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={Gertrud Haeseler and Martin Leuwer},
  journal={European Journal of Anaesthesiology},
  year={2003},
  volume={20},
  pages={220-224}
}
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… 
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In vitro and in vivo measurements show that 4-fluoropropofol and propofol have similar effects on NaChBac function and nearly identical anesthetizing effects on tadpole mobility, and the molecular basis for understanding the net inhibitory action of prop ofol on NaV channels is provided.
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TLDR
This clinical case demonstrates that Propofol could possibly have antihyperalgesic effects on opioid induced hyperalgesia caused by high-doses of chronic opioids and worsened by fentanyl.
Effect of cholinergic crisis on the potency of different emergency anaesthesia protocols in soman-poisoned rats
TLDR
Despite severe cholinergic crisis, sufficient anaesthetic depth could be achieved in all animals and did not confirm concerns of altered potency of existing anaesthetic protocols for the application of propofol or thiopental with fentanyl due to soman poisoning.
The Effects of Etomidate and Propofol Induction on Hemodynamic and Endocrine Response in Patients Undergoing Coronary Artery Bypass Graft Surgery on Cardiopulmonary Bypass
TLDR
Serum cortisol levels in both groups are well above the baseline at twenty-four hours without any untoward effects, and etomidate provides more stable hemodynamic parameters when used for induction of anesthesia as compared to propofol.
The comparison of preemptive effects of propofol, remifentanil and ketamine on post-operative pain scores and analgesic requirements in elective lower abdominal surgery under general anesthesia: A randomized, double-blinded study
  • K. Naghibi, P. Kashefi, A. Abtahi
  • Medicine, Biology
    Journal of research in medical sciences : the official journal of Isfahan University of Medical Sciences
  • 2013
TLDR
The pain scores were significantly lower in remifentanil group immediately after recovery and also at 2 and 6 h post-operatively, but it reversed at 12 and 24 h after recovery comparing with propofol and ketamine.
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