Agomelatine

阿戈美拉汀,阿戈美拉丁,S-20098,S 20098,S20098,

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。

目录号
EY0374
EY0374
EY0374
EY0374
EY0374
纯度
99.27%
99.27%
99.27%
99.27%
99.27%
规格
1 mg
5 mg
10 mg
50 mg
100 mg
原价
210
432
685
1900
3100
售价
210
432
685
1900
3100
库存
现货
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Agomelatine is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.

  • 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] 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

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

    NCT01731899 Major Depression|Fibromyalgia Drug: agomelatine Universidad de Granada 2010-06-01 2014-05-06
    NCT01822418 Schizophrenia|Schizophrenia-spectrum-disorders Drug: agomelatine Central Institute of Mental Health, Mannheim|Servier Phase 4 2013-01-01 2013-03-27
    NCT01483053 Major Depressive Disorder (MDD) Drug: Agomelatine|Drug: Escitalopram Baker IDI Heart and Diabetes Institute|Servier Laboratories (Australia) Pty Ltd|The Alfred|Monash Medical Centre Phase 4 2014-01-01 2013-12-16
    NCT00463242 Major Depressive Disorder Drug: Agomelatine|Drug: paroxetine|Drug: placebo Novartis Phase 3 2007-03-01 2012-05-02
    NCT01108393 Obsessive Compulsive Disorder Drug: Agomelatine A|Drug: Placebo Servier Phase 2 2010-05-01 2014-02-12
    NCT01531309 Hepatic Impairment Drug: AGO178 Novartis Pharmaceuticals|Servier|Novartis Phase 1|Phase 2 2011-02-01 2013-03-06
    NCT01156415 Major Depressive Disorder Drug: AGO178|Drug: AGO178 Novartis Pharmaceuticals|Novartis Phase 3 2010-06-01 2013-03-06
    NCT01488071 Major Depressive Disorder Drug: Vortioxetine (Lu AA21004)|Drug: Agomelatine H. Lundbeck A/S Phase 3 2012-01-01 2014-02-11
    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
    NCT02374567 Dementia|Depression|Schizophrenia|Psychosomatic Disorders|Anxiety Disorders Drug: Phenobarbital|Drug: Phenytoin|Drug: Carbamazepine|Drug: Oxcarbazepine|Drug: Valproic Acid|Drug: Lamotrigine|Drug: Topiramate|Drug: Gabapentin|Drug: Levetiracetam|Drug: Pregabalin|Drug: Lacosamide|Drug: Clonazepam|Drug: Biperiden|Drug: Levomepromazine|Drug: Fluphenazine|Drug: Perphenazine|Drug: Perazine|Drug: Thioridazine|Drug: Haloperidol|Drug: Melperone|Drug: Pipamperone|Drug: Bromperidol|Drug: Benperidol|Drug: Sertindole|Drug: Ziprasidone|Drug: Flupentixol|Drug: Chlorprothixene|Drug: Zuclopenthixol|Drug: Fluspirilene|Drug: Pimozide|Drug: Clozapine|Drug: Olanzapine|Drug: Quetiapine|Drug: Sulpiride|Drug: Tiapride|Drug: Amisulpride|Drug: Prothipendyl|Drug: Risperidone|Drug: Aripiprazole|Drug: Paliperidone|Drug: Diazepam|Drug: Oxazepam|Drug: Lorazepam|Drug: Bromazepam|Drug: Clobazam|Drug: Alprazolam|Drug: Hydroxyzine|Drug: Buspirone|Drug: Chloral Hydrate|Drug: Flurazepam|Drug: Nitrazepam|Drug: Triazolam|Drug: Lormetazepam|Drug: Temazepam|Drug: Midazolam|Drug: Brotizolam|Drug: Zopiclone|Drug: Zolpidem|Drug: Zaleplon|Drug: Melatonin|Drug: Clomethiazole|Drug: Diphenhydramine|Drug: Promethazine|Drug: Imipramine|Drug: Clomipramine|Drug: Opipramol|Drug: Trimipramine|Drug: Amitriptyline|Drug: Nortriptyline|Drug: Doxepin|Drug: Maprotiline|Drug: Amitriptyline oxide|Drug: Fluoxetine|Drug: Citalopram|Drug: Paroxetine|Drug: Sertraline|Drug: Fluvoxamine|Drug: Escitalopram|Drug: Tranylcypromine|Drug: Moclobemide|Drug: Mianserin|Drug: Trazodone|Drug: Mirtazapine|Drug: Bupropion|Drug: Venlafaxine|Drug: Reboxetine|Drug: Duloxetine|Drug: Agomelatine|Drug: Pyritinol|Drug: Piracetam|Drug: Donepezil|Drug: Rivastigmine|Drug: Galantamine|Drug: Memantine|Drug: Nicergoline|Drug: Acamprosate|Drug: Lithium Hannover Medical School Phase 3 2015-01-01 2017-02-23

    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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