S 38093

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Chemical Structure| 862896-30-8 同义名 : -
CAS号 : 862896-30-8
货号 : A642303
分子式 : C17H24N2O2
纯度 : 98%
分子量 : 288.38
MDL号 : MFCD31560487
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • H3 receptor

    rat H3 receptor, Ki:1.44 μM

    human H3 receptor, Ki:1.2 μM

  • H3 receptor

    rat H3 receptor, Ki:1.44 μM

    human H3 receptor, Ki:1.2 μM

  • H3 receptor

    rat H3 receptor, Ki:1.44 μM

    human H3 receptor, Ki:1.2 μM
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: APPSWEWT and APPSWETg[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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.47mL

0.69mL

0.35mL

17.34mL

3.47mL

1.73mL

34.68mL

6.94mL

3.47mL
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.