Biological Activity
Orally active, subtype-selective NR1A/NR2B NMDA receptor antagonist (IC50 values are 5.3, 35000 and > 100000 nM for NR1A/2B, NR1A/2A and NR1A/2C receptor subtypes respectively). Potentiates the effect of L-DOPA in 6-OHDA-lesioned rats following oral administration.
Technical Data
| M. Wt | 345.44 |
| Formula | C22H23N3O |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 302799-86-6 |
| PubChem ID | 9863010 |
| InChI Key | JJEXWPHPFZLTCU-UHFFFAOYSA-N |
| Smiles | O=C2NC1=CC=C(C#CCN3CCC(CC4=CC=CC=C4)CC3)C=C1N2 |
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 | 34.54 | 100 | |
| ethanol | 34.54 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 345.44. 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 | 2.89 mL | 14.47 mL | 28.95 mL |
| 5 mM | 0.58 mL | 2.89 mL | 5.79 mL |
| 10 mM | 0.29 mL | 1.45 mL | 2.89 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.58 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Wright et al (2000) Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(heteroarylalkynyl)-4-benzylpiperidines. J.Med.Chem. 43 3408 PMID: 10978188
Roger et al (2003) Synthesis, radiosynthesis and in vivo evaluation of 5-[3-(4-benzylpiperidin-1-yl)prop-1-ynyl]-1,3-dihydrobenzoimidazol-2-[11C]one, as a potent NR1A/2B subtype selective NMDA PET radiotracer. Bioorg.Med.Chem. 11 5401 PMID: 14642584
Keywords: TCS 46b, supplier, Orally, active, subtype-selective, NR1A/NR2B, antagonists, Glutamate, NMDA, Receptors, N-Methyl-D-Aspartate, iGluR, Ionotropic, TCS46b, NMDA, Receptors, NMDA, Receptors, Tocris Bioscience
