Eplivanserin hemifumarate

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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)
Reviews (1)
Literature (3)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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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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).

PMID: 16001122 Reference
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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!

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5-HT Receptors Scientific Review

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.

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