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

Eplivanserin hemifumarate (Synonyms: SR-46349 hemifumarate; SR 46349B)

Cat. No.: HY-110129
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Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C.

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

Eplivanserin hemifumarate Chemical Structure

Eplivanserin hemifumarate Chemical Structure

CAS No. : 130580-02-8

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Estimated Time of Arrival: December 31
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Description

Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C[1][2].

IC50 & Target[1][2]

5-HT2A Receptor

5.8 nM (IC50)

5-HT2C Receptor

120 nM (IC50)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].
SR 46349B (0.25-1 mg/kg; i.p.) blocks Cocaine-evoked hyperactivity following repeated Cocaine treatment in rats[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

386.43

Formula

C₁₉H₂₁FN₂O₂.₁/₂C₄H₄O₄

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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Eplivanserin hemifumarate
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