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帕潘立酮 /Paliperidone {[allProObj[0].p_purity_real_show]}

货号:A267994 同义名: 9-羟基利培酮 / 9-Hydroxyrisperidone;RO76477

Paliperidone is a potent serotonin-2A and dopamine-2 receptor antagonist, it is the main active metabolite of risperidone and used in the treatment of schizophrenia.

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Paliperidone 化学结构 CAS号:144598-75-4
Paliperidone 化学结构
CAS号:144598-75-4
Paliperidone 3D分子结构
CAS号:144598-75-4
Paliperidone 化学结构 CAS号:144598-75-4
Paliperidone 3D分子结构 CAS号:144598-75-4
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Paliperidone 纯度/质量文件 产品仅供科研

货号:A267994 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 D1 receptor D2 receptor D3 receptor D4 receptor D5 receptor DAT Dopamine receptor 其他靶点 纯度
Penfluridol +

Dopamine receptor, Ki: 1.6 μM

98%
Ansofaxine HCl ++

Dopamine receptor, IC50: 491 nM

98%
Tetrahydroberberine,THB +

D2 receptor, pKi: 6.08

98+%
Prochlorperazine Maleate 95%
Olanzapine 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

98%
Ropinirole hydrochloride ++

D2 receptor, Ki: 29 nM

99%
Lurasidone ++++

D2 receptor, Ki: 1 nM

98%
Levosulpiride 99+%
Pridopidine 95%
Metoclopramide 99+%
Molindone HCl 98%
Sulpiride 99+%
Perospirone ++++

D2 receptor, Ki: 1.4 nM

99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

98+%
Phenothiazine 98%
Pimozide +

Dopamine D1 receptor, Ki: 6600 nM

+++

Dopamine D2 receptor, Ki: 3.0 nM

++++

Dopamine D3 receptor, Ki: 0.83 nM

98%
Rotundine ++

D1 receptor, IC50: 166 nM

+

D2 receptor, IC50: 1.47 μM

+

D3 receptor, IC50: 3.25 μM

98%
Domperidone 99+%
ONC206 97%
Pimethixene maleate ++

Dopamine D1 Receptor, pKi: 6.37

+++

Dopamine D2 Receptor, pKi: 8.19

++

Dopamine D4.4 Receptor, pKi: 7.54

97%
Loxapine succinate ++

D1 receptor (human), Ki: 26 nM

D2 receptor (Human), Ki: 62 nM

++

D2 receptor (bovine), Ki: 26 nM

D2 receptor (human), Ki: 24 nM

+++

D4 receptor (human), Ki: 7.5 nM

99%
Chlorprothixene +++

D1 receptor, Ki: 18 nM

+++

D2 receptor, Ki: 2.96 nM

+++

D3 receptor, Ki: 4.56 nM

+++

D5 receptor, Ki: 9 nM

98%
SCH-23390 HCl ++++

D1 dopamine receptor, Ki: 0.2 nM

++++

D5 dopamine receptor, Ki: 0.3 nM

98%
MPP+ iodide 97%
σ1 Receptor antagonist-1 +

DAT, pKi: 5.8

97%
Benztropine mesylate ++

DAT, IC50: 118 nM

98%
Azaperone 98%
Ziprasidone HCl 98+%
Paliperidone 98%
Alizapride HCl 99+%
Amisulpride 98%
Quetiapine hemifumarate Adrenergic Receptor 98%
Clozapine N-oxide 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Paliperidone 生物活性

靶点
  • Dopamine receptor

描述 Paliperidone is a second-generation antipsychotic drug belonging to the class of benzisoxasole derivatives. Paliperidone is the major active metabolite of risperidone (9-OH-risperidone) and, as such, is comparable to the latter in terms of pharmacodynamic properties[3]. Paliperidone has demonstrated efficacy in the reduction of acute schizophrenia symptoms and clinical benefits were maintained also in the long-term treatments. Paliperidone ER (extended-release) and PP (paliperidone palmitate) are generally well tolerated with a predictable adverse event profile[4]. Paliperidone inhibited MK-801 induced neurotoxicity both in MTT metabolism assay and in lactate dehydrogenase (LDH) activity assay. Time course studies revealed that paliperidone effectively attenuated the elevation of intracellular free calcium concentration ([Ca(2+)]i) induced by exposure to MK-801. Moreover, paliperidone could significantly retard MK-801-mediated inhibition of neurite outgrowth and reverse MK-801-induced decreases of gene expression and phosphorylation of Akt1 and GSK3β[5]. Moreover, paliperidone works finely at low concentrations (10 and 50 μM) against Aβ(25-35) and MPP(+) and solely protected SH-SY5Y from hydrogen peroxide. At 100 μM, paliperidone completely diminished cell reduction induced by different stressors, regardless of their dosages. Paliperidone was demonstrated with a higher oxidative stress-scavenging properties than other APDs (Antipsychotic drugs) in several aspects, such as generated bulk glutathione, low HNE, and protein carbonyl productions[6].

Paliperidone 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01742390 Sexual Dysfunction ... 展开 >> Hyperprolactinemia 收起 << Phase 4 Unknown June 2014 China, Beijing ... 展开 >> Institute of mental health, Peking University Not yet recruiting Beijing, Beijing, China, 100191 Contact: Tianmei Si, MD.    8610-82801948    si.tian-mei@163.cm    Principal Investigator: Tianmei Si, MD.          China, Hebei The first hospital of Hebei Province University Recruiting Shijiazhuang, Hebei, China, 050000 Contact: Xueyi Wang, Professor    0311-85917290       Sub-Investigator: Xueyi Wang 收起 <<
NCT00589914 Schizophrenia Phase 3 Completed - -
NCT02532842 - Completed - Croatia ... 展开 >> Rijeka, Croatia Split, Croatia Zagreb, Croatia Russian Federation Moscow, Russian Federation St Petersburg N/A, Russian Federation St-Petersburg, Russian Federation Turkey Ankara, Turkey Denizli, Turkey 收起 <<

Paliperidone 参考文献

[1]Zhu HJ, Wang JS, et al. Risperidone and paliperidone inhibit p-glycoprotein activity in vitro. Neuropsychopharmacology. 2007 Apr;32(4):757-64.

[2]Woestenborghs R, Lorreyne W, et al. Determination of risperidone and 9-hydroxyrisperidone in plasma, urine and animal tissues by high-performance liquid chromatography. J Chromatogr. 1992 Dec 2;583(2):223-30.

[3]Valsecchi P, Garozzo A, Nibbio G, et al. Paliperidone extended-release in the short- and long-term treatment of schizophrenia. Riv Psichiatr. 2019;54(2):43‐58

[4]Mauri MC, Reggiori A, Paletta S, Di Pace C, Altamura AC. Paliperidone for the treatment of schizophrenia and schizoaffective disorders - a drug safety evaluation. Expert Opin Drug Saf. 2017;16(3):365‐379

[5]Peng L, Zhu D, Feng X, et al. Paliperidone protects prefrontal cortical neurons from damages caused by MK-801 via Akt1/GSK3β signaling pathway. Schizophr Res. 2013;147(1):14‐23

[6]Yang MC, Lung FW. Neuroprotection of paliperidone on SH-SY5Y cells against β-amyloid peptide(25-35), N-methyl-4-phenylpyridinium ion, and hydrogen peroxide-induced cell death. Psychopharmacology (Berl). 2011;217(3):397‐410

Paliperidone 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.72mL

2.34mL

1.17mL

23.45mL

4.69mL

2.34mL

Paliperidone 技术信息

CAS号144598-75-4
分子式C23H27FN4O3
分子量 426.484
别名 9-羟基利培酮 ;9-Hydroxyrisperidone;RO76477
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 4 mg/mL(9.38 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

IP 5% DMSO+water 1 mg/mL clear

PO 0.5% CMC-Na 65 mg/mL suspension

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