ChemicalBook--->CAS DataBase List--->862896-30-8

862896-30-8

862896-30-8 Structure

862896-30-8 Structure
IdentificationBack 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 PropertiesBack 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
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P305+P351+P338
Hazard InformationBack 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]

TargetValue
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
Spectrum DetailBack Directory
[Spectrum Detail]

s38093 free(862896-30-8)1HNMR
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