Reduced Haloperidol
(Synonyms: 还原氟哌啶醇) 目录号 : GC44810
An active metobolite of haloperidol
Cas No.:34104-67-1
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
Reduced haloperidol is an active metabolite of haloperidol . It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (Kis = 1.4 and 31 nM, respectively) and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells. It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake (Kis = 21, 25, and 33 μM, respectively, in COS-7 cells expressing the human transporters). Reduced haloperidol (0.5 mg/kg) increases latency to paw withdrawal in mouse models of capsaicin- but not force-induced mechanical hypersensitivity.
| Cas No. | 34104-67-1 | SDF | |
| 别名 | 还原氟哌啶醇 | ||
| Canonical SMILES | OC1(CCN(CCCC(C2=CC=C(F)C=C2)O)CC1)C3=CC=C(Cl)C=C3 | ||
| 分子式 | C21H25ClFNO2 | 分子量 | 377.9 |
| 溶解度 | Dichloromethane: slightly soluble,Methanol: slightly soluble | 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 | 2.6462 mL | 13.231 mL | 26.462 mL |
| 5 mM | 0.5292 mL | 2.6462 mL | 5.2924 mL |
| 10 mM | 0.2646 mL | 1.3231 mL | 2.6462 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。
Pharmacokinetics of haloperidol
Clin Pharmacokinet 1989 Dec;17(6):396-423.PMID:2689040DOI:10.2165/00003088-198917060-00004.
Haloperidol has been used extensively for the treatment of psychotic disorders, and it has been suggested that the monitoring of plasma haloperidol concentration is clinically useful. Different assay methodologies have been used in research and clinical practice to examine the relationship between response and plasma concentration of the drug. Chemical assays such as high pressure liquid chromatography (HPLC) and gas-liquid chromatography (GLC) have good precision and sensitivity; radioimmunoassay (RIA) is generally more sensitive, but less precise and specific. Radioreceptor assay quantifies dopaminereceptor blocking activity but does not provide results comparable with those of HPLC, GLC and RIA. Large doses of haloperidol can safely be given intravenously and intramuscularly for rapid neuroleptisation; the bioavailability of this agent administered orally ranges from 60 to 65%. However, there is large interindividual, but not intraindividual, variability in plasma haloperidol concentrations and most pharmacokinetic parameters. This interindividual variability could be partially explained by the reversible oxidation/reduction metabolic pathway of haloperidol: it is metabolised via reduction to Reduced Haloperidol, which is biologically inactive. Different extents of enterohepatic recycling, and ethnic differences in metabolism, could also account for the observed variability in haloperidol disposition. Although not conclusive from different clinical studies, it appears that a plasma haloperidol concentration range of 4 micrograms/L to an upper limit of 20 to 25 micrograms/L produces therapeutic response. The role of Reduced Haloperidol in determining clinical response is not clear, although in some studies a high Reduced Haloperidol/haloperidol concentration ratio has been suggested to be associated with therapeutic failure. Measurements of red blood cell or cerebrospinal fluid haloperidol concentration have also been proposed as determinants of therapeutic response, but results from different studies are inconsistent, and do not seem to provide a significant advantage over plasma concentration monitoring. Physiological parameters such as prolactin and homovanillic acid levels have been evaluated, with the latter showing some promise that warrants further investigation. Haloperidol decanoate can be characterised by a flip-flop pharmacokinetic model because its absorption rate constant is slower than the elimination rate constant. Its plasma concentration peaks on day 7 after intramuscular injection. The elimination half-life is about 3 weeks, and the time to steady-state is about 3 months.
Reduced Haloperidol: a factor in determining the therapeutic benefit of haloperidol treatment?
Psychopharmacology (Berl) 1992;106(3):289-96.PMID:1570373DOI:10.1007/BF02245407.
One of the metabolic pathways of haloperidol (HAL) is the reduction of the molecule at the benzylic ketone to form an alcohol metabolite, known as reduced HAL (RHAL). The basic and clinical pharmacology of RHAL is the subject of this review. The investigation of RHAL in biological samples has been suggested to be important, as the reduced metabolite can be reconverted back to the parent drug and is shown to be 20-50% as potent as HAL in some in vivo neuroleptic tests. Nevertheless, the metabolic reduction/oxidation cycle of the drug is unbalanced. The interconversion process largely favours the reduction of HAL to RHAL but not vice versa. The RHAL/HAL ratios are dose and time dependent. The higher the dose or the longer the duration of treatment, the greater the ratio. The results concerning relationship between plasma RHAL level or RHAL/HAL ratio and clinical response are inconsistent, yet interesting. Some studies in schizophrenic patients have suggested a diminished therapeutic response to HAL when elevated plasma RHAL concentrations or RHAL/HAL ratios are presented. However, this finding has not been replicated by other investigations. Possible interference by RHAL with HAL at dopamine receptors thus reducing the effectiveness of HAL treatment has been suggested by some authors. Measurements of RHAL as well as HAL plasma concentrations for evaluating drug level-clinical response might be necessary in psychiatric patients.
Haloperidol and Reduced Haloperidol plasma levels in Chinese vs. non-Chinese psychiatric patients
Psychiatry Res 1989 Oct;30(1):45-52.PMID:2594870DOI:10.1016/0165-1781(89)90170-4.
Haloperidol and Reduced Haloperidol plasma concentrations were measured in age-matched Chinese and non-Chinese patients (n = 32). Steady-state plasma concentrations were obtained 10-12 hours after the bedtime dose. Haloperidol and Reduced Haloperidol concentrations were measured by liquid chromatography and radioimmunoassay. Haloperidol plasma concentrations did not significantly differ between the populations, but Reduced Haloperidol levels were 3 times greater in non-Chinese patients than in Chinese patients. The incidence of extrapyramidal side effects was higher in Chinese patients (18 vs. 10), while non-Chinese patients with extrapyramidal symptoms had higher Reduced Haloperidol plasma levels. Logistic regression analysis revealed that ethnicity and Reduced Haloperidol/haloperidol ratios were important variables in predicting extrapyramidal symptoms. These results suggest that the metabolism and disposition of haloperidol and Reduced Haloperidol could differ among ethnic populations.
Reduced Haloperidol/haloperidol ratio and clinical outcome in schizophrenia: preliminary evidences
Prog Neuropsychopharmacol Biol Psychiatry 1988;12(5):689-94.PMID:3222450DOI:10.1016/0278-5846(88)90013-9.
1. The possible influence of haloperidol and its metabolite plasma levels on clinical outcome in schizophrenic patients was evaluated. 2. 18 schizophrenic inpatients diagnosed according to DSM III, were treated with conventional haloperidol p.o. for four weeks. 3. Plasma levels of haloperidol and its reduced metabolite were measured by mass-spectrometry assay. Clinical outcome was evaluated by BPRS. 4. Cluster analysis only considering BPRS improvement and Reduced Haloperidol/haloperidol ratio was able to discriminate two groups of patients: one of non responders and the other of responders. The former group presented higher ratios than the latter. 5. Reduced Haloperidol/haloperidol ratio could be considered as a good marker for prediction of the clinical outcome.
Reduced Haloperidol in the post-mortem brains of haloperidol-treated patients
Psychiatry Res 1984 Mar;11(3):259-69.PMID:6587418DOI:10.1016/0165-1781(84)90074-x.
We measured the concentrations of haloperidol and its reduced alcohol metabolite in human post-mortem tissues with high-performance/liquid chromatography using electrochemical detection. Both haloperidol and Reduced Haloperidol were detected and quantified in the occipital cortex of nine schizophrenic patients with a history of haloperidol treatment, but not in six samples from nontreated subjects. Reduced Haloperidol concentrations were below the detection limit of the assay in several tissues of rats and mice even after 10 days of haloperidol treatment. The results suggest that Reduced Haloperidol is present in the brains of haloperidol-treated patients at slightly higher concentrations than haloperidol itself. Further studies are warranted to establish the possible biological importance of this haloperidol metabolite.