Eplivanserin

SKU: orb1309695

Description

Eplivanserin (SR-46349) is a potent and selective 5-HT2A receptor antagonist, exhibiting a Kd of 1.14 nM and an IC50 of 5.8 nM in rat cortical membranes. It is a valuable research tool for studying serotonin signaling in in vitro binding assays and in vivo models related to sleep and psychiatric disorders.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 130579-75-8
• MW: 328.38
• Purity: 97.04% (May vary between batches)
• Formula: C₁₉H₂₁FN₂O₂
• SMILES: CN(C)CCO\N=C(\C=Cc1ccc(O)cc1)c1ccccc1F
• Target: 5-HT Receptor
• Solubility: DMSO:50 mg/mL (152.26 mM)

Bioactivity

• Target IC50:
  5-HT2C receptor:120 nM|5-HT2 receptor:5.8 nM (in rat cortical membrane)|5-HT2 receptor:1.14 nM (Ki)
• 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. In rats, SR 46349B (0.25-1 mg/kg; i.p.) blocks Cocaine-evoked hyperactivity following repeated Cocaine treatment.
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• 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).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

dopamine, 5HTReceptor, 5-hydroxytryptamine Receptor, 5-HT2C, 5-HT2 Receptor, 5-HT2A, 5HT Receptor, 5-HT Receptor, Eplivanserin, Inhibitor, oral, inhibit, Serotonin Receptor, release, SR 46349, SR46349, SR-46349

Compound Identifiers

PubChem CID

136167714