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Submit ReviewEMD 281014 hydrochloride
Description: Selective 5-HT2A antagonist
Chemical Name: 7-[[4-[2-(4-Fluorophenyl)ethyl]-1-piperazinyl]carbonyl]-1H-indole-3-carbonitrile hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for EMD 281014 hydrochloride
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 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 Data 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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Product Datasheets for EMD 281014 hydrochloride
References for EMD 281014 hydrochloride
References are publications that support the biological activity of the product.
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: 12892843
Hamadjida et al (2018) The highly selective 5-HT2A antagonist EMD-281,014 reduces dyskinesia and psychosis in the l-DOPA-treated parkinsonian marmoset. Neuropharmacology. 139 61 PMID: 29969592
If you know of a relevant reference for EMD 281014 hydrochloride, please let us know.
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Keywords: EMD 281014 hydrochloride, EMD 281014 hydrochloride supplier, EMD281014, 5-HT2A, selective, serotonergics, antagonists, h5-HT2A, h5-HT2C, Receptors, 4470, Tocris Bioscience
2 Citations for EMD 281014 hydrochloride
Citations are publications that use Tocris products. Selected citations for EMD 281014 hydrochloride include:
Georgia et al (2019) Multimodal Single-Cell Analysis Reveals Physiological Maturation in the Developing Human Neocortex. Neuron 102 143-158.e7 PMID: 30770253
Wieland B et al (2020) Serotonin Receptor 2A Activation Promotes Evolutionarily Relevant Basal Progenitor Proliferation in the Developing Neocortex. Neuron 108 1113-1129.e6 PMID: 33080227
Do you know of a great paper that uses EMD 281014 hydrochloride from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.