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| 品牌 | absin | CAS | 78246-49-8 |
|---|---|---|---|
| 分子式 | C19H21CIFNO3 | 纯度 | 99% |
| 分子量 | 365.83 | 货号 | abs47027796 |
| 规格 | 100mg | 供货周期 | 现货 |
| 主要用途 | is a antidepressant agents | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Paroxetine hydrochloride 78246-49-8
| 产品描述 | |
| 描述 | Paroxetine Hydrochloride is a antidepressant agents known as selective serotonin-reuptake inhibitors (SSRIs).Paroxetine is a potent and highly selective inhibitor of neuronal serotonin reuptake. Paroxetine likely inhibits the reuptake of serotonin at the |
| 纯度 | 99% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 盐酸帕luo西汀；BRL29060 hydrochloride；BRL29060A |
| 外观 | 白色或类白色结晶性粉末 |
| 可溶性/溶解性 | Ethanol : 35 mg/mL (95.67 mM) Water : 10 mg/mL (27.33 mM) DMSO : 73 mg/mL (199.54 mM) |
| 生物活性 | |
| 靶点 | AChR,5-HT |
| In vitro(体外研究) | Paroxetine apparently exerts their antidepressant activity by increasing the concentration of 5-HT in the extracellular compartment, thereby enhancing serotoninergic neurotransmission. Paroxetine (1-300 μM) results in a concentration-dependent reduction in the firing rate of DRN serotoninergic neurons with IC50 values of 1.4 μM in the ACSF superfusing brain stem slices. Paroxetine is a highly potent inhibitor of desipramine hydroxylation, the inhibition constant (Ki) value of 2.0 mM indicated greater inhibiting potency than fluoxetine or norfluoxetine. Paroxetine is shown to be a potent (Ki = 1.1 nM) and specific inhibitor of -5-hydroxytryptamine (5-HT) uptake into rat cortical and hypothalamic synaptosomes in vitro. Paroxetine demonstrates weak affinity for muscarinic receptors (Ki = 89 nM) but is at least 15 fold weaker than amitriptyline (Ki = 5.1 nM). Paroxetine inactivates CYP2D6 via the formation of a metabolite intermediate complex. |
| In vivo(体内研究) | Paroxetine produces a dose-related inhibition of -5-HT uptake (ED50 = 1.9 mg/kg) into rat hypothalamic synaptosomes ex vivo with little effect on -l-noradrenaline (NA) uptake (ED50 greater than 30 mg/kg). Paroxetine (ED50 1-3 mg/kg PO) prevents the 5-HT depleting effect of p-chloroamphetamine (PCA) in rat brain, demonstrating 5-HT uptake blockade in vivo. |
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| 研究领域 | |
| 研究领域 | Neuroscience CancerTumor immunology Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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