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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Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
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Inaccessible (Haz class 6.1), International | USD 150+ |
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Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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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。 |
靶点 |
|
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]. |
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 << | |
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 |
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 |