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EMD 281014 hydrochloride

4470 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
4470/10
4470/50
5-HT2A Receptor Antagonists Small Molecule
1 Image
Description: Selective 5-HT2A antagonist

Chemical Name: 7-[[4-[2-(4-Fluorophenyl)ethyl]-1-piperazinyl]carbonyl]-1H-indole-3-carbonitrile hydrochloride

Purity: ≥98%

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Biological Activity

Selective 5-HT2A antagonist; displays high affinity for human 5-HT2A over 5-HT2C receptors (Ki values are 0.87 and 557 nM respectively). Exhibits low off-target activity (Ki values are >1000 and 1268 nM for human D2 receptors and IKr channels, respectively).

Technical Data

M.Wt:
412.89
Formula:
C22H21FN4O.HCl
Solubility:
Soluble to 100 mM in DMSO and to 25 mM in ethanol
Purity:
≥98%
Storage:
Desiccate at RT
CAS No:
443144-27-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. A new class of selective, non-basic 5-HT2A receptor antagonists.
    Ladduwahetty et al.
    Bioorg.Med.Chem.Lett., 2006;16:3201
  2. The highly selective 5-hydroxytryptamine (5-HT)2A receptor antagonist, EMD 281014, significantly increases swimming and decreases immobility in male congenital learned helpless rats in the forced swim test.
    Patel et al.
    Synapse, 2004;52:73
  3. EMD 281014, a new selective serotonin 5-HT2A receptor antagonist.
    Bartoszyk et al.
    Eur.J.Pharmacol., 2003;473:229
  4. The highly selective 5-HT2A antagonist EMD-281,014 reduces dyskinesia and psychosis in the l-DOPA-treated parkinsonian marmoset.
    Hamadjida et al.
    Neuropharmacology., 2018;139:61

Product Datasheets

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VersaClone cDNA Plasmids

Human 5-HT2A (NP_000612) VersaClone cDNA

RDC0288

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