产品
编 号:F485479
分子式:C17H24N2O2
分子量:288.38
产品类型
结构图
CAS No: 862896-30-8
联系客服
产品详情
生物活性:
S 38093 is a brain-penetrant, orally active antagonist of H3 receptor, with Kis of 8.8, 1.44 and 1.2 μM for rat, mouse and human H3 receptors, respectively.
体内研究:
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?0.01), with a significant effect from 50 to 80 in APPSWETG 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.
体外研究:
In cellular models, S 38093 is 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). 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 μM, respectively).