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]