Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: binding and patch clamp studies

@article{Kornhuber2005OrphenadrineIA,
  title={Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: binding and patch clamp studies},
  author={Johannes Kornhuber and Chris G. Parsons and S. Hartmann and Wolfgang Retz and S. Kamolz and Johannes Thome and Peter Franz Riederer},
  journal={Journal of Neural Transmission / General Section JNT},
  year={2005},
  volume={102},
  pages={237-246}
}
Orphenadrine has been used as an antiparkinsonian, antispastic and analgesic drug for many years. Here we show that orphenadrine inhibits [3H]MK-801 binding to the phencyclidine (PCP) binding site of the N-methyl-D-aspartate (NMDA)-receptor in homogenates of postmortem human frontal cortex with a Ki-value of 6.0 ± 0.7 μM. The NMDA receptor antagonistic effects of orphenadrine were assessed using concentration- and patch-clamp techniques on cultured superior colliculus neurones. Orphenadrine… 
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