EMD 281014 hydrochloride

Catalog # Availability Size / Price Qty
EMD 281014 hydrochloride | CAS No. 443144-27-2 | 5-HT2A Receptor Antagonists
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Description: Selective 5-HT2A antagonist

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

Purity: ≥98%

Product Details
Supplemental Products

Biological Activity

EMD 281014 hydrochloride is a 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

Soluble to 100 mM in DMSO and to 25 mM in ethanol
Desiccate at RT

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

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