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  • S 38093
    • S38093;S-38093;S38093(Free base)
    货号: abs814469
    CAS号: 862896-30-8
    分子式: C17H24N2O2
    产品说明书
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    货号-规格 货期 价格 数量
    abs814469-5mg 1-2周 ¥1766.00
    - +
    abs814469-10mg 1-2周 ¥2818.00
    - +
    大包装询价
    产品描述
    描述

    S 38093 is a histamine H3 antagonist/inverse agonist with a moderate affinity for rat, mouse and human H3 receptors (Ki = 8.8, 1.44 and 1.2 μM, respectively) and no affinity for other histaminergic receptors. 

    纯度
    >98%
    储存/保存方法
    Store at -20°C
    基本信息
    别名
    S38093;S-38093;S38093(Free base)
    外观
    白色或类白色固体
    可溶性/溶解性
    DMSO :57 mg/mL (197.66 mM)
    生物活性
    靶点
    Human H3 receptor,Mouse H3 receptor,Rat H3 receptor,H3
    In vitro(体外研究)
    In cellular models, the compound was able to antagonize mice H3 receptors (KB = 0.65 μM) and to suppress cAMP decrease induced by an H3 agonist via human H3 receptors (KB = 0.11 μM). Among the four histaminergic receptor subtypes, S 38093 is selective for the H3 receptor, its binding affinity for H1, H2 and H4 receptors being negligible.
    In vivo(体内研究)
    S 38093, a novel brain-penetrant antagonist/inverse agonist of H3 receptors, on AHN (proliferation, maturation and survival) in 3-month-old and in aged 16-month-old mice. In aged animals, S 38093 induced a reversal of age-dependent effects on hippocampal brain-derived neurotrophic factor (BDNF) BDNF-IX, BDNF-IV and BDNF-I transcripts and increased vascular endothelial growth factor (VEGF) expression. The effects of chronic administration of S 38093 were assessed on a neurogenesis-dependent “context discrimination (CS) test” in aged mice. While ageing altered mouse CS, chronic S 38093 treatment significantly improved CS. Chronic S 38093 treatment increases adult hippocampal neurogenesis and may provide an innovative strategy to improve age-associated cognitive deficits. S 38093 is found to be active at a mean pharmacological dose of 0.3–1 mg/kg p.o./i.p. in animal behavioral tests of working memory (Morris water maze in rats; spontaneous alternation and concurrent serial alternation tests in mice; delayed matching to sample in aged monkeys) and episodic-like memory (social and object recognition tests in rats; contextual discrimination task in mice). S 38093 also improves attention, executive functioning, and cognitive flexibility in MPTP-treated monkeys. Moreover, in line with its H3 antagonist/inverse agonist properties, S 38093 dose-dependently increases extracellular histamine levels in the prefrontal cortex and facilitates cholinergic transmission in the prefrontal cortex and hippocampus of rats after both acute and chronic administrations. S 38093 was rapidly absorbed in mouse and rat (Tmax= 0.25-0.5h), slowly in monkey (2h), with a bioavailability ranging from 20 to 60% and t1/2 ranging from 1.5h to 7.4h. The compound was widely distributed with a moderate volume of distribution and low protein binding. The brain distribution of S 38093 was rapid and high.
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