JNJ-5207852
货号：
11998-50mg 基本售价：
8064.0 元 规格：
50 mg
产品信息
概述| 货号 | 11998-50mg |
| 描述 | Histamine has been implicated in a variety of biological functions including thermo- and immunoregulation, food intake, hyperexcitability, pain transmission, arousal, reward, memory, and emotional responses. The histamine H3 receptor is a Gi-coupled presynaptic auto- and hetero-receptor whose activation leads to a decreased release of histamine, glutamate, norepinephrine, and acetylcholine in the brain. H3R antagonists are expected to increase the release of these neurotransmitters, which may contribute therapeutic benefit in diseases characterized by sleep/wake disturbances or cognitive disorders.1,2 JNJ-5207852 is a selective, non-imidazole histamine H3R antagonist with high affinity at the rat (pKi = 8.9) and human (pKi = 9.24) H3 receptors.3 In rodents, 1-10 mg/kg JNJ-5207852 administered subcutaneously increases time spent awake and decreases REM sleep and slow-wave sleep.3 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Tiligada, E.,Zampeli, E.,Sander, K., et al. Histamine H3 and H4 receptors as novel drug targets. Expert Opinion on Investigational Drugs 18(10), 1519-1532 (2009).
2.Barbier, A.J.,Dugovic, B.C.,Laposky, A.D., et al. Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. British Journal of Pharmacology 143, 649-661 (2004).
3.Esbenshade, T.A.,Browman, K.E.,Bitner, R.S., et al. The histamine H3 receptor: An attractive target for the treatment of cognitive disorders. British Journal of Pharmacology 154, 1166-1181 (2008).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 316.5 |
| 分子式 | C20H32N2O |
| CAS号 | 398473-34-2 |
| 稳定性 | ≥ 1 year |
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