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/ Risperidone/利培酮

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

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

Risperidone是一种多靶点抗精神病药，对 5-HT2A 和 D2 受体、α1、α2 受体和 H1 受体有较高亲和力。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
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Risperidone/利培酮 化学结构 CAS号：106266-06-2
Risperidone/利培酮 化学结构
CAS号：106266-06-2
Risperidone/利培酮 3D分子结构
CAS号：106266-06-2
Risperidone/利培酮 化学结构 CAS号：106266-06-2
Risperidone/利培酮 3D分子结构 CAS号：106266-06-2
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Risperidone/利培酮 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:

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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 ✔ 99%
Fluvoxamine maleate ✔ 99%
Iloperidone ✔ 99%
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 ✔ 97%
Sertraline HCl ++

5-HT, Ki: 13 nM

 		98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

 		98%
Latrepirdine 2HCl ✔ GluR 99%
Fluoxetine HCl ✔ 99.5%
Paroxetine HCl ✔ AChR 99%
BMY 7378 ++

5-HT1A, pIC50: 6.4

5-HT1D, pIC50: 5.9

 		+

5-HT2, pIC50: 5.5

 		97%
Flibanserin +++

5-HT1A, Ki: 1 nM

 		+

5-HT2A, Ki: 49 nM

 		95%
LY310762 +

5-HT1D, Ki: 249 nM

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

5-HT2, Ki: 3.98 nM

 		99%
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

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

5-HT2A, pIC50: 8.7

 		99%
Ketanserin +++

5-HT2C (Human), Ki: 2.5 nM

5-HT2C (Rat), Ki: 50 nM

 		99%+
Loxapine succinate ++

5-HT2 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 nM

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

5-HT2, Ki: 235 nM

 		SERT 99%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

 		98+%
RS-127445 ++++

5-HT2B, pIC50: 10.4

5-HT2B, pKi: 9.5

 		99%+
Sarpogrelate HCl ++++

5-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 nM

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

5-HT3 receptor, Ki: 0.091 nM

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

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

 		99%+
Azasetron HCl ++++

5-HT3, IC50: 0.33 nM

 		99%
Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

 		++++

5-HT2A, pKi: 9.75

5-HT2C, pKi: 10.46

 		+++

5-HT5A, pKi: 8.84

 		++++

5-HT6, pKi: 9.6

 		++++

5-HT7, pKi: 9.94

 		97%
Risperidone ++

5-HT1D, Ki: 84.6 nM

5-HT1B, Ki: 14.9 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-HT2A, pKi: 6.6

5-HT2B, pKi: 6.2

 		+

5-HT6, pKi: 5.9

 		+

5-HT7, pKi: 6.3

 		95%
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

 		99%
Tetrahydroberberine +

D2 receptor, pKi: 6.08

 		98+%
Prochlorperazine Maleate ✔ 98% (HPLC)
Olanzapine ✔ 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

 		98%
Ropinirole HCl ++

D2 receptor, Ki: 29 nM

 		99%
Lurasidone ++++

D2 receptor, Ki: 1 nM

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

D2 receptor, Ki: 1.4 nM

 		99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

 		99%
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 ✔ 99%
Pimethixene maleate ++

Dopamine D1 Receptor, pKi: 6.37

 		+++

Dopamine D2 Receptor, pKi: 8.19

 		++

Dopamine D4.4 Receptor, pKi: 7.54

 		97%
Loxapine succinate ++

D2 receptor (Human), Ki: 62 nM

D1 receptor (human), Ki: 26 nM

 		++

D2 receptor (human), Ki: 24 nM

D2 receptor (bovine), Ki: 26 nM

 		+++

D4 receptor (human), Ki: 7.5 nM

 		98%
Chlorprothixene +++

D1 receptor, Ki: 18 nM

 		+++

D2 receptor, Ki: 2.96 nM

 		+++

D3 receptor, Ki: 4.56 nM

 		+++

D5 receptor, Ki: 9 nM

 		99%
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/利培酮 生物活性

靶点

  • 5-HT2

    5-HT2A, Ki:61.9 nM

    5-HT2C, Ki:12 nM

  • 5-HT1

    5-HT1D, Ki:84.6 nM

    5-HT1B, Ki:14.9 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/利培酮 细胞实验

Cell Line
Concentration Treated Time Description References
MC3T3-E1 cells 150 µM 48 hours To investigate the effects of Risperidone on differentiation, autophagy, and apoptosis of MC3T3-E1 cells. Results showed that Risperidone inhibited differentiation and autophagy, and promoted apoptosis of MC3T3-E1 cells. Mol Med. 2022 May 3;28(1):46.

Risperidone/利培酮 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Neonatal ventral hippocampus lesion (NVHL) model Intraperitoneal injection 0.25 mg/kg Once daily for 21 consecutive days Risperidone ameliorated neural atrophy and oxidative/nitrosative stress in the prefrontal cortex of NVHL rats and improved behavioral abnormalities. J Neurosci. 2019 Oct 23;39(43):8584-8599
Mice DISC1 mutated Mice model Intranasal administration 0.25µg/5µl/per Mice Once daily for one month Risperidone significantly improved the performance of DISC1 mutated mice in the object recognition test but did not reduce their anxiety behavior. Sci Rep. 2015 Nov 10;5:16300
Sprague-Dawley rats Autism Spectrum Disorder (ASD) rat model Oral 0.5 mg/kg Once daily for 30 days Risperidone treatment significantly improved VPA-induced ASD-like behavioral deficits, including social impairment, repetitive behaviors, and anxiety. Psychopharmacology (Berl). 2023 Jun;240(6):1313-1332
C57BL/6J mice Osteoporosis model Oral 0.75 mg/kg 4 weeks To investigate the effects of Risperidone on femur tissues in mice. Results showed that Risperidone inhibited autophagy and promoted apoptosis in femur tissues, leading to bone loss. Mol Med. 2022 May 3;28(1):46.
Long Evans rats Maternal-offspring interactions and juvenile play fighting model Subcutaneous injection 1.0 or 3.0 mg/kg Once daily from postnatal day 14 to 42 To assess the effects of risperidone on maternal-offspring interactions and juvenile play fighting. Results showed that risperidone significantly suppressed several aspects of maternal-offspring interactions at one-hour post-injection, and at 23 hours post-injection, pups administered risperidone had lower activity scores and made fewer non-nursing contacts with their moms. In play-fighting observations, risperidone profoundly decreased many forms of social interaction at one hour post-injection, and at 23 hours post-injection, rats administered risperidone made more non-social contacts with their cage mates, but engaged in less social grooming. Pharmacol Biochem Behav. 2015 Mar;130:90-6
C57BL6/J mice Cuprizone-induced acute demyelination model Oral gavage 2 mg/kg Once daily for five weeks To evaluate the protective effect of risperidone on cuprizone-induced demyelination, results showed that risperidone significantly improved motor performance and sensitivity to a cold stimulus, and reduced myelin degradation. Int J Mol Sci. 2021 Jul 2;22(13):7183.
C57BL/6J mice Wild-type mice Oral administration in drinking water 80 μg/day Continuous treatment for 58 days To investigate the mechanism of risperidone-induced weight gain via gut microbiome alterations, showing reduced energy expenditure and weight gain. EBioMedicine. 2015 Nov;2(11):1725-34

Risperidone/利培酮 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/利培酮 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/利培酮 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/利培酮 技术信息

CAS号106266-06-2
分子式C23H27FN4O2
分子量 410.48
SMILES Code O=C1C(CCN2CCC(CC2)C3=NOC4=C3C=CC(F)=C4)=C(N=C5N1CCCC5)C
MDL No. MFCD00274576
别名 利哌酮 ;R 64 766; Apexidone; Psychodal
运输蓝冰
InChI Key RAPZEAPATHNIPO-UHFFFAOYSA-N
Pubchem ID 5073
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

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/利培酮 纯度/质量文件 | Risperidone/利培酮 亚型比较 | Risperidone/利培酮 生物活性 | Risperidone/利培酮 临床数据 | Risperidone/利培酮 参考文献 | Risperidone/利培酮 实验方案 | Risperidone/利培酮 技术信息

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