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862896-30-8 (S 38093)

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Identification

S 38093 S 38093
Name S 38093
Formula C17H24N2O2
MW 288.38
CAS No. 862896-30-8
EINECS
Smiles O=C(N)C1=CC=C(OCCCN2CC3C(CCC3)C2)C=C1
Synonyms
InChI InChI=1S/C17H24N2O2/c18-17(20)13-5-7-16(8-6-13)21-10-2-9-19-11-14-3-1-4-15(14)12-19/h5-8,14-15H,1-4,9-12H2,(H2,18,20)
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Introduction

S 38093 is a brain-penetrant antagonist of H3 receptor, with Ki of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively.

Background Information

S 38093 is a brain-penetrant antagonist of <b>H3 receptor</b>, with <b>K<sub>i</sub></b> of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively. IC50 & Target: Ki: 8.8 µM (Rat H3 receptor), 1.44 µM (Mouse H3 receptor), 1.2 µM (Human H3 receptor)<sup>[2]</sup> <i><b>In Vitro:</b></i> In cellular models, S 38093 is able to antagonize mice H3 receptors (K<sub>B</sub>=0.65 µM) and to suppress cAMP decrease induced by an H3 agonist via human H3 receptors (K<sub>B</sub>=0.11 µM). In cells expressing a high H3 density, S 38093 behaves as a moderate inverse agonist at rat and human H3 receptors (EC<sub>50</sub>=9 and 1.7 µM, respectively)<sup>[2]</sup>. <i><b>In Vivo:</b></i> 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<sup>+</sup> 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 APPSWE<sup>TG</sup> 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<sup>[1]</sup>. 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<sup>[2]</sup>. ......by MedChemexpress Co., Ltd.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance: EBNumber:EB000134603

Storage condition

Solubility

DMSO: 15 mg/mL by MedChemexpress Co., Ltd.
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Mechanism and Indication

Signaling Pathways Immunology/Inflammation GPCR/G Protein
Target Histamine Receptor
Research Area
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
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Safety Data of S 38093

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
MedChemexpress Co., Ltd. USA
Shanghai Haoyuan Chemexpress Co., Ltd. China
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Related Products

Other Forms of 862896-30-8

Name CAS No Formula MW

Recommended Compounds in Histamine Receptor

Name CAS No Formula MW
Doxylamine (succinate) 562-10-7 C21H28N2O5 388.46
Ebastine 90729-43-4 C32H39NO2 469.66
Azelastine 58581-89-8 C22H24ClN3O 381.9
Epinastine 80012-43-7 C16H15N3 249.31
Hydroxyzine (dihydrochloride) 2192-20-3 C21H29Cl3N2O2 447.83
Hydroxyzine 68-88-2 C21H27ClN2O2 374.9
Desloratadine 100643-71-8 C19H19ClN2 310.82
Pemirolast (potassium) 100299-08-9 C10H7KN6O 266.3
Betahistine (dihydrochloride) 5579-84-0 C8H14Cl2N2 209.12
Brompheniramine (maleate) 980-71-2 C20H23BrN2O4 435.31
Azelastine (hydrochloride) 79307-93-0 C22H25Cl2N3O 418.36
Olopatadine (hydrochloride) 140462-76-6 C21H24ClNO3 373.87
Famotidine 76824-35-6 C8H15N7O2S3 337.45
Meclizine (dihydrochloride) 1104-22-9 C25H29Cl3N2 463.87
Nizatidine 76963-41-2 C12H21N5O2S2 331.46
Roxatidine (Acetate Hydrochloride) 93793-83-0 C19H29ClN2O4 384.9
Diphenhydramine (hydrochloride) 147-24-0 C17H22ClNO 291.82
Clemastine (fumarate) 14976-57-9 C25H30ClNO5 459.96
Chlorpheniramine (maleate) 113-92-8 C20H23ClN2O4 390.86
Ranitidine (hydrochloride) 66357-59-3 C13H23ClN4O3S 350.86

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

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References

Protocol Reference

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More Information

S 38093

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