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Category: Ion ChannelsarrowLigand-gated Ion ChannelsarrowGlutamate (Ionotropic) ReceptorsarrowNMDA SelectivearrowNMDA SitearrowAntagonists
Cat.No. Product Name
2782 TCS 46b
Price and Availability

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TCS 46b
Chemical Name: 1,3-Dihydro-5-[3-[4-(phenylmethyl)-1-2H-benzimidazol-2- one

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:

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M.Wt: 345.44
Formula: C22H23N3O
Storage: Store at RT
Solubility: Soluble to 100 mM in DMSO and to 100 mM in Ethanol
Purity: >98%
CAS No: [302799-86-6]

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    References:

    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. 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.
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    Keywords: TCS 46b, Ligand-gated Ion Channels, Orally Active, Subtype-selective NR1A / NR2B Antagonist, TCS46b, Tocris Bioscience
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