EMD 281014 hydrochloride

Name: EMD 281014 hydrochloride
Brand: Tocris Bioscience
SKU: 4470

Tocris Bioscience, part of Bio-Techne | Catalog # 4470

Citations (3)

COA / SDS

Selective 5-HT2A antagonist

Key Product Details

Description:	Selective 5-HT_2A antagonist
Chemical Name:	7-[[4-[2-(4-Fluorophenyl)ethyl]-1-piperazinyl]carbonyl]-1H-indole-3-carbonitrile hydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	412.89

View Full Technical Details for EMD 281014 hydrochloride

Technical Data
Citations

Biological Activity for EMD 281014 hydrochloride

EMD 281014 hydrochloride is a selective 5-HT_2A antagonist; displays high affinity for human 5-HT_2A over 5-HT_2C receptors (K_i values are 0.87 and 557 nM respectively). Exhibits low off-target activity (K_i values are >1000 and 1268 nM for human D₂ receptors and IKr channels, respectively).

Technical Data for EMD 281014 hydrochloride

M. Wt	412.89
Formula	C₂₂H₂₁FN₄O.HCl
Storage	Desiccate at RT
Purity	≥98% (HPLC)
CAS Number	443144-27-2
PubChem ID	9887933
InChi Key	UYGNZRVLPYZLTF-UHFFFAOYSA-N
Smiles	O=C(N3CCN(CCC4=CC=C(F)C=C4)CC3)C1=C2C(C(C#N)=CN2)=CC=C1.Cl

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.

Solubility for EMD 281014 hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	41.29	100
	ethanol	10.32	25

Preparing Stock Solutions for EMD 281014 hydrochloride

The following data is based on the product molecular weight 412.89.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.42 mL	12.11 mL	24.22 mL
5 mM	0.48 mL	2.42 mL	4.84 mL
10 mM	0.24 mL	1.21 mL	2.42 mL
50 mM	0.05 mL	0.24 mL	0.48 mL

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References for EMD 281014 hydrochloride

References are publications that support the biological activity of the product.

Hamadjida The highly selective 5-HT_2A antagonist EMD-281,014 reduces dyskinesia and psychosis in the l-DOPA-treated parkinsonian marmoset. Neuropharmacology. 2018 PMID: 29969592
Patel 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. Synapse 2004 PMID: 14755634
Bartoszyk EMD 281014, a new selective serotonin 5-HT_2A receptor antagonist. Eur.J.Pharmacol. 2003 PMID: 12892843
Ladduwahetty A new class of selective, non-basic 5-HT_2A receptor antagonists. Bioorg.Med.Chem.Lett. 2006 PMID: 16632354