Chemical Name |
Eplivanserin |
CAS Number |
130579-75-8 |
MDL Number |
MFCD00893359 |
Molecular Formula |
C19H21FN2O2 |
Molecular Weight |
328.38 |
Synonyms |
SR-46349 |
Introduction of 130579-75-8 :
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. IC50 & 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].
Purity |
NLT 98% |
Storage |
at 20ºC 2 years |
*The above information is for reference only.