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.
| 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
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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