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S 38093

CAS No. : 862896-30-8

MCE 站：S 38093

产品活性：S 38093 是一种可透过大脑的，具有口服活性的 H3 receptor 拮抗剂，对大鼠，小鼠和人的 H3 受体具有不同的亲和力，K_i 值分别为 8.8，1.44 和 1.2 ?M。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation

作用靶点：Histamine Receptor

In Vitro: In cellular models, S 38093 is able to antagonize mice H3 receptors (K_B=0.65 ?M) and to suppress cAMP decrease induced by an H3 agonist via human H3 receptors (K_B=0.11 ?M). In cells expressing a high H3 density, S 38093 behaves as a moderate inverse agonist at rat and human H3 receptors (EC₅₀=9 and 1.7 ?M, respectively).

In Vivo: S 38093 (0.3 and 3?mg/kg/d p.o., 28 days) significantly increases proliferation of progenitors in the DG of hippocampus in young adult mice. S 38093 (0.3?mg/kg/d) treatment significantly increases the number of DCX⁺ cells with tertiary dendrites. S 38093 (0.3, 1 and/or 3?mg/kg) significantly increases cell proliferation, survival, and maturation in the DG of hippocampus in aged mice relative to vehicle. S 38093 (3?mg/kg/d p.o., 28 days) increases cell proliferation and has a strong effect on cell survival, also increases the dendritic intersections in both genotypes (one-way ANOVA with repeated measure, p?TG mice only. In aged mice, chronic administration of S 38093 (1 and/or 3?mg/kg/day p.o., 28 days) reverses this age-dependent decrease in BDNF-IX, BDNF-IV and BDNF-I transcripts. In addition, S 38093 at three tested doses (0.3, 1 and 3?mg/kg/d) increases VEGF transcripts compared to vehicle-aged group. In mice, S 38093 significantly increases ex vivo N-tele-Methylhistamine cerebral levels from 3 mg/kg p.o. and antagonized R-α-Methylhistamine-induced dipsogenia from 10 mg/kg i.p.

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