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Eplivanserin

Names

[ CAS No. ]:
130579-75-8

[ Name ]:
Eplivanserin

[Synonym ]:
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

Biological Activity

[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.


[Related Small Molecules]

Harmine | Pimavanserin | Serotonin hydrochloride | Sodium Ferulate | Thioridazine hydrochloride | Brexpiprazole | Risperidone | TG6-10-1 | Cariprazine | Quetiapine | SERTINDOLE | Alprenolol hydrochloride | B-HT 920 | Ketanserin | Palonosetron hydrochloride

Chemical & Physical Properties

[ 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

Related Compounds