Agomelatine是人和猪的5-HT2C受体竞争性拮抗剂,pKi分别为6.2和6.4。
Agomelatine is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.
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] Dagytė G, et al. Behav Brain Res, 2011, 218(1), 121-128.
[2] Dan J Stein et. Al. Journal of Clinical Psychiatry, 73(7), 1002-1008 (2012).
[3] Dan J Stein et. Al. Journal of Clinical Psychiatry, 75(4), 362-368 (2014)
分子式 C15H17NO2 |
分子量 243.3 |
CAS号 138112-76-2 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 50 mg/mL |
Water <1 mg/mL |
Ethanol 50 mg/mL |
体内溶解度
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NCT00467402 | Major Depressive Disorder | Drug: agomelatine|Drug: placebo | Novartis | Phase 3 | 2007-04-01 | 2012-05-02 |
NCT00411242 | Major Depressive Disorder (MDD) | Drug: agomelatine|Drug: placebo | Novartis | Phase 3 | 2006-12-01 | 2012-05-02 |
NCT00411099 | Major Depressive Disorder | Drug: agomelatine|Drug: placebo | Novartis | Phase 3 | 2006-12-01 | 2012-05-02 |
NCT01459250 | Renal Impairment | Drug: AGO178C | Novartis Pharmaceuticals|Novartis | Phase 1 | 2011-03-01 | 2011-10-21 |
NCT01110902 | Major Depressive Disorder | Drug: Agomelatine (AGO178C)|Drug: Placebo | Novartis Pharmaceuticals|Novartis | Phase 3 | 2010-05-01 | 2012-09-19 |
NCT01110889 | Major Depressive Disorder | Drug: Agomelatine (AGO178C)|Drug: Agomelatine (AGO178C)|Drug: Placebo | Novartis Pharmaceuticals|Novartis | Phase 3 | 2010-05-01 | 2013-02-21 |
NCT00451490 | Depressive Disorder, Major | Drug: Agomelatine|Drug: Fluoxentine | National Taiwan University Hospital | 2006-10-01 | 2007-12-24 | |
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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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