For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I006688 |
| CAS Number | 130580-02-8 |
| Molecular Formula | C19H21FN2O2.1/2C4H4O4 |
| Purity | ≥95% |
| Reference | [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. |
