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CAS No.: 398473-34-2

1-(4-(3-(Piperidin-1-yl)propoxy)benzyl)piperidine Catalog No. CSN25273

JNJ-5207852 is a novel, non-imidazole histamine H3 receptor antagonist, with high affinity at the rat (pKi=8.9) and human (pKi=9.24) H3 receptor.

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技术信息

生物活性

描述The H₃ receptor is a G_i-coupled presynaptic auto- and hetero-receptor whose activation leads to a decreased release of neurotransmitter. Its antagonists are thus expected to offer therapeutic benefits in diseases characterized by disturbances of neurotransmission, such as depression, Alzheimer's disease and schizophrenia. JNJ-5207852 is a novel, non-imidazole H₃ receptor antagonist, with high affinity at the rat (pK_i = 8.9) and human (pK_i = 9.24) H₃ receptor. Ex vivo brain autoradiography indicated that JNJ-5207852 penetrates rapidly into the brain and achieves good receptor occupancy. The ED₅₀ for receptor occupancy 1 h after dosing was 0.13 mg/kg. In vivo, JNJ-5207852 elicited a dose-dependent increase in the total time spent awake. This wake-promoting effect was most noticeable at the higher dose, where 10 mg/kg JNJ-5207852 caused an increase in time spent awake that manifested within the first 30 min after dosing and remained present throughout the observation period. The increase in waking was accompanied by significant decreases in the amount of time spent in SWS (slow - wave sleep). Administration of JNJ-5207852 (10 mg/kg) to H₃^+/+ mice significantly increased wakefulness in hours 1 - 2 (+143%, P<0.01), hours 7 - 8 (+153%, P<0.001), hours 11 - 12 (+118%, P<0.05) and hours 22 - 24 (+125%, P<0.01) compared to the vehicle condition. Consequently, the amount of 24-h accumulated wakefulness was greater following JNJ-5207852 administration (P<0.001)^[1].
参考文献

[1] Barbier AJ, Berridge C, Dugovic C, et al. Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist [published correction appears in Br J Pharmacol. 2005 Jan;144(1):145]. Br J Pharmacol. 2004;143(5):649-661

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1597 mL
- 15.7987 mL
- 31.5975 mL
- 5 mM
- 0.6319 mL
- 3.1597 mL
- 6.3195 mL
- 10 mM
- 0.3160 mL
- 1.5799 mL
- 3.1597 mL

技术信息

CAS号

398473-34-2

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H32N2O

运输

蓝冰

分子量

316.48

别名

溶解度

DMSO	75.5 mg/mL (238.6 mM) warming

动物实验配方

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1-(4-(3-(Piperidin-1-yl)propoxy)benzyl)piperidine Catalog No. CSN25273

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