S-38093

Research use only, not for human use.

S-38093 is a brain-penetrant antagonist of the H3 receptor (Ki: 8.8/1.44/1.2 μM, for rat/mouse/human).

S-38093 is a brain-penetrant antagonist of the H3 receptor (Ki: 8.8/1.44/1.2 μM, for rat/mouse/human).(In Vitro):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).(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 < 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.

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).

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?

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Others

Other Targets

Human H3 receptor| Mouse H3 receptor| Rat H3 receptor

Neurological Disease

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862896-30-8

288.38

C17H24N2O2

>98% (HPLC)

DMSO : 15 mg/mL. 52.01 mM;

NC(=O)c1ccc(OCCCN2CC3CCCC3C2)cc1

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(-20℃)

With Ice Pack

≥ 2 years