Perospirone
(Synonyms: 哌罗匹隆; SM-9018 free base) 目录号 : GC39237
Perospirone (SM-9018 free base) is an orally active antagonist of 5-hydroxytryptamine2 (5-HT2) receptor, dopamine2 (D2) receptor and 5-HT1A receptor with Ki of 0.6 nM, 1.4 nM and 2.9 nM, respectively.
Cas No.:150915-41-6
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
Perospirone (SM-9018 free base) is an orally active antagonist of 5-hydroxytryptamine2 (5-HT2) receptor, dopamine2 (D2) receptor and 5-HT1A receptor with Ki of 0.6 nM, 1.4 nM and 2.9 nM, respectively.
[1] T Kato, et al. Jpn J Pharmacol. 1990 Dec;54(4):478-81.
| Cas No. | 150915-41-6 | SDF | |
| 别名 | 哌罗匹隆; SM-9018 free base | ||
| Canonical SMILES | O=C([C@@]1([H])[C@]2([H])CCCC1)N(C2=O)CCCCN3CCN(C4=NSC5=C4C=CC=C5)CC3 | ||
| 分子式 | C23H30N4O2S | 分子量 | 426.57 |
| 溶解度 | DMSO : 5 mg/mL (11.72 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 | 2.3443 mL | 11.7214 mL | 23.4428 mL |
| 5 mM | 0.4689 mL | 2.3443 mL | 4.6886 mL |
| 10 mM | 0.2344 mL | 1.1721 mL | 2.3443 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。
Perospirone
CNS Drugs 2001;15(4):329-37; discussion 338.PMID:11463136DOI:10.2165/00023210-200115040-00006.
Perospirone is an atypical antipsychotic agent for the treatment of schizophrenia. Its primary mode of action is through antagonism of serotonin 5-HT2A and dopamine D2 receptors. An 8-week course of oral Perospirone 8 to 48 mg/day displayed efficacy in up to 75% of patients with schizophrenia participating in phase II and phase III trials. The onset of action of the drug was about 2 weeks. Perospirone was effective against positive, negative and general symptoms in patients with schizophrenia, as assessed with standard rating scales (Brief Psychiatric Rating Scale, Positive and Negative Symptom Scale). Compared with haloperidol 2 to 12 mg/day, Perospirone 8 to 48 mg/day was significantly more effective against negative symptoms and tended to be more effective against general symptoms and most positive symptoms in a trial in 145 patients with schizophrenia. Perospirone had efficacy similar to that of mosapramine 50 to 300 mg/day in a comparative phase III trial in 159 patients. Extrapyramidal symptoms (EPS) tended to occur less often and were generally milder with Perospirone than with haloperidol or mosapramine.
Perospirone (Sumitomo Pharmaceuticals)
Curr Opin Investig Drugs 2002 Jan;3(1):121-9.PMID:12054062doi
Perospirone is a serotonin 5-HT2 antagonist and dopamine D2 antagonist developed by Sumitomo Pharmaceuticals for the potential treatment of schizophrenia and other psychoses [381769]. Its receptor binding profile and animal pharmacology resemble those of other atypical antipsychotic agents, in particular risperidone. In November 2000, CPAC's First Committee on Drugs recommended the approval of this product in Japan, [394007]; approval was granted in December 2000 [396121]. In January 2001, the NHI price was agreed by the Chuikyo [398222] and the drug was added to the NHI price list in February 2001 13982261. It was finally launched in Japan on February 8 2001 [399401]. In November 2000, Sumitomo and Welfide signed an agreement whereby Welfide's subsidiary Yoshitomi Yakuhin will copromote Perospirone [394007]. Based on data from the Chuikyo, peak sales of Perospirone are forecast to be yen9 billion in the sixth year following launch [398222], [398226]. In February 2001, Sumitomo predicted that Perospirone would reach sales of yen10 billion within five to six years [399401].
Efficacy and tolerability of Perospirone in schizophrenia: a systematic review and meta-analysis of randomized controlled trials
CNS Drugs 2013 Sep;27(9):731-41.PMID:23812802DOI:10.1007/s40263-013-0085-7.
Background: Perospirone is a second-generation antipsychotic (SGA) used only in Japan, and acts as a serotonin (5-HT)1A receptor partial agonist, 5-HT2A receptor inverse agonist, and dopamine (D)₂, D₄, and α₁-adrenergic receptor antagonist. To our knowledge, no meta-analysis addressing the efficacy and effectiveness of Perospirone in schizophrenia has been published to date. Objective: The aim of the study was to identify the characteristics of Perospirone by assessing the efficacy, discontinuation rate, and side effects of Perospirone versus other antipsychotics in the treatment of patients with schizophrenia. Methods: Using information obtained from the PubMed, PsycINFO, Google Scholar and Cochrane Library databases without language restrictions published up to 10 June 2013, we conducted a systematic review and meta-analysis of patient data from randomized controlled trials comparing Perospirone with other antipsychotic medications. Risk ratio (RR), standardized mean difference (SMD) and 95% confidence intervals were calculated. All studies used the Positive and Negative Syndrome Scale (PANSS) for the evaluation of the schizophrenia psychopathology. Results: The search in PubMed, Cochrane Library databases, Google Scholar and PsycINFO yielded 69 hits. We included three studies in the current meta-analysis and excluded 66 studies based on title, abstract, and full text review. Moreover, two additional studies were identified from a review article. Across the five studies (mean duration 9.6 weeks), 562 adult patients with schizophrenia were randomized to Perospirone (n = 256), olanzapine (n = 20), quetiapine (n = 28), risperidone (n = 53), aripiprazole (n = 49), haloperidol (n = 75), or mosapramine (n = 81). Perospirone was not different from other pooled antipsychotics regarding reduction in PANSS negative (SMD = 0.38, p = 0.09) and general (SMD = 0.28, p = 0.06) subscale scores, and discontinuation due to any cause (RR = 1.03, p = 0.83), inefficacy (RR = 0.99, p = 0.98) and side effects (RR = 0.72, p = 0.25). However, Perospirone was inferior to other pooled antipsychotics in the reduction of PANSS total scores (SMD = 0.36, p = 0.04) and positive subscale scores (SMD = 0.34, p = 0.03). Moreover, excluding the comparison of Perospirone with the first-generation antipsychotic (haloperidol), Perospirone was inferior to other pooled SGAs in the reduction of PANSS total scores (SMD = 0.46, p = 0.02), positive (SMD = 0.42, p = 0.03), negative (SMD = 0.52, p = 0.02) and general subscale scores (SMD = 0.37, p = 0.03). However, Perospirone was superior to haloperidol in the reduction of PANSS negative subscale scores (SMD = -0.41, p = 0.01). Perospirone also had lower scores related to extrapyramidal symptoms than other pooled antipsychotics (SMD = -0.30, p = 0.01). Conclusions: Our results suggest that although Perospirone seems to be a well tolerated treatment, Perospirone does not reduce PANSS score as much as other SGAs.
[Pharmacological characteristics of Perospirone hydrochloride, a novel antipsychotic agent]
Nihon Yakurigaku Zasshi 2000 Oct;116(4):225-31.PMID:11084919DOI:10.1254/fpj.116.225.
It is now known that the blockade of 5-HT2 receptors can ameliorate the negative symptoms of schizophrenia and extrapyramidal side effects (EPS) associated with antipsychotic treatments. Perospirone hydrochloride (Perospirone), which was identified as a novel serotonin-dopamine antagonist (SDA)-type antipsychotic agent in 1987 by Sumitomo Pharmaceuticals, possesses high affinities both for dopamine 5-HT2 and D2 receptors. Perospirone, like conventional antipsychotics, significantly inhibited various behaviors induced by dopaminergic hyperactivation. Perospirone also produced a significant improvement in animal models of the negative symptoms and mood disorders, where the conventional antipsychotics were unaffected. In addition, Perospirone was weaker than the conventional antipsychotics (e.g., haloperidol) in inducing EPS signs (e.g., catalepsy and bradykinesia), suggesting that the drug has an atypical antipsychotic property. A recent double-blind study with schizophrenia patients demonstrated that Perospirone was comparative with haloperidol in improving the positive symptoms, but was significantly superior to haloperidol against the negative symptoms. Furthermore, the extrapyramidal score in patients with Perospirone treatment was lower that those with haloperidol treatment. These findings suggested that Perospirone acts as an antagonist both for 5-HT2 and D2 receptors and has broader clinical efficacy and lower EPS liability than haloperidol in schizophrenia treatment.
Safety and Effectiveness of Perospirone in Comparison to Risperidone for Treatment of Delirium in Patients with Advanced Cancer: A Multicenter Prospective Observational Study in Real-World Psycho-Oncology Settings
Acta Med Okayama 2022 Apr;76(2):195-202.PMID:35503448DOI:10.18926/AMO/63414.
The clinical benefit of Perospirone for treatment of delirium in patients with advanced cancer is not sufficiently clear. The objective of this study was to compare the safety and effectiveness of Perospirone to those of risperidone for the treatment of delirium in patients with advanced cancer. This is a secondary analysis of a multicenter prospective observational study in nine psycho-oncology consultation services in Japan. The study used the Delirium Rating Scale (DRS) Revised-98 to measure effectiveness and the CTCAE (Common Terminology Criteria for Adverse Events) version 4 to assess safety. Data from 16 patients who received Perospirone and 53 patients who received risperidone were analyzed. The mean age was 70 years in the Perospirone group and 73 years in the risperidone group. Both groups showed a significant decrease in the total score of DRS-R-98 after three days of treatment (Perospirone: 11.7 (7.9-15.4) to 7.0 (3.3-10.7), difference -4.7, effect size=0.72, p=0.003; risperidone: 15.5 (13.6-17.4) to 12.2 (10.1-14.2), difference -3.3, effect size=0.55, p=0.00). The risperidone group showed significant improvements in sleep-wake cycle disturbance, orientation, attention, and visuospatial ability. In the Perospirone group, there was a significant improvement of sleep-wake cycle disturbance. The median daily dose of Perospirone was 4 mg/day. There were fewer episodes of somnolence as an adverse event in the Perospirone group. Low-dose Perospirone was thus found to be effective for the treatment of delirium in patients with advanced cancer and may be associated with fewer episodes of over-sedation as an adverse event.