Introduction：Basic information about CAS 130579-75-8|Eplivanserin, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Eplivanserin |
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| CAS Number | 130579-75-8 | Molecular Weight | 328.381 |
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| Density | 1.1±0.1 g/cm3 | Boiling Point | 453.4±55.0 °C at 760 mmHg |
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| Molecular Formula | C19H21FN2O2 | Melting Point | / |
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| MSDS | / | Flash Point | 228.0±31.5 °C |
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Names
| Name | Eplivanserin |
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| Synonym | More Synonyms |
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Eplivanserin BiologicalActivity
| Description | Eplivanserin is a potent, selective and orally available 5-HT2 receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. |
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| Related Catalog | Signaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT ReceptorResearch Areas >>Neurological Disease |
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| Target | IC50: 5.8 nM (5-HT2 receptor, rat cortical membrane)[1] Kd: 1.14 nM (5-HT2 receptor)[1] |
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| In Vitro | Eplivanserin is a potent, selective and orally available 5-HT2 antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate (SR 46349B) shows weak inhibition on other 5-HT kinases, with IC50s of 0.12 μM (Pig cortex 5-HT1C), 14 μM (Rat hippocampus 5-HT1A), and 16 μM (Rat stnatum 5-HT1B, Ox caudate nucleus 5-HT1D). Eplivanserin also has inhibitory effects on rat cortex adrenergic α1 and α2, rat whole brain histammine H1, Na+ channel, and rat striatum dopamine D1 and D2, with IC50s of 3.4 μM, 1.0 μM, 5.0 μM, 39 μM, 9 μM and 28 μM, respectively[1]. |
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| In Vivo | Eplivanserin hemifumarate (SR 46349B) inhibits 5-HT2 receptor binding of [3H]ketanserin with an ED50 of 0.087 mg/kg after i.p. injection, and 0.097 mg/kg after p.o administration in mice[1]. |
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| References | [1]. Rinaldi-Carmona M, et al. Biochemical and pharmacological properties of SR 46349B, a new potent and selective 5-hydroxytryptamine2 receptor antagonist. J Pharmacol Exp Ther. 1992 Aug;262(2):759-68. |
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Chemical & Physical Properties
| Density | 1.1±0.1 g/cm3 |
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| Boiling Point | 453.4±55.0 °C at 760 mmHg |
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| Molecular Formula | C19H21FN2O2 |
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| Molecular Weight | 328.381 |
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| Flash Point | 228.0±31.5 °C |
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| Exact Mass | 328.158691 |
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| PSA | 45.06000 |
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| LogP | 4.22 |
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| Vapour Pressure | 0.0±1.1 mmHg at 25°C |
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| Index of Refraction | 1.534 |
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| InChIKey | VAIOZOCLKVMIMN-UHFFFAOYSA-N |
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| SMILES | CN(C)CCON=C(C=Cc1ccc(O)cc1)c1ccccc1F |
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| Storage condition | 2-8°C |
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Synonyms
| 4-[(1E,3Z)-3-{[2-(Dimethylamino)ethoxy]imino}-3-(2-fluorophenyl)-1-propen-1-yl]phenol |
| Ciltyri |
| Eplivanserin |
| 2-Propen-1-one, 1-(2-fluorophenyl)-3-(4-hydroxyphenyl)-, O-[2-(dimethylamino)ethyl]oxime, (1Z,2E)- |
| 4-[(1E,3Z)-3-{[2-(dimethylamino)ethoxy]imino}-3-(2-fluorophenyl)prop-1-en-1-yl]phenol |
