| Identification | Back Directory | [Name]
s38093 free | [CAS]
862896-30-8 | [Synonyms]
s38093 free S38093 FREE BASE S-38093 free base S38093;S-38093;S 38093 S38093;S-38093;S38093(FREE BASE) Benzamide, 4-[3-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)propoxy]- | [Molecular Formula]
C17H24N2O2 | [MDL Number]
MFCD31560487 | [MOL File]
862896-30-8.mol | [Molecular Weight]
288.38 |
| Chemical Properties | Back Directory | [Boiling point ]
473.5±25.0 °C(Predicted) | [density ]
1.130±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO : 15 mg/mL (52.01 mM) | [form ]
Solid | [pka]
16.34±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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. | [Biological Activity]
S 38093 is a histamine H3 antagonist/inverse agonist with moderate affinity for rat, mouse and human H3 receptors (Ki values of 8.8, 1.44, 1.2 μM, respectively) and no affinity for other histaminergic receptors . | [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[1]. 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[2]. | [target]
| Target | Value | human H3 receptor () | 1.2 μM(Ki) | mouse H3 receptor () | 1.44 μM(Ki) | rat H3 receptor () | 8.8 μM(Ki) |
| [IC 50]
H3 receptor | [References]
[1] Guilloux JP, et al. S 38093, a histamine H3 antagonist/inverse agonist, promotes hippocampal neurogenesis and improves context discrimination task in aged mice. Sci Rep. 2017 Feb 20;7:42946. DOI:10.1038/srep42946 [2] Sors A, et al. Mechanistic characterization of S 38093, a novel inverse agonist at histamine H3 receptors. Eur J Pharmacol. 2017 May 15;803:11-23 DOI:10.1016/j.ejphar.2017.03.013 |
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