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Submit ReviewTCS 46b
Description: GluN1A/GluN2B-selective NMDA antagonist; orally bioavailable
Chemical Name: 1,3-Dihydro-5-[3-[4-(phenylmethyl)-1-2H-benzimidazol-2-one
Purity: ≥98% (HPLC)
Biological Activity for TCS 46b
TCS 46b is an orally active, subtype-selective GluN1A/GluN2B (formally NR1A/NR2B) NMDA receptor antagonist (IC50 values are 5.3, 35000 and > 100000 nM for GluN1A/2B (NR1A/2B), GluN1A/2B (NR1A/2B) and GluN1A/2C (NR1A/2C) receptor subtypes respectively). Potentiates the effect of L-DOPA in 6-OHDA-lesioned rats following oral administration.
Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
Technical Data for TCS 46b
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for TCS 46b
References for TCS 46b
References are publications that support the biological activity of the product.
Wright et al (2000) Subtype-selective N-MthD.-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
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Keywords: TCS 46b, TCS 46b supplier, Orally, active, subtype-selective, NR1A/NR2B, antagonists, Glutamate, NMDA, Receptors, N-Methyl-D-Aspartate, iGluR, Ionotropic, TCS46b, GluN1, GluN2B, 2782, Tocris Bioscience
1 Citation for TCS 46b
Citations are publications that use Tocris products. Selected citations for TCS 46b include:
Carlson et al (2012) Pharmacological evidence that D-aspartate activates a current distinct from ionotropic glutamate receptor currents in Aplysia californica. Brain Behav 2 391 PMID: 22950043
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