The NMDA receptor complex (NRC) consists of 4 subunits surrounding a central channel with high permeability for Ca2+ ions. The channel is blocked by the dissociative anesthetics phencyclidine and ketamine. In cooperation with Friedrich Hammerschmidt (Organic Chemistry, University Vienna) we studied SARs of various phenyl and diphenylamines as blockers of [3H]MK-801 binding to the NRC on rat brain membranes. Molecular modeling studies in cooperation with Peter Wolschann (Theoretical Chemistry, University Vienna) elucidate SARs of indolalkylamines at this site.
Berger & Rebernik (2015) Bioorg Med Chem Lett 25:4131
Palangsuntikul et al (2013) Molecules 18:8799
Berger et al (2012) Curr Med Chem 19:3044
Berger et al (2009) Bioorg Med Chem 17:3456 pdf
Berger (2000) Neurosci Lett 296:29
The polyamines spermidine and spermine are better known for their essential role in DNA duplication, but they also stimulate conductance and opening frequency of the NRC associated ion channel. This activity is related to influences by protons, by zinc, and by ifenprodil. In cooperation with several organic synthesis labs, we study SARs of polyamine derivatives at the NRC.
Berger et al (2015) Bioorg Med Chem 23:4489
Berger et al (2013) ChemMedChem 8:82 pdf
Pöhler et al (2007) Eur J Med Chem 42:175 pdf
Berger et al (2006) Bioorg Med Chem Lett 16:2837 pdf
Berger & Noe (2003) Curr Top Med Chem 3:51 pdf
Berger & Rebernik (1999) J Pharmacol Exp Ther 289:1584
Berger et al (1998) Eur J Med Chem 33:3
Donkor & Berger (1997) Bioorg Med Chem Lett 7:1455
Berger et al (1996) Neurosci Lett 203:25
Berger et al (1992) Neurosci Lett 142:85