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。
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.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km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。
[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
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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