Determinants of trapping block of N-methyl-d-aspartate receptor channels.

  title={Determinants of trapping block of N-methyl-d-aspartate receptor channels.},
  author={Konstantin V Bolshakov and Valery E Gmiro and Denis B. Tikhonov and Lev G Magazanik},
  journal={Journal of neurochemistry},
  volume={87 1},
Open channel blockers of NMDA receptors interact with the channel gate in different ways. Compounds like MK-801 and phencyclidine exhibit pronounced trapping block, whereas 9-aminoacridine and tetrapentylammonium cannot be trapped. Some blockers such as memantine and amantadine exhibit intermediate properties, so called 'partial trapping'. To analyze the determinants of trapping we have synthesized a series of mono- and dicationic derivatives of phenylcyclohexyl. The blocking action of these… CONTINUE READING