Eplivanserin (hemifumarate)

Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C[1][2].

Product Specifications

CAS Number

[130580-02-8]

Product Name Alternative

SR-46349 (hemifumarate) ; SR 46349B

UNSPSC

12352005

Hazard Statement

H302, H410

Target

5-HT Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/eplivanserin-hemifumarate.html

Purity

99.10

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(O)/C=C/C(O)=O.OC(C=C1)=CC=C1/C=C/C(C2=C(C=CC=C2)F)=N/OCCN(C)C.[1/2]

Molecular Formula

C19H21FN2O2.1/2C4H4O4

Molecular Weight

386.43

Precautions

H302, H410

References & Citations

[1]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.|[2]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.