Risperidone

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Chemical Structure| 106266-06-2 同义名 : 利哌酮 ;R 64 766; Apexidone; Psychodal
CAS号 : 106266-06-2
货号 : A324792
分子式 : C23H27FN4O2
纯度 : 98%
分子量 : 410.48
MDL号 : MFCD00274576
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -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
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].
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NCT02758067 Schizophrenia Phase 3 Withdrawn(This study was withd...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 - -
实验方案
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
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.