Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | 6-8 weeks | $ 195.00 | |
5 mg | 6-8 weeks | $ 437.00 | |
10 mg | 6-8 weeks | $ 646.00 | |
25 mg | 6-8 weeks | $ 987.00 | |
50 mg | 6-8 weeks | $ 1,380.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 443.00 |
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. |
Targets&IC50 | 5-HT2 receptor:1.14 nM (ki), 5-HT2 receptor: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]. |
Synonyms | SR-46349 |
Molecular Weight | 328.38 |
Formula | C19H21FN2O2 |
CAS No. | 130579-75-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (152.26 mM)
You can also refer to dose conversion for different animals. More
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Eplivanserin 130579-75-8 GPCR/G Protein Neuroscience 5-HT Receptor 5-hydroxytryptamine Receptor Serotonin Receptor 5-HT2A SR46349 SR 46349 oral dopamine Inhibitor SR-46349 inhibit release inhibitor