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Asenapine maleate

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Chemical Structure| 85650-56-2 同义名 : 阿塞那平盐酸盐 ;Org 5222 maleate;Org 5222
CAS号 : 85650-56-2
货号 : A504366
分子式 : C21H20ClNO5
纯度 : 97%
分子量 : 401.84
MDL号 : MFCD00900588
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(62.21 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

H2O: 6 mg/mL(14.93 mM)
动物实验配方：
生物活性
靶点

  • α-adrenergic receptor

    α2B-adrenergic receptor, pKi:8.9

    α2A-adrenergic receptor, pKi:8.9

  • 5-HT2

    5-HT2A, pKi:9.75

    5-HT2C, pKi:10.46

  • 5-HT6

    5-HT6, pKi:9.6

  • 5-HT1

    5-HT1A, pKi:8.6

    5-HT1B, pKi:8.4
描述 Asenapine maleate is an antagonist of 5-HT (1a, 1b, 2a, 2b, 2C, 5A, 6, 7) and D2, with Ki values of 0.03-4.0 nm and 1.3 nm, respectively and also an antipsychotic[3]. Asenapine reduced freezing behaviour and increased serotonin release in the rat hippocampus[4]. Asenapine ameliorated this serotonin deficit in a dose-related manner that matched its efficacy for reversing the cognitive deficit[5].In vivo, Asenapine displays robust antimanic property and effective antagonistic activity at 5‐HT 1A/7 receptors[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
NCT02181803 Schizophrenia Phase 1 Completed - -
NCT02600741 - Completed - -
NCT03565068 Schizophrenia Phase 1 Suspended(Study is on hold pen... 展开 >>ding evaluation of emerging preclinical findings) 收起 << October 9, 2019 United States, California ... 展开 >> California Clinical Trials ( Site 0001) Glendale, California, United States, 91206 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.49mL

0.50mL

0.25mL

12.44mL

2.49mL

1.24mL

24.89mL

4.98mL

2.49mL
参考文献

[1]Stoner SC, Pace HA. Asenapine: a clinical review of a second-generation antipsychotic. Clin Ther. 2012 May;34(5):1023-40.

[2]Shahid M, Walker GB, et al. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73.

[3]Shahid M, Walker GB, Zorn SH, Wong EH. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. PMID: 18308814.

[4]Ohyama M, Kondo M, Yamauchi M, Imanishi T, Koyama T. Asenapine reduces anxiety-related behaviours in rat conditioned fear stress model. Acta Neuropsychiatr. 2016 Dec;28(6):327-336. doi: 10.1017/neu.2016.17. Epub 2016 Apr 21. PMID: 27099073.

[5]Elsworth JD, Groman SM, Jentsch JD, Valles R, Shahid M, Wong E, Marston H, Roth RH. Asenapine effects on cognitive and monoamine dysfunction elicited by subchronic phencyclidine administration. Neuropharmacology. 2012 Mar;62(3):1442-52. doi: 10.1016/j.neuropharm.2011.08.026. Epub 2011 Aug 23. PMID: 21875607; PMCID: PMC3711239.

[6]Delcourte S, Abrial E, Etiévant A, Rovera R, Arnt J, Didriksen M, Haddjeri N. Asenapine modulates mood-related behaviors and 5-HT1A/7 receptors-mediated neurotransmission. CNS Neurosci Ther. 2017 Jun;23(6):518-525. doi: 10.1111/cns.12698. Epub 2017 Apr 17. PMID: 28417559; PMCID: PMC6492759.