Asenapine

阿塞那平,Org 5222,Saphris maleate,Org-5222 maleate,Org5222 maleate

Asenapine马来酸盐能抑制肾上腺素受体,对α1,α2A,α2B和α2C的Ki为0.25-1.2 nM,还能抑制 5-HT受体,对1A,1B,2A,2B,2C,5A,6和7的Ki为0.03-4.0 nM。

目录号
EY0586
EY0586
EY0586
EY0586
纯度
99.34%
99.34%
99.34%
99.34%
规格
5 mg
10 mg
50 mg
100 mg
原价
220
420
1000
1850
售价
220
420
1000
1850
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Asenapine is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm系数


    例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。


  • 参考文献

    [1] Shahid M, et al. J Psychopharmacol,?009, 23(1), 65-73.
    [2] Tarazi FI, Shahid M. Asenapine maleate: a new drug for the treatment of schizophrenia and bipolar mania. Drugs Today (Barc). 2009 Dec;45(12):865-76.
    [3] Potkin SG. Asenapine: a clinical overview. J Clin Psychiatry. 2011;72 Suppl 1:14-8.

    分子式
    C21H20ClNO5
    分子量
    401.84
    CAS号
    85650-56-2
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    >80 mg/mL
    Water
    <1 mg/mL
    Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01460290 Bipolar Disorder Drug: Asenapine University Hospitals Cleveland Medical Center|Case Western Reserve University Phase 4 2011-10-01 2014-12-08
    NCT01587118 Posttraumatic Stress Disorder Drug: Adjunctive asenapine Lori Davis, MD|Merck Sharp & Dohme Corp.|Forest Laboratories|Tuscaloosa Research & Education Advancement Corporation Phase 4 2012-06-01 2016-10-12
    NCT01549041 Schizophrenia Drug: Asenapine 10 mg daily in the evening|Drug: Asenapine 5 mg twice daily Duke University|Merck Sharp & Dohme Corp. Phase 4 2012-04-01 2014-04-23
    NCT01190267 Schizophrenia, Paranoid|Schizophrenia, Disorganized|Schizophrenia, Undifferentiated Drug: asenapine Merck Sharp & Dohme Corp. Phase 3 2010-09-01 2015-08-04
    NCT00281320 Psychosis Drug: Asenapine Merck Sharp & Dohme Corp. Phase 3 2006-02-01 2015-02-20
    NCT01395992 Bipolar I Disorder Drug: asenapine|Drug: asenapine Forest Laboratories Phase 3 2012-04-01 2015-05-26
    NCT00143182 Bipolar Disorder Drug: Asenapine|Drug: Olanzapine Merck Sharp & Dohme Corp.|Pfizer Phase 3 2005-01-01 2015-05-15
    NCT01396291 Bipolar 1 Disorder Drug: asenapine|Drug: placebo Forest Laboratories Phase 3 2011-12-01 2015-12-03
    NCT01349907 Bipolar Disorder Drug: Asenapine|Drug: Rescue medication Merck Sharp & Dohme Corp. Phase 3 2011-06-01 2016-09-13
    NCT01684657 Stuttering Drug: Asenapine University of California, Irvine|Merck Sharp & Dohme Corp. Phase 3 2012-09-01 2014-05-19
    NCT00145509 Bipolar Disorder Drug: Asenapine|Drug: Placebo Merck Sharp & Dohme Corp. Phase 3 2005-08-01 2015-01-07
    NCT01190254 Schizophrenia, Paranoid|Schizophrenia, Disorganized|Schizophrenia, Undifferentiated Drug: asenapine 2.5 mg|Drug: asenapine 5.0 mg|Drug: placebo Merck Sharp & Dohme Corp. Phase 3 2010-09-01 2015-08-04
    NCT01807741 Bipolar Depression Drug: Asenapine|Drug: Placebo University of Cincinnati|University of Louisville|Merck Sharp & Dohme Corp. Phase 2 2013-09-01 2016-05-09
    NCT00159783 Bipolar Disorder Drug: asenapine|Drug: Olanzapine Merck Sharp & Dohme Corp.|Pfizer Phase 3 2005-07-01 2015-02-06
    NCT01400113 Agitation Drug: Asenapine|Drug: Placebo St. Joseph Hospital Health Center|Schering-Plough Phase 4 2012-04-01 2016-04-26
    NCT00145470 Bipolar Disorder Drug: Asenapine|Drug: placebo Merck Sharp & Dohme Corp. Phase 3 2005-06-01 2015-04-21
    NCT00764478 Bipolar 1 Disorder Drug: Asenapine|Drug: Asenapine|Drug: Placebo Merck Sharp & Dohme Corp. Phase 3 2012-04-01 2015-11-24
    NCT01206517 Schizophrenia|Bipolar I Disorder Drug: Asenapine 2.5 mg|Drug: Asenapine 5 mg|Drug: Asenapine 10 mg Merck Sharp & Dohme Corp. Phase 1 2010-07-01 2015-10-29
    NCT01244815 Bipolar Disorder, Pediatric Drug: asenapine|Drug: Placebo to match asenapine|Drug: Rescue medication Merck Sharp & Dohme Corp. Phase 3 2011-06-01 2015-08-25
    NCT01101464 Schizophrenia|Schizoaffective Disorder Drug: Asenapine 3x5mg followed by 1x15mg|Drug: Asenapine 1x15mg followed by 3x5mg Merck Sharp & Dohme Corp. Phase 2 2002-10-01 2015-10-30
    NCT01142596 Schizophrenia Drug: Asenapine|Drug: Placebo Merck Sharp & Dohme Corp.|Meiji Seika Pharma Co., Ltd. Phase 3 2010-05-01 2016-05-24
    NCT01244828 Schizophrenia Drug: Asenapine Merck Sharp & Dohme Corp. Phase 3 2011-04-01 2015-07-30
    NCT01670019 Major Depressive Disorder Without Psychotic Features Drug: Asenapine 5-20 mg daily|Drug: Placebo 1-4 tablets daily Duke University|Merck Sharp & Dohme Corp. Phase 4 2012-10-01 2015-08-31

    注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。

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