130580-02-8

130580-02-8 structure

Name: Eplivanserin hemifumarate
Chemical Name: Eplivanserin Fumarate
CAS Number: 130580-02-8
Molecular Formula: C₂₃H₂₅FN₂O₆
Molecular Weight: 444.45300
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2018-09-16 18:43:27
Modify Date: 2024-01-02 12:11:06
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].

Name	Eplivanserin Fumarate
Synonyms	Eplivanserin hemifumarate (Z,E)-1-(2-Fluorophenyl)-3-(4-hydroxyphenyl)-2-propen-1-one O-[2-(dimethylamino)ethyl]oxime fumarate (2:1) TRANS-2'-FLUORO-4-HYDROXYCHALCONE O-[(Z)-2-(DIMETHYLAMINO)ETHYL]OXIME--FUMARIC ACID (2:1) SR-46349 hemifumarate salt

Description	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].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	5-HT2A Receptor:5.8 nM (IC50) 5-HT2C Receptor:120 nM (IC50)
In Vitro	Eplivanserin hemifumarate (SR 46349B) shows weak inhibition on other 5-HT kinases, 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). Eplivanserin also 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[1].
In Vivo	Eplivanserin hemifumarate (SR 46349B) inhibits 5-HT2 receptor binding of [3H]ketanserin with an ED50 of 0.087 mg/kg after i.p. injection, and 0.097 mg/kg after p.o administration in mice[1]. SR 46349B (0.25-1 mg/kg; i.p.) blocks Cocaine-evoked hyperactivity following repeated Cocaine treatment in rats[2].
References	[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.

Boiling Point	456.3ºC at 760mmHg
Molecular Formula	C₂₃H₂₅FN₂O₆
Molecular Weight	444.45300
Flash Point	229.8ºC
Exact Mass	444.17000
PSA	119.66000
LogP	3.23880
Vapour Pressure	1.63E-08mmHg at 25°C

Symbol	GHS07, GHS09
Signal Word	Warning
Hazard Statements	H302-H410
Precautionary Statements	P273-P501
RIDADR	UN 3077 9 / PGIII

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