| Name | Eplivanserin |
| Description | Eplivanserin (SR-46349) is an effective and selective antagonist of 5-HT2A receptor with a Kd of 1.14 nM and an IC50 value of 5.8 nM in rat cortical membrane. |
| In vitro | Eplivanserin 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. Eplivanserin displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C 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)[1]. |
| In vivo | In mice, Eplivanserin(0.097 mg/kg; i.p.) inhibits 5-HT2 receptor binding of [3H]ketanserin with an ED50 of 0.087 mg/kg[1]. In rats, SR 46349B (0.25-1 mg/kg; i.p.) blocks Cocaine-evoked hyperactivity following repeated Cocaine treatment[2]. |
| Storage | keep away from moisture,store at low temperature | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (152.26 mM), Sonication is recommended.
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| Keywords | SR46349 | SR 46349 | Serotonin Receptor | release | oral | Inhibitor | inhibit | Eplivanserin | dopamine | 5-hydroxytryptamine Receptor | 5HTReceptor | 5-HT2C | 5-HT2A | 5-HT2 Receptor | 5-HT Receptor | 5HT Receptor |
| Inhibitors Related | Alverine citrate | Sevoflurane | Dapoxetine hydrochloride | Cefaclor monohydrate | Clozapine N-Oxide | 1,8-Cineole | Dopamine hydrochloride | Cloperastine hydrochloride | Mianserin hydrochloride | Trazodone hydrochloride | Cinchonidine | Doxepin hydrochloride |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Anti-Alzheimer's Disease Compound Library | Pediatric Drug Library | ReFRAME Related Library | Anti-Cancer Clinical Compound Library | Neurotransmitter Receptor Compound Library | Drug Repurposing Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library | Serotonin Receptor-Targeted Compound Library |
United States
