Eplivanserin

Modify Date: 2024-01-02 12:39:51

Eplivanserin structure	Common Name	Eplivanserin
	CAS Number	130579-75-8	Molecular Weight	328.381
	Density	1.1±0.1 g/cm3	Boiling Point	453.4±55.0 °C at 760 mmHg
	Molecular Formula	C₁₉H₂₁FN₂O₂	Melting Point	N/A
	MSDS	N/A	Flash Point	228.0±31.5 °C

Use of Eplivanserin

Eplivanserin is a potent, selective and orally available 5-HT2 receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM.

Name	Eplivanserin
Synonym	More Synonyms

Description	Eplivanserin is a potent, selective and orally available 5-HT2 receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Research Areas >> Neurological Disease
Target	IC50: 5.8 nM (5-HT2 receptor, rat cortical membrane)[1] Kd: 1.14 nM (5-HT2 receptor)[1]
In Vitro	Eplivanserin is a potent, selective and orally available 5-HT2 antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. 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].
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.

Density	1.1±0.1 g/cm3
Boiling Point	453.4±55.0 °C at 760 mmHg
Molecular Formula	C₁₉H₂₁FN₂O₂
Molecular Weight	328.381
Flash Point	228.0±31.5 °C
Exact Mass	328.158691
PSA	45.06000
LogP	4.22
Vapour Pressure	0.0±1.1 mmHg at 25°C
Index of Refraction	1.534
Storage condition	2-8°C

4-[(1E,3Z)-3-{[2-(Dimethylamino)ethoxy]imino}-3-(2-fluorophenyl)-1-propen-1-yl]phenol

Ciltyri

Eplivanserin

2-Propen-1-one, 1-(2-fluorophenyl)-3-(4-hydroxyphenyl)-, O-[2-(dimethylamino)ethyl]oxime, (1Z,2E)-

4-[(1E,3Z)-3-{[2-(dimethylamino)ethoxy]imino}-3-(2-fluorophenyl)prop-1-en-1-yl]phenol

Eplivanserin

Use of Eplivanserin

Names

Eplivanserin Biological Activity

Chemical & Physical Properties

Synonyms