EMD 281014 hydrochloride

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Cat.No. 4470 - EMD 281014 hydrochloride | C22H21FN4O.HCl | CAS No. 443144-27-2
Description: Selective 5-HT2A antagonist
Chemical Name: 7-[[4-[2-(4-Fluorophenyl)ethyl]-1-piperazinyl]carbonyl]-1H-indole-3-carbonitrile hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

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).

Compound Libraries

EMD 281014 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 412.89. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Ladduwahetty et al (2006) A new class of selective, non-basic 5-HT2A receptor antagonists. Bioorg.Med.Chem.Lett. 16 3201 PMID: 16632354

Patel et al (2004) 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 52 73 PMID: 14755634

Bartoszyk et al (2003) EMD 281014, a new selective serotonin 5-HT2A receptor antagonist. Eur.J.Pharmacol. 473 229 PMID:


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Keywords: EMD281014 5-HT2A selective serotonergics antagonists h5-HT2A h5-HT2C 5-HT2A Receptors

Citations for EMD 281014 hydrochloride

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Literature in this Area

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5-HT Receptors Scientific Review

Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.

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Pathways for EMD 281014 hydrochloride

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