Pericyazine
(Synonyms: 氰噻嗪,Propericiazine; RP 8909) 目录号 : GC38231
A typical antipsychotic
Cas No.:2622-26-6
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
Periciazine is a typical antipsychotic.1 It binds to the dopamine D1 receptor and androgen receptor (Kis = 0.01 and 3 ?M, respectively).1,2 Periciazine is an α1-adrenergic receptor (α1-AR) antagonist (IC50 = 0.0041 ?M in rat forebrain homogenates), as well as an α2-AR antagonist (IC50 = 2 ?M in rat cortical homogenates).3 It also inhibits severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro) activity by 55% when used at a concentration of 100 ?M.4 Periciazine (0.075 mg/kg) increases the number of entries into, and the percentage of time spent in, the open arms of the elevated plus maze in rats, indicating anxiolytic-like activity.5 Formulations containing periciazine have been used in the treatment of schizophrenia and psychosis.
1.Kanba, S., Suzuki, E., Nomura, S., et al.Affinity of neuroleptics for D1 receptor of human brain striatumJ. Psychiatry Neurosci.19(4)265-269(1994) 2.Bisson, W.H., Cheltsov, A.V., Bruey-Sedano, N., et al.Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugsProc. Natl. Acad. Sci. USA104(29)11927-11932(2007) 3.Megens, A.A.H.P., Leysen, J.E., Awouters, F.H.L., et al.Further validation of in vivo and in vitro pharmacological procedures for assessing the ɑ2/ɑ1-selectivity of test compounds: (1) ɑ-adrenoceptor antagonistsEur. J. Pharmacol.129(1-2)49-55(1986) 4.Ghahremanpour, M.M., Tirado-Rives, J., Deshmukh, M., et al.Identification of 14 known drugs as inhibitors of the main protease of SARS-CoV-2ACS Med. Chem. Lett.11(12)2526-2533(2020) 5.Cechin, E.M., Quevedo, J., Barichello, T., et al.Dose-related effects of propericiazine in ratsBraz. J. Med. Biol. Res.36(2)227-231(2003)
| Cas No. | 2622-26-6 | SDF | |
| 别名 | 氰噻嗪,Propericiazine; RP 8909 | ||
| Canonical SMILES | N#CC(C=C1N2CCCN3CCC(O)CC3)=CC=C1SC4=C2C=CC=C4 | ||
| 分子式 | C21H23N3OS | 分子量 | 365.49 |
| 溶解度 | DMSO: 250 mg/mL (684.01 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 | 2.7361 mL | 13.6803 mL | 27.3605 mL |
| 5 mM | 0.5472 mL | 2.7361 mL | 5.4721 mL |
| 10 mM | 0.2736 mL | 1.368 mL | 2.7361 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。
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Pericyazine for schizophrenia
Cochrane Database Syst Rev 2014 May 13;(5):CD007479.PMID:24825770DOI:10.1002/14651858.CD007479.pub2.
Background: Pericyazine is a 3-cyano-10 (3-4'-hydroxypiperidinopropyl) phenothiazine. It is overall pharmacologically similar with chlorpromazine, though particularly sedating. Dopamine receptor subtype analysis has not been performed for Pericyazine, but the drug appears to induce greater noradrenergic than dopaminergic blockade. Compared to chlorpromazine, Pericyazine reportedly has more potent antiemetic, antiserotonin, and anticholinergic activity. Objectives: To evaluate the clinical effects and safety of Pericyazine in comparison with placebo, typical and atypical antipsychotic agents and standard care for people with schizophrenia. Search methods: We searched the Cochrane Schizophrenia Group Trials Register (February 2013) which is based on regular searches of CINAHL, EMBASE, MEDLINE and PsycINFO. We inspected references of all identified studies for further trials. Selection criteria: All relevant randomised controlled trials focusing on Pericyazine for schizophrenia and other types of schizophrenia-like psychoses (schizophreniform and schizoaffective disorders). We excluded quasi-randomised trials. Data collection and analysis: Data were extracted independently from included papers by at least two review authors. Risk ratios (RR) and 95% confidence intervals (CI) of homogeneous dichotomous data were calculated. We assessed risk of bias for included studies and used GRADE to judge quality of evidence. Main results: We could only include five studies conducted between 1965 and 1980. Most of the included studies did not report details of randomisation, allocation concealment, details of blinding and we could not assess the impact of attrition due to poor reporting.For the primary outcome of Global state - not improved, the confidence interval was compatible with a small benefit and increased risk of not improving with Pericyazine compared with typical antipsychotics (2 RCTs, n = 122, RR 1.24 CI 0.93 to 1.66, very low quality of evidence) or atypical antipsychotics (1 RCT, n = 93, RR 0.97 CI 0.67 to 1.42, very low quality of evidence).When compared with typical antipsychotics relapse was only experienced by one person taking Pericyazine (1 RCT, n = 80, RR 2.59 CI 0.11 to 61.75, very low quality of evidence).Pericyazine was associated with more extrapyramidal side effects than typical antipsychotics (3 RCTs, n = 163, RR 0.52 CI 0.34 to 0.80, very low quality of evidence) and atypical antipsychotics (1 RCT, n = 93, RR 2.69 CI 1.35 to 5.36, very low quality of evidence).The estimated risk of leaving the study early for specific reasons was imprecise for the comparisons of Pericyazine with typical antipsychotics (2 RCTs, n = 71, RR 0.46 CI 0.11 to 1.90, very low quality of evidence), and with atypical antipsychotics (1 RCT, n = 93, RR 0.13 CI 0.01 to 2.42, very low quality of evidence). Authors' conclusions: On the basis of very low quality evidence we are unable to determine the effects of Pericyazine in comparison with typical or atypical antipsychotics for the treatment of schizophrenia. However, there is some evidence that Pericyazine may be associated with a higher incidence of extrapyramidal side effects than other antipsychotics, and again this was judged to be very low quality evidence. Large, robust studies are still needed before any firm conclusions can be drawn.
Pericyazine in the treatment of cannabis dependence in general practice: a naturalistic pilot trial
Subst Abuse Rehabil 2012 May 28;3:43-7.PMID:24474865DOI:10.2147/SAR.S30052.
Cannabis is one of the most widely used illicit drugs worldwide. However, while the rates of cannabis dependence and treatment increase, there remains no medications approved for this use. Due to its sedative effects and low abuse liability, the typical antipsychotic Pericyazine has been utilized in some parts of Australia for the treatment of cannabis dependence. We aimed to provide documentation of preliminary outcomes and acceptability of Pericyazine treatment in a small sample. A naturalistic case series study was conducted in which 21 patients were enrolled for a 4-week course of Pericyazine (up to 8 × 2.5 mg tablets daily) and weekly medical review. Levels of cannabis use were reported and side effects with electrocardiography and blood tests were monitored. Measures of dependence severity, depression, anxiety, and insomnia were taken at baseline and follow-up utilizing validated psychometric tools. Significant reductions in cannabis use, depression, anxiety, and insomnia severity occurred across time. Pericyazine appeared to be well tolerated and easily administered in the community clinics. The results provide some preliminary evidence that low-dose short-term Pericyazine may be an acceptable mode of treatment in this population. Given the open-label nature of the design, we cannot conclude that pharmacotherapy was uniquely responsible for the treatment effect. Nonetheless, low-dose Pericyazine may be a potentially effective approach to the treatment of cannabis dependence, and further evaluation via a randomized placebo-controlled trial is warranted.
Experience with Pericyazine in profoundly and severely retarded children
Can Med Assoc J 1972 Jan 22;106(2):136-41.PMID:4400557doi
The effectiveness of Pericyazine in severe behavioural disorders was evaluated in 15 profoundly and severely retarded children. Pericyazine provided significant improvement in such parameters as co-operation, temper, purposeless activities, hyperactivity, communication and mood. It proved to be statistically superior to the minor tranquillizers in improving co-operation and helpfulness, temper, mood, the understanding of commands and table manners, and in reducing self-abusiveness and abusiveness to staff. The safety of this agent was confirmed and photosensitivity was not found to be associated with its use.
A sensitive LC-MS/MS method for analysis of Pericyazine in presence of 7-hydroxypericyazine and Pericyazine sulphoxide in human plasma and its application to a comparative bioequivalence study in Chinese healthy volunteers
J Pharm Biomed Anal 2017 Feb 20;135:67-74.PMID:28012307DOI:10.1016/j.jpba.2016.12.007.
A robust and highly sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the determination of Pericyazine in human plasma. The plasma sample was alkalized with sodium hydroxide solution and handled by liquid-liquid extraction with ethyl acetate after adding perphenazine as an internal standard (IS). The analytes were separated on an Ultimate™ AQ-C18 analytical column at 40°C, with a gradient elution consisting of A (aqueous phase: 5mM ammonium acetate buffer solution containing 0.1% formic acid) and B (organic phase: acetonitrile) at a flow rate of 0.350mL/min. The detection was conducted on an API 4000 tandem mass spectrometer coupled with electrospray ionization (ESI) source in positive ion mode. The multiple reaction monitoring (MRM) transitions, m/z 366.5>142.4 for Pericyazine, m/z 382.5>142.4 for its 7-hydroxy and sulphoxide metabolites and m/z 404.3>171.3 for IS were chosen to achieve high selectivity in the simultaneous analyses. The method exhibited great improvement in sensitivity (LLOQ of 0.021ng/mL) and good linearity over the concentration range of 0.021-9.90ng/mL. The intra- and inter-day precision, accuracy, and stability results were within the acceptable limits and no matrix effect was observed. This method was successfully applied in a bioequivalence study to evaluate the pharmacokinetics in 20 healthy male Chinese volunteers. Additional exploratory analyses of 7-hydroxy and sulphoxide metabolites of Pericyazine in the same samples suggest that the unchanged drug is predominant in the plasma and suitable for the bioequivalence comparison after a single oral administration of 10mg Pericyazine.
[The efficacy and tolerability of Pericyazine in the treatment of patients with schizotypal disorder, organic personality disorders and pathocharacterological changes within personality disorders]
Zh Nevrol Psikhiatr Im S S Korsakova 2017;117(10):65-71.PMID:29171491DOI:10.17116/jnevro201711710165-71.
Aim: To assess the efficacy and tolerability of Pericyazine in the treatment of patients with mental disorders manifesting with psychopathic-like symptoms and correction of pathocharacterological disorders in patients with personality disorders during the short-term admission to the hospital or the long-term outpatient treatment. Material and methods: Sixty-three patients with schizotypal personality disorder and organic personality disorder with psychopathic-like symptoms and pathocharacterological changes within the diagnosis of dissocial personality disorder and borderline personality disorder were examined. Patients received Pericyazine during the short-term admission to the hospital (6 weeks) or the long-term outpatient treatment (6 month). Efficacy, tolerability and compliance were assessed in the study. Results and conclusion: Treatment with pricyazine was effective in all patients. The improvement was seen in patients with organic personality disorders and patients with personality disorders (psychopathy). The maximal effect was observed in inpatients and this effect remained during outpatient treatment. The improvement of mental state of patients with schizotypal personality disorder achieved during inpatient treatment with Pericyazine continued during the long-term outpatient treatment. Side-effects were restricted to extrapyramidal symptoms, the frequency of metabolic syndrome was low. During outpatient treatment, the compliance was higher if the patient was managed by the same psychiatrist during inpatient- and outpatient treatment.