Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Chemical Compound Review:

L-CCG-IV (1S,2R)-2-[(S)-amino- carboxy...

Synonyms: Tocris-0332, Tocris-0333, AC1NSJQH, CHEMBL282842, SureCN9078498, ...

Sugawara, M. et al., Hirano, A. et al., Nakamura, Y. et al.

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High impact information on L-CCG-IV

The (2S,3R,4S)-isomer (L-CCG-IV) also inhibited the glutamate uptake in GPV and synaptosomes, but it was about 100 times less active than L-CCG-III [1].
These results suggest that the agonist selectivity in terms of the total ion flux through the single epsilon1/zeta1 NMDA receptor is in the order of L-CCG-IV approximately = L-glutamate > NMDA [2].
The order of selectivity among the relevant agonists for the NMDA receptor subtype was found to be L-CCG-IV > L-glutamate > NMDA, which is consistent with the order of binding affinity of these agonists towards the same NMDA subtypes [3].
A new method for evaluating chemical selectivity of agonists towards receptor ion channel proteins is proposed by using glutamate receptor (GluR) ion channel proteins and their agonists N-methyl-D-aspartic acid (NMDA), L-glutamate, and (2S, 3R, 4S) isomer of 2-(carboxycyclopropyl)glycine (L-CCG-IV) [3].

References

(2S,3S,4R)-2-(carboxycyclopropyl)glycine, a potent and competitive inhibitor of both glial and neuronal uptake of glutamate. Nakamura, Y., Kataoka, K., Ishida, M., Shinozaki, H. Neuropharmacology (1993) [Pubmed]
Evaluation of agonist selectivity for the NMDA receptor ion channel in bilayer lipid membranes based on integrated single-channel currents. Hirano, A., Sugawara, M., Umezawa, Y., Uchino, S., Nakajima-Iijima, S. Biosensors & bioelectronics. (2000) [Pubmed]
Electrochemical evaluation of chemical selectivity of glutamate receptor ion channel proteins with a multi-channel sensor. Sugawara, M., Hirano, A., Rehák, M., Nakanishi, J., Kawai, K., Sato, H., Umezawa, Y. Biosensors & bioelectronics. (1997) [Pubmed]

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