Eplivanserin  (Synonyms: SR-46349)

Eplivanserin (SR-46349) is a potent, selective and orally active 5-HT_2A receptor antagonist, with an IC₅₀ of 5.8 nM in rat cortical membrane, and a K_d of 1.14 nM. Eplivanserin displays >20-fold selectivity more selective for 5-HT_2A than 5-HT_2B and 5-HT_2C^[1][2].

Eplivanserin hemifumarate (SR 46349B) shows weak inhibition on other 5-HT kinases, with IC₅₀s of 0.12 μM (Pig cortex 5-HT_1C), 14 μM (Rat hippocampus 5-HT_1A), and 16 μM (Rat stnatum 5-HT_1B, Ox caudate nucleus 5-HT_1D). 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].

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

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].

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

328.39

C₁₉H₂₁FN₂O₂

130579-75-8

OC1=CC=C(/C=C/C(C2=CC=CC=C2F)=N/OCCN(C)C)C=C1.[(E)]

Room temperature in continental US; may vary elsewhere.

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• [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.  [Content Brief]

  [2]. Malgorzata Filip, et al. 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. 2004 Sep;310(3):1246-54.  [Content Brief]