EPLIVANSERIN FUMARATE
EPLIVANSERIN FUMARATE Basic information
- Product Name:
- EPLIVANSERIN FUMARATE
- Synonyms:
-
- EPLIVANSERIN FUMARATE
- SR 46349B
- TRANS-2''-FLUORO-4-HYDROXYCHALCONE O-[(Z)-2-(DIMETHYLAMINO)ETHYL]OXIME--FUMARIC ACID (2:1)
- (Z,E)-1-(2-Fluorophenyl)-3-(4-hydroxyphenyl)-2-propen-1-one O-[2-(dimethylamino)ethyl]oxime fumarate (2:1)
- Eplivanserin hemifumarate
- 4-((3Z)-3-(2-Dimethylaminoethyl)oxyimino-3-(2-fluorophenyl)propen-1-yl)phenol hemifumarate salt
- Eplivanserin hemifumarate salt
- SR-46349 hemifumarate salt
- CAS:
- 130580-02-8
- MF:
- C23H25FN2O6
- MW:
- 444.46
- Mol File:
- 130580-02-8.mol
EPLIVANSERIN FUMARATE Chemical Properties
- storage temp.
- 2-8°C
- solubility
- DMSO: ≥10mg/mL
- form
- powder
- color
- white to off-white
EPLIVANSERIN FUMARATE Usage And Synthesis
Uses
Eplivanserin Hemifumarate is a 5-HT2A antagonist.
Biological Activity
SR-46349 is an antagonist of 5-HT (2A/2C) receptor and increases the release of dopamine by medial prefrontal cortex in rats.1 It increases the signal transduction induced by 5-HT2 receptor by binding with high affinity.2 SR-46349 inhibits the aggregation of rabbit and human platelets in response to serotonin.3', 'ASTAR (Antagonist of Serotonin 5HT2A Receptors).
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].
SR 46349B (0.25-1 mg/kg; i.p.) blocks Cocaine-evoked hyperactivity following repeated Cocaine treatment in rats[2].
IC 50
5-HT2A Receptor: 5.8 nM (IC50); 5-HT2C Receptor: 120 nM (IC50)
storage
Store at +4°C
EPLIVANSERIN FUMARATESupplier
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