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CAS No.: 862896-30-8

S 38093 Catalog No. CSN21281

Synonyms: S 38093

S 38093 is a brain-penetrant antagonist/inverse agonist of H3 receptors.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述S 38093 is a novel Histamine H3 receptor inverse agonist with Ki of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively^[1]. S 38093 (0.3, 1 and/or 3 mg/kg) significantly increased cell proliferation, survival, and maturation in the dentate gyrus of hippocampus in aged mice relative to vehicle, and high doses of S 38093 also increased the maturation of newborn neurons. Chronic administration of S 38093 (3 mg/kg/d p.o., 28 days) administration also increased the dendritic intersections in Alzheimer's disease transgenic mice: APPSWE^WT and APPSWE^Tg^[2]. Donepezil and S 38093 (at 0.1, 0.3, and 1.0 mg/kg) induced a dose-dependent synergistic memory-enhancing effect in middle-aged mice, which is mediated by its action on the septo-hippocampal circuitry, since it canceled out the reduction of CREB phosphorylation (pCREB) observed in these brain areas in vehicle-treated middle-aged animals^[3].
参考文献

[1] Sors A, Panayi F, Bert L, et al. Mechanistic characterization of S 38093, a novel inverse agonist at histamine H3 receptors. Eur J Pharmacol. 2017;803:11‐23.
[2] Guilloux JP, Samuels BA, Mendez-David I, et al. S 38093, a histamine H3 antagonist/inverse agonist, promotes hippocampal neurogenesis and improves context discrimination task in aged mice. Sci Rep. 2017;7:42946.
[3] Sors A, Krazem A, Kehr J, et al. The Synergistic Enhancing-Memory Effect of Donepezil and S 38093 (a Histamine H3 Antagonist) Is Mediated by Increased Neural Activity in the Septo-hippocampal Circuitry in Middle-Aged Mice. Front Pharmacol. 2016;7:492.

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
- 3.4676 mL
- 17.3380 mL
- 34.6759 mL
- 5 mM
- 0.6935 mL
- 3.4676 mL
- 6.9352 mL
- 10 mM
- 0.3468 mL
- 1.7338 mL
- 3.4676 mL

技术信息

CAS号

862896-30-8

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H24N2O2

运输

蓝冰

分子量

288.38

别名

S 38093

溶解度

DMSO	57.0 mg/mL (197.7 mM)
Water	Insoluble
Ethanol	57.0 mg/mL (197.7 mM)

动物实验配方

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