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  • Olanzapine
  • 奧氮平;LY170053
  • 貨號: abs817970
    CAS號: 132539-06-1
    分子式: C17H20N4S
    分子量: 312.44
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    貨號-規格 貨期 價格 數量
    abs817970-25mg 現貨 ¥294.00
    - +
    abs817970-100mg 現貨 ¥788.00
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    ! 該貨號為 abs47030106 的新貨號。
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    產品描述
    描述

    Olanzapine is an atypical antipsychotic that is used currently in the treatment of schizophrenia and bipolar illness.

    純度
    99%
    儲存/保存方法
    Store at -20°C
    基本信息
    別名
    奧氮平;LY170053
    外觀
    黃色粉末
    可溶性/溶解性
    1eq. HCl : 31.2 mg/mL (100 mM)

    DMSO : 31.2 mg/mL (100 mM)
    生物活性
    靶點
    5-HT2 ,D2 receptor
    In vitro(體外研究)
    Olanzapine interacts with key receptors of interest in schizophrenia, having a nanomolar affinity for dopaminergic, serotonergic, alpha 1-adrenergic, and muscarinic receptors. Olanzapine has a receptor profile that is similar to that of clozapine: it is relatively nonselective at dopamine receptor subtypes and it shows selectivity for mesolimbic and mesocortical over striatal dopamine tracts (electrophysiology; Fos).
    In vivo(體內研究)
    Olanzapine is a potent antagonist at DA receptors (DOPAC levels; pergolide-stimulated increases in plasma corticosterone) and 5-HT receptors (quipazine-stimulated increases in corticosterone), but is weaker at alpha-adrenergic and muscarinic receptors. Olanzapine combined with fluoxetine produces robust, sustained increases of extracellular levels of dopamine ((ex)) and norepinephrine ((ex)) up to 361% and 272% of the baseline in rat prefrontal cortex, respectively, which are significantly greater than either drug alone. Olanzapine at 0.5 mg/kg, 3 mg/kg and 10 mg/kg (s.c.) dose-dependently increases the extracellular dopamine (DA) and norepinephrine (NE) levels in rat prefrontal cortex, nucleus accumbens and striatum. Olanzapine also increases extracellular levels of a DA metabolite, DOPAC, and tissue concentrations of a released DA metabolite, 3-methoxytyramine. Olanzapine results in an 8-11% reduction in mean fresh brain weights as well as left cerebrum fresh weights and volumes in macaque monkeys. Olanzapine results in substantial increases in adiposity: increased total body fat reflecting marked increases in subcutaneous and visceral adipose stores. Olanzapine results in marked hepatic insulin resistance.
    參考文獻
    參考文獻
    [1] Bymaster FP, et al. J Clin Psychiatry, 1997, 58, 28-36.
    [2] Moore, N.A., et al.: Curr. Opin Invest. Drugs, 2, 281 (1993)
    [3] Baldwin, D.S. and Montgomery, S.A.: Int. Clin. Psychopharmacol., 10, 239 (1995)
    [4] Tohen, M., et al.: Am. J. Psychiatry, 156, 702 (1999)
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