EMD 281014 hydrochloride
Chemical Name: 7-[[4-[2-(4-Fluorophenyl)ethyl]-1-piperazinyl]carbonyl]-1H-indole-3-carbonitrile hydrochloride
Purity: ≥98%
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
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
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A new class of selective, non-basic 5-HT2A receptor antagonists.
Ladduwahetty et al.
Bioorg.Med.Chem.Lett., 2006;16:3201 -
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 -
EMD 281014, a new selective serotonin 5-HT2A receptor antagonist.
Bartoszyk et al.
Eur.J.Pharmacol., 2003;473:229 -
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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