Overview

  • Product name
    (R)-CPP, NMDA antagonist
  • Description
    Potent NMDA antagonist
  • Biological description
    Highly potent, competitive NMDA antagonist; more active enantiomer of (RS)-CPP (ab120160). (Ki values are 0.04 (NR1/NR2A), 0.3 (NR1/NR2B), 0.6 (NR1/NR2C) and 2.0 μM (NR1/NR2D)).

    Also available in simple stock solutions (ab144495) - add 1 ml of water to get an exact, ready-to-use concentration.
  • CAS Number
    126453-07-4
  • Chemical structure
    Chemical Structure

Properties

Associated products

Images

  • Transporter blockade does not reveal an ambient glutamate concentration gradient between extracellular compartments.

    A. Average Ca2+ increase in a spine during a 40 ms voltage step, with iontophoresis of L-aspartate (black), without iontophoresis (red), a second L-aspartate application (gray), L-aspartate in the presence of 100 µM TBOA (blue), and TBOA alone (green).

    B. Comparison of spine Ca2+ transients in each condition, normalized to the first response to L-aspartate iontophoresis (n = 5). Error bars indicate SEM. Significance determined by Friedman ANOVA with Conover posthoc test: *p<0.05; **p<0.01; ***p<0.001.

    If the extrasynaptic glutamate concentration is higher than that in the cleft because transporters prevent diffusion of glutamate into the synapse, blocking transporters should result in a large Ca2+ increase in the spine as extrasynaptic glutamate rushes into the cleft and activates synaptic NMDARs. Spines exhibited a Ca2+ increase during a 40 ms depolarization with iontophoresis of the glutamate transporter substrate and NMDAR agonist, L-aspartate (A; black and gray traces), confirming the presence of NMDARs. However, TBOA (100 µM) did not increase the Ca2+ transient in the same spines during the 40 ms depolarization when compared to the control voltage step without L-aspartate iontophoresis (See image compare green and red traces; 20.6±13.62%; p>0.5; n = 5;). TBOA was effective in blocking transporters, however, as the NMDAR-mediated Ca2+ signal evoked by iontophoresis of L-aspartate was increased in the presence of TBOA (See image). This result indicates that glutamate transporters do not normally generate a concentration gradient of ambient glutamate between extrasynaptic and synaptic extracellular compartments.

References

This product has been referenced in:
  • Paoletti P & Neyton J NMDA receptor subunits: function and pharmacology. Curr Opin Pharmacol 7:39-47 (2007). Read more (PubMed: 17088105) »
  • Lowe DA  et al. D-CPP-ene (SDZ EAA 494), a potent and competitive N-methyl-D-aspartate (NMDA) antagonist: effect on spontaneous activity and NMDA-induced depolarizations in the rat neocortical slice preparation, compared with other CPP derivatives and MK-801. Neurosci Lett 113:315-21 (1990). Read more (PubMed: 2166255) »
See all 11 Publications for this product

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