s38093
s38093 Basic information
- Product Name:
- s38093
- Synonyms:
-
- S 38093; S38093; S-38093; S38093 HCL
- s38093
- S38093 HCl
- S 38093 Hydrochloride
- S 38093 HydrochL
- 4-(3-(Hexahydrocyclopenta[c]pyrrol-2(1H)-yl)propoxy)benzamide hydrochloride
- S 38093 HCl, 10 mM in DMSO
- CAS:
- 1222097-72-4
- MF:
- C17H25ClN2O2
- MW:
- 324.85
- Product Categories:
-
- API
- Mol File:
- 1222097-72-4.mol
s38093 Usage And Synthesis
Description
S38093 is an inverse agonist at histamine H3 receptors. S 38093 displays a moderate affinity for rat, mouse and human H3 receptors (Ki=8.8, 1.44 and 1.2μM, respectively) with no affinity for other histaminergic receptors. In cellular models, the compound was able to antagonize mice H3 receptors (KB=0.65μM) and to suppress cAMP decrease induced by an H3 agonist via human H3 receptors (KB=0.11μM).
Uses
S 38093 hydrochloride 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.
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].
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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