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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 | Price | Availability | Quantity |
---|---|---|---|
1 mg | $195 | 6-8 weeks | |
5 mg | $437 | 6-8 weeks | |
10 mg | $646 | 6-8 weeks | |
25 mg | $987 | 6-8 weeks | |
50 mg | $1,380 | 6-8 weeks | |
1 mL x 10 mM (in DMSO) | $443 | 6-8 weeks |
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]. |
Alias | SR-46349 |
Molecular Weight | 328.38 |
Formula | C19H21FN2O2 |
Cas No. | 130579-75-8 |
Relative Density. | 1.08 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (152.26 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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