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/ Risperidone

利培酮 /Risperidone {[allProObj[0].p_purity_real_show]}

货号：A324792 同义名： 利哌酮 / R 64 766;Apexidone

Risperidone is a multiple-target antipsychotic with high affinity for 5-HT2A and D2 receptors, alpha 1, alpha 2 and H1 receptors.

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Risperidone 化学结构 CAS号：106266-06-2
Risperidone 化学结构
CAS号：106266-06-2
Risperidone 3D分子结构
CAS号：106266-06-2
Risperidone 化学结构 CAS号：106266-06-2
Risperidone 3D分子结构 CAS号：106266-06-2
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Risperidone 纯度/质量文件 产品仅供科研

货号：A324792 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]
• JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]
• BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]
• J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]
• PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]
更多 >
产品名称 5-HT ↓ 5-HT1 ↓ 5-HT2 ↓ 5-HT3 ↓ 5-HT5 ↓ 5-HT6 ↓ 5-HT7 ↓ 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

 		98%
Lamotrigine +

5-HT (rat brain synaptosomes), IC50: 474 μM

5-HT (human platelets), IC50: 240 μM

 		98%
Venlafaxine ✔ 98%
Fluvoxamine maleate ✔ 99%
Iloperidone ✔ 98%
Ziprasidone HCl ✔ 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

 		98%
Dapoxetine HCl ✔ 97%
Trazodone ✔ 98+%
Clomipramine HCl ✔ 98%
Mirtazapine ✔ 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

 		97%
Duloxetine ✔ 98+%
Sertraline HCl ++

5-HT, Ki: 13 nM

 		98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

 		98%
Latrepirdine 2HCl ✔ GluR 98%
Fluoxetine HCl ✔ 99.5%
Paroxetine hydrochloride ✔ AChR 97%
BMY 7378 ++

5-HT1D, pIC50: 5.9

5-HT1A, pIC50: 6.4

 		+

5-HT2, pIC50: 5.5

 		97%
Flibanserin +++

5-HT1A, Ki: 1 nM

 		+

5-HT2A, Ki: 49 nM

 		98%
LY310762 +

5-HT1D, Ki: 249 nM

 		99%+
Cyclobenzaprine HCI ✔ 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

 		98% HPLC
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

 		99+%
Olanzapine ✔ 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

 		99%
Ketanserin +++

5-HT2C (Rat), Ki: 50 nM

5-HT2C (Human), Ki: 2.5 nM

 		99%+
Loxapine succinate ++

5-HT2 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 nM

 		99%
Agomelatine ✔ 98%
Clozapine ✔ 98%
Amitriptyline +

5-HT2, Ki: 235 nM

 		SERT 98%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

 		98+%
RS-127445 ++++

5-HT2B, pKi: 9.5

5-HT2B, pIC50: 10.4

 		99%+
Sarpogrelate HCl ++++

5-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 nM

 		98%
Tropisetron ✔ 99%
Palonosetron ✔ 98+%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

 		98%
Ondansetron ✔ 99%
Granisetron ✔ 98%
Alosetron HCl ✔ 98%
Ondansetron hydrochloride dihydrate ✔ 98%
VUF10166 ++++

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

 		99%+
Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

 		98%
Asenapine maleate +++

5-HT1A, pKi: 8.6

5-HT1B, pKi: 8.4

 		++++

5-HT2C, pKi: 10.46

5-HT2A, pKi: 9.75

 		+++

5-HT5A, pKi: 8.84

 		++++

5-HT6, pKi: 9.6

 		++++

5-HT7, pKi: 9.94

 		97%
Risperidone ++

5-HT1B, Ki: 14.9 nM

5-HT1D, Ki: 84.6 nM

 		++++

5-HT2A, Ki: 61.9 nM

5-HT2C, Ki: 12 nM

 		+

5-HT5A, Ki: 206 nM

 		++

5-HT7, Ki: 6.6 nM

 		98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

 		99%+
Intepirdine ++++

5-HT6, pKi: 9.63

 		99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

 		98+%
BRL 15572 ++

5-HT1D, pKi: 6

5-HT1B, pKi: 6.1

 		++

5-HT2B, pKi: 6.2

5-HT2A, pKi: 6.6

 		+

5-HT6, pKi: 5.9

 		+

5-HT7, pKi: 6.3

 		98%
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。
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 (human), Ki: 24 nM

D2 receptor (bovine), Ki: 26 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。

Risperidone 生物活性

靶点

  • 5-HT2

    5-HT2A, Ki:61.9 nM

    5-HT2C, Ki:12 nM

  • 5-HT1

    5-HT1B, Ki:14.9 nM

    5-HT1D, Ki:84.6 nM

  • 5-HT5

    5-HT5A, Ki:206 nM

  • 5-HT7

    5-HT7, Ki:6.6 nM
描述 Risperidone, with high affinity at dopamine D2 and serotonin 5-HT2 receptors, is mainly used as an antipsychotic drug[3]. In vitro studies, it was found that risperidone showed higher affinity for 5-HT2A- than for D2-receptors in animal brain or cloned (human) receptors[4]. In vivo studies, risperidone could markedly decrease locomotor activity in developing and adult rats immediately, when injected separately with 1.0 and 3.0 mg/kg, also, the emergence of compensatory hyperactivity during long-term risperidone administration is delayed in developing rats in comparison with adult rats[5]. In addition, risperidone wouldn’t produce severely impair behavior for male Sprague-Dawley rats, when given 0.04 mg/day encompassing the peri-adolescent to adolescent timeframe, while could result in a working memory deficit[6].

Risperidone 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
NCT02758067 Schizophrenia Phase 3 Withdrawn(This study was withd... 展开 >>rawn for administrative reasons. There were no safety concerns.) 收起 << - -
NCT01788774 Schizophrenia ... 展开 >> Schizoaffective Disorder 收起 << Phase 1 Completed - -
NCT00236444 Attention Deficit and Disrupti... 展开 >>ve Behavior Disorders 收起 << Phase 3 Completed - -

Risperidone 参考文献

[1]Tarazi FI, Zhang K, et al. Long-term effects of olanzapine, risperidone, and quetiapine on dopamine receptor types in regions of rat brain: implications for antipsychotic drug treatment. J Pharmacol Exp Ther. 2001 May;297(2):711-7.

[2]Angelucci F, Mathe AA, et al. Brain-derived neurotrophic factor and tyrosine kinase receptor TrkB in rat brain are significantly altered after haloperidol and risperidone administration. J Neurosci Res. 2000 Jun 15;60(6):783-94.

[3]Knable MB, Heinz A, Raedler T, Weinberger DR. Extrapyramidal side effects with risperidone and haloperidol at comparable D2 receptor occupancy levels. Psychiatry Res. 1997 Sep 29;75(2):91-101. doi: 10.1016/s0925-4927(97)00023-1. PMID: 9351491.

[4]Schotte A, Bonaventure P, Janssen PF, Leysen JE. In vitro receptor binding and in vivo receptor occupancy in rat and guinea pig brain: risperidone compared with antipsychotics hitherto used. Jpn J Pharmacol. 1995 Dec;69(4):399-412. doi: 10.1254/jjp.69.399. PMID: 8786644.

[5]Stevens RM, Gannon MA, Griffith MS, Bardgett ME. Delayed yet persistent effects of daily risperidone on activity in developing rats. Behav Pharmacol. 2016 Aug;27(5):460-9. doi: 10.1097/FBP.0000000000000230. PMID: 26960160; PMCID: PMC4935566.

[6]Boman L, De Butte M. Neurobehavioral effects of chronic low-dose risperidone administration in juvenile male rats. Behav Brain Res. 2019 May 2;363:155-160. doi: 10.1016/j.bbr.2019.02.009. Epub 2019 Feb 5. PMID: 30735760.

Risperidone 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.18mL

2.44mL

1.22mL

24.36mL

4.87mL

2.44mL

Risperidone 技术信息

CAS号106266-06-2
分子式C23H27FN4O2
分子量 410.485
别名 利哌酮 ;R 64 766;Apexidone;Psychodal
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: 9 mg/mL(21.93 mM)，配合低频超声，并水浴加热至45℃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 10% DMSO+water 0.5 mg/mL clear

PO 0.5% CMC-Na 51 mg/mL suspension

Tags: Risperidone | 106266-06-2 | R 64 766 | GPCR/G Protein | Neuronal Signaling | Membrane Transporter/Ion Channel | 5-HT Receptor | Dopamine Receptor | P-glycoprotein | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Risperidone 纯度/质量文件 | Risperidone 亚型比较 | Risperidone 生物活性 | Risperidone 临床数据 | Risperidone 参考文献 | Risperidone 实验方案 | Risperidone 技术信息

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