In vivo characterization of 6beta-naltrexol, an opioid ligand with less inverse agonist activity compared with naltrexone and naloxone in opioid-dependent mice.

@article{Raehal2005InVC,
  title={In vivo characterization of 6beta-naltrexol, an opioid ligand with less inverse agonist activity compared with naltrexone and naloxone in opioid-dependent mice.},
  author={Kirsten M. Raehal and John J. Lowery and Castigliano Murthy Bhamidipati and Ryan M Paolino and Jennifer R Blair and Danxin Wang and Wolfgang Sadee and Edward J. Bilsky},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2005},
  volume={313 3},
  pages={1150-62}
}
The mu-opioid receptor displays basal signaling activity, which seems to be enhanced by exposure to opioid agonists. This study assesses the in vivo pharmacology of the putative "neutral" antagonist 6beta-naltrexol in comparison to other ligands with varying efficacy, such as naloxone, an inverse agonist in the opioid-dependent state. ICR mice were used to generate full antagonist dose-response curves for naloxone, naltrexone, nalbuphine, and 6beta-naltrexol in blocking acute antinociceptive… CONTINUE READING
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