenia or schizoaffective disorder. Cross-sectional analysis of a larger sample of patients with PRL data was also performed. Results: For males, post-treatment PRL levels were significantly higher in the typical neuroleptic group compared with the Melperone (p = 0.0001) and clozapine (p = 0.0001) groups, with no significant difference between clozapine and Melperone. For females, post-treatment PRL levels were significantly higher in the Melperone group as compared to the clozapine group (p = 0.004). There were too few typical neuroleptic-treated females to permit analysis of this sample. However, the cross-sectional analysis of PRL data confirmed the results for melperone- and clozapine-treated females, and showed higher PRL levels in typical neuroleptic-treated females as compared with those who received Melperone and clozapine. Conclusion: Melperone did not significantly increase PRL levels in male patients. However, Melperone and typical neuroleptics caused increase in PRL levels in females. Further study of Melperone's effects on PRL concentration is warranted.