1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor

Eplivanserin (Synonyms: SR-46349)

Cat. No.: HY-10792
Handling Instructions

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.

For research use only. We do not sell to patients.

Eplivanserin Chemical Structure

Eplivanserin Chemical Structure

CAS No. : 130579-75-8

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  • Biological Activity

  • Technical Information

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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.

IC50 & Target

IC50: 5.8 nM (5-HT2 receptor, rat cortical membrane)[1]
Kd: 1.14 nM (5-HT2 receptor)[1]

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].

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].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0453 mL 15.2263 mL 30.4525 mL
5 mM 0.6091 mL 3.0453 mL 6.0905 mL
10 mM 0.3045 mL 1.5226 mL 3.0453 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

328.38

Formula

C₁₉H₂₁FN₂O₂

CAS No.

130579-75-8

SMILES

FC1=CC=CC=C1C(/C=C/C2=CC=C(O)C=C2)=N\OCCN(C)C

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Eplivanserin
Cat. No.:
HY-10792
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Eplivanserin

Cat. No.: HY-10792