Elsevier

Mendeleev Communications

Volume 30, Issue 3, May–June 2020, Pages 342-343
Mendeleev Communications

Ifenprodil-like NMDA receptor modulator based on the biphenyl scaffold

https://doi.org/10.1016/j.mencom.2020.05.027Get rights and content

Ifenprodil-like NMDA receptor negative allosteric modulator based on the biphenyl scaffold has been identified using virtual screening. Docking approach demonstrated that the modulator maintains some characteristic interactions with protein similar to ifenprodil. Electrophysiological and radioligand investigations demonstrated the concentration-dependent NMDA/Gly-induced currents inhibition with IC50 = 5 μM and significant displacement of [H3]ifenprodil with EC50 = 30 μM, respectively.

References (19)

  • R.M. Berman et al.

    Biol. Psychiatry

    (2000)
  • D.S. Karlov et al.

    Biochem. Biophys. Res. Commun.

    (2012)
  • I. Borza et al.

    Bioorg. Med. Chem. Lett.

    (2006)
  • K. Finlayson et al.

    Eur. J. Pharmacol.

    (2004)
  • S.F. Traynelis et al.

    Pharmacol. Rev.

    (2010)
  • J.C. Watkins et al.

    Br. J. Pharmacol.

    (2006)
  • J.W. Olney et al.

    Science

    (1989)
  • B. Moghaddam et al.

    J. Neurosci.

    (1997)
  • M.C. Regan et al.

    Nat. Commun.

    (2019)
There are more references available in the full text version of this article.
View full text