Eplivanserin (hemifumarate)

• 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].

• Product Name Alternative :

  SR-46349 (hemifumarate) ; SR 46349B

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H410

• Target :

  5-HT Receptor

• Type :

  Reference compound

• Related Pathways :

  GPCR/G Protein; Neuronal Signaling

• Applications :

  Neuroscience-Neuromodulation

• Field of Research :

  Neurological Disease

• Assay Protocol :

  https://www.medchemexpress.com/eplivanserin-hemifumarate.html

• Purity :

  99.10

• Solubility :

  DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

• Smiles :

  O=C(O)/C=C/C(O)=O.OC(C=C1)=CC=C1/C=C/C(C2=C(C=CC=C2)F)=N/OCCN(C)C.[1/2]

• Molecular Formula :

  C19H21FN2O2.1/2C4H4O4

• Molecular Weight :

  386.43

• Precautions :

  H302, H410

• References & Citations :

  [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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  4°C (Powder, sealed storage, away from moisture)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 3

• Isoform :

  5-HT2 Receptor; α-1 microglobulin

• CAS Number :

  [130580-02-8]