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Eplivanserin

Catalog No. T11217   CAS 130579-75-8
Synonyms: SR-46349

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.

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Eplivanserin Chemical Structure
Eplivanserin, CAS 130579-75-8
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
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (152.26 mM)

TargetMolReferences and Literature

1. 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. 2. 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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Clinical Compound Library GPCR Compound Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Pediatric Drug Library Bioactive Compounds Library Max Neurotransmitter Receptor Compound Library Human Metabolite Library

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Keywords

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

 

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