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Submit ReviewS 38093
Description: Selective H3 antagonist and inverse agonist; also σ1 receptor antagonist; antinociceptive
Chemical Name: rel-4-[3-[(3aR,6aS)-Hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy]benzamide
Purity: ≥98% (HPLC)
Biological Activity
H3 antagonist and inverse agonist (Ki values are 8.8, 1.2 and 1.44 μM, at rat, human and mouse, respectively). Exhibits no activity at other histaminergic receptors. Antagonizes agonist action at mouse H3 receptors (KB = 0.65 μM). Displays inverse agonist action in cells expressing a high H3 receptor density, (EC50 values are 9 and 1.7 μM, at human and rat H3 receptors, respectively). Exhibits antihyperalgesic effect in a mouse diabetic neuropathy model in vivo. Promotes hippocampal neurogenesis in a mouse Alzheimer's disease model. Antinociceptive and procognitive. Also σ1 receptor antagonist. Exhibits ~30-fold selecitivity for σ1 over H3 and occupies σ1 but not H3 receptors at procognitive does in mice.
Technical Data
| M. Wt | 288.39 |
| Formula | C17H24N2O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1403835-45-9 |
| PubChem ID | 70941112 |
| InChI Key | MRNMYWNBLVJWKG-GASCZTMLSA-N |
| Smiles | [H][C@@]12CCC[C@@]1(CN(C2)CCCOC3=CC=C(C(N)=O)C=C3)[H] |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 28.84 | 100 | |
| ethanol | 14.42 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 288.39. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.47 mL | 17.34 mL | 34.68 mL |
| 5 mM | 0.69 mL | 3.47 mL | 6.94 mL |
| 10 mM | 0.35 mL | 1.73 mL | 3.47 mL |
| 50 mM | 0.07 mL | 0.35 mL | 0.69 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Guilloux et al (2017) S 38093, a histamine H3 antagonist/inverse agonist, promotes hippocampal neurogenesis and improves context discrimination task in aged mice. Sci.Rep. 7 42946 PMID: 28218311
Chaumette et al (2018) Effects of S 38093, an antagonist/inverse agonist of histamine H3 receptors, in models of neuropathic pain in rats. Eur.J.Pain. 22 127 PMID: 28877402
Guilloux et al (2017) S 38093, a histamine H3 antagonist/inverse agonist, promotes hippocampal neurogenesis and improves context discrimination task in aged mice. Sci.Rep. 7 42946 PMID: 28218311
Riddy et al (2019) Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H3 receptor antagonists. Neuropharmacology 144 244 PMID: 30359639
If you know of a relevant reference for S 38093, please let us know.
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Keywords: S 38093, S 38093 supplier, S38093, H3, agonists, Receptors, Histamine, histaminergic, selective, antagonists, antagonism, inverse, agonism, antinociceptive, σ1, sigma1, procognitive, Sigma1, 6778, Tocris Bioscience
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