High-affinity block of voltage-operated rat IIA neuronal sodium channels by 2,6 di-tert-butylphenol, a propofol analogue

@article{Haeseler2003HighaffinityBO,
  title={High-affinity block of voltage-operated rat IIA neuronal sodium channels by 2,6 di-tert-butylphenol, a propofol analogue},
  author={G. Haeseler and M. Leuwer},
  journal={European Journal of Anaesthesiology},
  year={2003},
  volume={20},
  pages={220-224}
}
  • G. Haeseler, M. Leuwer
  • Published 2003
  • Medicine
  • European Journal of Anaesthesiology
  • Background and objective: Propofol is a phenol derivative (2,6 di-isopropylphenol) with a unique effect profile including activating effects on GABAA and blocking effects on voltage-operated sodium channels. If the substituents in the 2- and the 6-positions are replaced by tert-butyl groups, the resulting phenol derivative, 2,6 di-tert-butylphenol, despite being a close structural propofol analogue, completely lacks GABAA receptor effects. The aim of this in vitro study was to investigate the… CONTINUE READING

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