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Submit ReviewEplivanserin hemifumarate
Description: Potent and selective 5-HT2A antagonist
Alternative Names: SR-46349 hemifumarate,SR-46349B
Chemical Name: (1Z,2E)-1-(2-Fluorophenyl)-3-(4-hydroxyphenyl)-2-propen-1-one O-[2-(dimethylamino)ethyl]oxime hemifumarate
Purity: ≥98% (HPLC)
Biological Activity for Eplivanserin hemifumarate
Eplivanserin hemifumarate is a potent and selective 5-HT2A antagonist (IC50 values are 5.8 and 120 and >100 nM for 5-HT2A, 5-HT2B and 5-HT2C, respectively). Attenuates cocaine-induced hyperactivity. Increases dopamine (DA) release in rat medial prefrontal cortex (mPFC); potentiates haloperidol-induced DA release in the mPFC and nucleus accumbens.
Technical Data for Eplivanserin hemifumarate
| M. Wt | 386.42 |
| Formula | C19H21FN2O2.0.5C4H4O4 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 130580-02-8 |
| PubChem ID | 6438382 |
| InChI Key | UCLIFEBROADCQW-PWERMGERSA-N |
| Smiles | OC(C=C2)=CC=C2/C=C/C(C1=CC=CC=C1F)=N/OCCN(C)C.O=C(/C=C/C(O)=O)O.OC(C=C4)=CC=C4/C=C/C(C3=CC=CC=C3F)=N/OCCN(C)C |
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 for Eplivanserin hemifumarate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 19.32 | 50 |
Preparing Stock Solutions for Eplivanserin hemifumarate
The following data is based on the product molecular weight 386.42. 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 |
|---|---|---|---|
| 0.5 mM | 5.18 mL | 25.88 mL | 51.76 mL |
| 2.5 mM | 1.04 mL | 5.18 mL | 10.35 mL |
| 5 mM | 0.52 mL | 2.59 mL | 5.18 mL |
| 25 mM | 0.1 mL | 0.52 mL | 1.04 mL |
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Product Datasheets for Eplivanserin hemifumarate
References for Eplivanserin hemifumarate
References are publications that support the biological activity of the product.
Yadav et al (2011) Antagonist functional selectivity: 5-HT2A serotonin receptor antagonists differentially regulate 5-HT2A receptor protein level in vivo. J.Pharmacol.Exp.Ther. 339 99 PMID: 21737536
Filip et al (2004) Contribution of serotonin (5-hydroxytryptamine; 5-HT) 5-HT2 receptor subtypes to the hyperlocomotor effects of cocaine: acute and chronic pharmacological analyses. J.Pharmacol.Exp.Ther. 310 1246 PMID: 15131246
Bonaccorso et al (2002) SR46349-B, a 5-HT(2A/2C) receptor antagonist, potentiates haloperidol-induced DA release in rat medial prefrontal cortex and nucleus accumbens. Neuropsychopharmacology. 27 430 PMID: 12225700
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Keywords: Eplivanserin hemifumarate, Eplivanserin hemifumarate supplier, antipsychotic, potent, selective, 5-HT2A, antagonist, SR-46349, hemifumarate, SR-46349B, Receptors, 4958, Tocris Bioscience
Citations for Eplivanserin hemifumarate
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Reviews for Eplivanserin hemifumarate
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Eplivanserin hemifumarate blocks MDMA-induced striatal activation and locomotion.
By
Kevin Ball on 01/25/2019
Assay Type: In Vivo
Species: Rat
We assessed the effect of the 5-HT2A antagonist, SR-46349B (eplivanserin hemifumarate; 0.5 mg/kg, s.c.), on MDMA (ecstasy)-induced locomotion and dorsal striatal single-unit electrophysiology. SR-46349B blocked nearly all MDMA-induced striatal excitations, which paralleled its significant attenuation of MDMA-induced locomotor activation (shown in figure).
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.