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利培酮 /Risperidone 99%+

货号:A324792 同义名: 利哌酮 / R 64 766;Apexidone Ambeed 开学季,买赠积分,赢豪礼

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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Excepted Quantity USD 0.00
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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
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: 99%+
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 (human platelets), IC50: 240 μM

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

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

5-HT, Ki: 77 nM

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

5-HT, Ki: 0.89 nM

99%+
Duloxetine 98+%
Sertraline HCl ++

5-HT, Ki: 13 nM

99%+
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

99%+
Latrepirdine 2HCl GluR 99%+
Fluoxetine hydrochloride 98%
Paroxetine hydrochloride 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

98%
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 (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 99%+
Clozapine 99%+
Amitriptyline +

5-HT2, Ki: 235 nM

SERT 98%
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-HT2A, Kd: 2.1 nM

5-HT2C, Kd: 1.1 nM

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

5-HT3 receptor, Ki: 0.091 nM

99%+
Ondansetron 99%
Granisetron 98%
Alosetron HCl 98%
Ondansetron hydrochloride dihydrate 99%+
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-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

99%+
Risperidone ++

5-HT1D, Ki: 84.6 nM

5-HT1B, Ki: 14.9 nM

++++

5-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 nM

+

5-HT5A, Ki: 206 nM

++

5-HT7, Ki: 6.6 nM

99%+
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-HT1B, pKi: 6.1

5-HT1D, pKi: 6

++

5-HT2A, pKi: 6.6

5-HT2B, pKi: 6.2

+

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 98%+
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 99%+
Sulpiride 99+%
Perospirone ++++

D2 receptor, Ki: 1.4 nM

99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

98+%
Phenothiazine 99%+
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

99%+
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 ++

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

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

99%+
Azaperone 99%+
Ziprasidone HCl 98+%
Paliperidone 99%+
Alizapride HCl 99+%
Amisulpride 99%+
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-HT2C, Ki:12 nM

    5-HT2A, Ki:61.9 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 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

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

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

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