An antagonist of NR1A/2B subunit-containing NMDA receptors
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TCS 46b

Item No. 42123

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1,3-dihydro-5-[3-[4-(phenylmethyl)-1-piperidinyl]-1-propyn-1-yl]-2H-benzimidazol-2-one
CAS Number
302799-86-6
Molecular Formula
C22H23N3O
Formula Weight
345.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C1NC2=CC(C#CCN3CCC(CC3)CC4=CC=CC=C4)=CC=C2N1
InChi Code
InChI=1S/C22H23N3O/c26-22-23-20-9-8-18(16-21(20)24-22)7-4-12-25-13-10-19(11-14-25)15-17-5-2-1-3-6-17/h1-3,5-6,8-9,16,19H,10-15H2,(H2,23,24,26)
InChi Key
JJEXWPHPFZLTCU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $80

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    10 mg

    $151

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    25 mg

    $357

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    50 mg

    $634

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    Product Description

    TCS 46b is an antagonist of NMDA receptors containing NR1A/2B subunits (IC50 = 0.0053 µM).1 It is selective for NMDA receptors containing NR1A/2B subunits over NMDA receptors containing NR1A/2A and NR1A/2C subunits (IC50s = 35 and >100 µM, respectively). TCS 46b (10 mg/kg) inhibits L-DOPA-induced contralateral rotations in a rat model of Parkinson's disease induced by 6-OHDA (Item No. 25330). It has been radiolabeled and used as an NR1A/2B-selective PET radiotracer.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wright, J.L., Gregory, T.F., Kesten, S.R., et al. Subtype-selective N-methyl-D-aspartate receptor antagonists: Synthesis and biological evaluation of 1-(heteroarylalkynyl)-4-benzylpiperidines. J. Med. Chem. 43(18), 3408-3419 (2000).

    2. Roger, G., Lagnel, B., Besret, L., et al. 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(24), 5401-5408 (2003).