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Journal of Pharmaceutical Analysis 2017年第6期7卷 406-410页

作者： Shixiao Wang Yang Wang Shuang Gao Yuanyuan Zhang Hanpei Wang Longshan Zhao Kaishun Bi Shaojie Wang Xiaohui Chen School of Pharmacy Shenyang Pharmaceutical University Shenyang 110016 China Key Laboratory of Structure-Based Drugs Design&Discovery of Ministry of Education Shenyang Pharmaceutical University Shenyang 110016 China

A simple, rapid and sensitive method based on an ultra-performance liquid chromatography tandem mass spectrometry （UPLC-MS/MS） has been developed and validated for the determination of Pimavanserin in rat plasma. The analyte was extracted by protein precipitation with methanol and separated on an ACQUITY BEH C18 column （100 mm × 2.1 mm, 1.7μm; Waters, USA）, with an isocratic elution of acetonitrile-water containing 10 mM ammonium acetate （70：30, v/v）, at a flow rate of 0.2 mL/min for 2.5 rain. The analyte and clarithromyein （the internal standard） were detected and quantified in positive ion mode using multiple reaction monitoring transitions at m/z 428.2 - 223.0 for Pimavanserin and m/z 748.5 - 589.5 for clarithromycin. Relative coefficient （r） for the calibration curve was more than 0.9980. The intra-day and inter-day precisions （relative standard deviation, RSD%） were less than 13.3% and 10.5%, respectively, and the accuracy （relative error, RE%） was within ± 11.5%. The analytical method was successfully applied to a routine pharmacokinetic study of Pimavanserin in rats after oral administration at the dose of 10 mg/kg.

关键词： UPLC-MS/MS Pimavanserin Pharmacokinetics Rat plasma

治疗帕金森精神症新药Pimavanserin

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中国新药杂志 2017年第5期26卷 481-483页

作者：宋品娆温利民姜锋李迪林彬彬曹丽萍江苏海岸药业有限公司苏州215211 扬子江药业集团有限公司泰州225321

Pimavanserin是一种口服高选择性的5-羟色胺受体2A亚型反向激动剂,于2016年4月获得美国FDA批准,是首个获准用于治疗帕金森精神症(Parkinson's disease psychosis)的药物。本文对Pimavanserin的作用机制、药动学性质、临床研究以及药物... 详细信息

Pimavanserin是一种口服高选择性的5-羟色胺受体2A亚型反向激动剂,于2016年4月获得美国FDA批准,是首个获准用于治疗帕金森精神症(Parkinson's disease psychosis)的药物。本文对Pimavanserin的作用机制、药动学性质、临床研究以及药物相互作用等方面进行综述。

关键词： Pimavanserin 帕金森精神症 5-羟色胺2A反向激动剂临床研究

Pimavanserin for the treatment of psychosis in Alzheimer’s disease: A literature review

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World Journal of Psychiatry 2020年第7期10卷 162-174页

作者： Shilpa Srinivasan Rajesh R Tampi Kripa Balaram Arushi Kapoor Department of Neuropsychiatry and Behavioral Science Palmetto Health USC Medical GroupUniversity of South Carolina School of MedicineColumbiaSC 29203United States Department of Psychiatry and Behavioral Sciences Cleveland Clinic Akron GeneralAkronOH 44307United States MD Department of PsychiatryMetroHealthClevelandOH 44109United States Penn Memory Center at the Penn Neuroscience Center Perelman Center for Advanced MedicinePhiladelphiaPA 19104United States

BACKGROUND Alzheimer’s disease(AD)is among the most prevalent forms of dementia in the world and neuropathological studies suggest similar high prevalence of mixed(AD+vascular)dementias.Approximately 25%-50%of individuals with AD develop psychosis sometime during their illness.The presence of psychosis in AD worsens outcomes.Currently there are no United States Food and Drug Administration(FDA)approved medications for the treatment of psychosis in AD.Pimavanserin,a novel atypical antipsychotic medication,was approved by the FDA for the treatment of hallucinations and delusions associated with Parkinson disease psychosis and is currently in clinical trials for the treatment of psychosis in AD.AIM To evaluate the existing literature regarding the use of Pimavanserin for treating psychosis among individuals with AD.METHODS A literature review of clinical studies of Pimavanserin treatment for psychosis in individuals with AD was performed using the Preferred Reporting Items for Systematic Review and Meta-Analysis guidelines.Trials were identified by systematically searching PubMed,MEDLINE,EMBASE,Cochrane Central Register of Controlled Trials,Web of Science,and Scopus through October 2019.The 5-point Jadad scoring system was used to assess the methodologic quality of the randomized placebo-controlled trials.RESULTS A total of 499 citations were retrieved and pooled in EndNote and de-duplicated to 258 citations.This set was uploaded to Covidence for screening.Two separate screeners(Srinivasan S and Tampi RR)evaluated the titles,abstracts,and full text of eligible articles.Of the identified 258 abstracts,98 articles underwent full text review and 2 publications from 1 randomized controlled trial(RCT)were included in the final analysis.The quality of evidence was assessed to be of good methodologic quality,scoring 4 out of 5 using the 5-point Jadad questionnaire with the Jadad Scoring calculation.This systematic review found only one RCT that evaluated the use of Pimavanserin for the treatment of psychosis among individu

关键词： Pimavanserin Alzheimer’s disease Psychosis Psychotic disorders Antipsychotic agents

Evidence for using Pimavanserin for the treatment of Parkinson’s disease psychosis

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World Journal of Psychiatry 2019年第3期9卷 47-54页

作者： Rajesh R Tampi Deena J Tampi Juan J Young Silpa Balachandran Rakin A Hoq Geetha Manikkara Department of Psychiatry and Behavioral Sciences Cleveland Clinic Akron GeneralOhioNH 44106United States Cleveland Clinic Lerner College of Medicine of Case Western Reserve University OhioCleveland 44195United States Diamond Healthcare RichmondVA 23219United States Case Western Reserve University School of Medicine Department of PsychiatryClevelandOH 44109United States Department of Psychiatry Summa Health SystemAkronOH 44304United States Department of Psychiatry Texas Tech University Health Science CenterMidlandTX 79701United States

The aim of this editorial is to evaluate the evidence for using Pimavanserin for the treatment of Parkinson's disease psychosis(PDP)from randomized controlled trials(RCTs).We only identified two published trials that evaluated the use of Pimavanserin among individuals with PDP.Both studies found that Pimavanserin improved psychotic symptoms among individuals with PDP when compared to placebo.Pimavanserin was fairly well tolerated in both studies and did not appear to cause significant sedation or worsen motor symptoms among individuals with PDP.However,given the limited data,additional confirmatory studies are required before Pimavanserin can be considered as a first line agent for the treatment of psychotic symptoms among individuals with PD.

关键词： Pimavanserin Parkinson’s disease Parkinson’s disease psychosis Psychosis Antipsychotic

Pimavanserin：治疗帕金森精神症的新药

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药学与临床研究 2017年第6期25卷 501-504页

作者：刘敏李月阳柯巍王婷婷吉林大学第一医院药学部长春130021

Pimavanserin是选择性5-HT2A反向激动剂,已于2016年4月29日经美国食品药品管理局批准用于治疗帕金森精神症。本文对该药的药理作用、临床应用、药动学研究、用法用量、药物相互作用和不良反应作一综述。

关键词： Pimavanserin 帕金森精神症药理作用

美国FDA批准Nuplazid(Pimavanserin)用于治疗帕金森病患者的精神病症状

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广东药学院学报 2016年第3期32卷 369-369页

作者：夏训明

美国FDA于2016年4月29日批准Acadia药业公司（Acadia Pharmaceuticals Inc.）研制生产的Nuplazid（Pimavanserin,匹莫范色林）片剂用于治疗帕金森病患者出现的精神病症状,如幻觉（hallucinations）和错觉（delusions）等。

关键词：帕金森病 Nuplazid Pimavanserin 精神病症状反向激动剂神经传递神经性疾病多巴阿尔茨海默病外周性

FDA批准治疗帕金森病相关精神症状药物Pimavanserin上市

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中国执业药师 2016年第8期13卷 14-14页

美国FDA于2016年4月29日批准阿卡迪亚（Acadia）制药公司的Pimavanserin（参考译名：哌马色林,商品名：Nuplazid）片剂上市,用于治疗帕金森病相关的幻觉和妄想。本药用于治疗帕金森病相关的幻觉和妄想的机制尚不明确。本药的效应可通过... 详细信息

美国FDA于2016年4月29日批准阿卡迪亚（Acadia）制药公司的Pimavanserin（参考译名：哌马色林,商品名：Nuplazid）片剂上市,用于治疗帕金森病相关的幻觉和妄想。本药用于治疗帕金森病相关的幻觉和妄想的机制尚不明确。本药的效应可通过在5-羟色胺2A（5-HT2A）受体和较少程度的5-HT2C受体上结合反向激动和拮抗活性来介导。

关键词：帕金森病 FDA Pimavanserin 阿卡迪亚商品名拮抗活性安慰剂对照色胺制药公司评分量表

伏隔核与腹侧海马5-羟色胺2A受体活性对小鼠“感觉门控”功能的调控作用

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伏隔核与腹侧海马5-羟色胺2A受体活性对小鼠“感觉门控”功能的调...

作者：石梦雯西南大学

学位级别：硕士

研究背景:在大量精神障碍中,都会出现前脉冲抑制(Prepulse inhibition,PPI)的破坏。前脉冲抑制是一种对感觉门控进行测量的经典范式,它是在强烈的刺激(脉冲)发生前30～500毫秒时,预先出现一种较弱的刺激(前脉冲),因此抑制了个体对更强... 详细信息

研究背景:在大量精神障碍中,都会出现前脉冲抑制(Prepulse inhibition,PPI)的破坏。前脉冲抑制是一种对感觉门控进行测量的经典范式,它是在强烈的刺激(脉冲)发生前30～500毫秒时,预先出现一种较弱的刺激(前脉冲),因此抑制了个体对更强烈刺激的惊跳反射。感觉门控是指在一个充满刺激的环境中,将无关的感官讯息过滤掉,再执行与注意力有关的认知活动,进而对重要的刺激作出反应。前脉冲抑制的损伤出现在精神分裂症、阿尔兹海默症、强迫症等一系列精神疾病患者中。作为一种中枢神经系统内大量表达的5-羟色胺受体亚型,5-羟色胺2A受体(5-hydroxytryptamine 2A receptor,5-HT受体)的结构和功能异常与许多精神疾病有关,非典型抗精神病药物正是以5-HT受体为治疗靶点。已有研究间接表明多巴胺D受体激动剂可以模拟前脉冲抑制的缺失,而5-HT受体反向激动剂Pimavanserin可通过下调5-HT受体活性缓解或逆转啮齿类动物的PPI缺失,恢复动物受损的前脉冲抑制,但5-HT受体反向激动剂逆转作用的确切机制和关键脑区尚不清楚。明确关键脑区能够为精神分裂症相关研究的临床转化起到重要作用。研究假设:在小鼠的腹腔注射5-HT受体反向激动剂Pimavanserin可以通过降低5-HT受体活性逆转由多巴胺D受体非选择性激动剂培高利特引起的PPI缺失,并且存在关键脑区参与这个过程,在该关键脑区微量注射5-HT受体反向激动剂Pimavanserin可以恢复由腹腔给药多巴胺D受体激动剂培高利特引起的PPI损伤。研究方法:实验一探讨5-HT受体反向激动剂Pimavanserin对动物前脉冲抑制的基线水平是否产生影响,使用听觉惊跳反射的前脉冲抑制测试,对基线在两个标准差以内的动物进行腹腔给药5-HT受体反向激动剂Pimavanserin(15 mg/kg或30 mg/kg),然后在60分钟后进行行为测试,记录小鼠在前脉冲刺激分别为73d B(分贝)、76d B、82d B时的抑制率以及小鼠的惊跳反射。实验二探讨5-HT受体反向激动剂Pimavanserin是否能逆转由多巴胺D受体激动剂培高利特引起的PPI缺失。实验二使用听觉惊跳反射的前脉冲抑制测试,对基线在两个标准差以内的动物在测试前60分钟腹腔注射5-HT受体反向激动剂Pimavanserin(15mg/kg或30mg/kg),然后在测试前15分钟腹腔注射多巴胺D受体激动剂培高利特,记录小鼠在前脉冲刺激分别为73d B、76d B、82d B时的抑制率以及小鼠的惊跳反射。实验三～六探讨了5-HT受体反向激动剂Pimavanserin恢复动物PPI缺失的关键脑区。实验三使用听觉惊跳反射的前脉冲抑制测试,对基线在两个标准差以内的动物进行脑立体定位手术,分别植入微量注射的双套管,之后使用5-HT受体反向激动剂Pimavanserin(0.25μg/0.25μl/侧)向脑区中进行微量注射,并在腹腔注射多巴胺D受体激动剂培高利特,记录小鼠在前脉冲刺激分别为73d B、76d B、82d B时的抑制率以及小鼠的惊跳反射。实验七～八探讨5-HT受体反向激动剂pimavaserin和多巴胺D受体激动剂培高利特是否会对动物的活动水平产生影响。实验七和实验八使用自发活动测试设备,对PPI测试基线水平在两个标准差以内的动物分别进行全身给药和脑区给药两种方式进行测试,在伏隔核、内侧前额叶皮层、腹侧海马、腹侧被盖区四个脑区注射5-HT受体反向激动剂Pimavanserin,并在腹腔注射多巴胺D受体激动剂培高利特,记录小鼠在60分钟内的活动距离和速度。研究结果:实验一的结果为腹腔注射Pimavanserin可以提高PPI基线水平。实验二的结果为腹腔注射Pimavanserin可以逆转由多巴胺D受体激动剂培高利特引起的PPI缺失。实验三～六的结果为在伏隔核和腹侧海马局部注射pimavansein可以恢复PPI缺失,而内侧前额叶皮层和腹侧被盖区的局部给药对PPI无显著影响。实验七～八的结果为培高利特腹腔给药会引起动物运动能力下降,但是在腹腔以及不同脑区给药Pimavanserin均不会恢复运动能力。研究结论:1)降低雄性小鼠5-HT受体的活性可以提高正常动物的PPI行为,并恢复由多巴胺D受体激动剂引起的PPI缺失;2)伏隔核和腹侧海马是5-HT受体参与调节前脉冲抑制的关键脑区;3)多巴胺D受体激动剂引起PPI缺失的同时也会对运动能力有破坏,5-HT受体反向激动剂Pimavanserin的恢复能力是针对PPI水平,而对运动能力无影响。

关键词： 5-羟色胺2A受体反向激动剂 Pimavanserin 前脉冲抑制精神分裂症