Inhibitors Product Data Sheet Eplivanserin • Agonists Cat. No.: HY-10792 CAS No.: 130579-75-8 Molecular Formula: C₁₉H₂₁FN₂O₂ • Molecular Weight: 328.38 Screening Libraries Target: 5-HT Receptor Pathway: GPCR/G Protein; Neuronal Signaling Storage: Please store the product under the recommended conditions in the Certificate of Analysis. BIOLOGICAL ACTIVITY Description Eplivanserin (SR-46349) 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 displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and [1][2] 5-HT2C . IC₅₀ & Target 5-HT2A Receptor 5-HT2A Receptor 5-HT2C Receptor 5.8 nM (IC50, in rat cortical 1.14 nM (Ki) 120 nM (IC50) membrane) In Vitro 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-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 [1] dopamine D1 and D2, with IC50s of 3.4 μM, 1.0 μM, 5.0 μM, 39 μM, 9 μM and 28 μM, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 3 In Vivo Eplivanserin hemifumarate (SR 46349B) inhibits 5-HT2 receptor binding of [ H]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. REFERENCES [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. [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. McePdfHeight Page 1 of 2 www.MedChemExpress.com Caution: Product has not been fully validated for medical applications. For research use only. Tel: 609-228-6898 Fax: 609-228-5909 E-mail: [email protected] Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA Page 2 of 2 www.MedChemExpress.com.