Functional antagonism of morphine analgesia by (+)-pentazocine: evidence for an anti-opioid sigma 1 system.

@article{Chien1993FunctionalAO,
  title={Functional antagonism of morphine analgesia by (+)-pentazocine: evidence for an anti-opioid sigma 1 system.},
  author={Chih Cheng Chien and Gavril W Pasternak},
  journal={European journal of pharmacology},
  year={1993},
  volume={250 1},
  pages={R7-8}
}
Both (+)-pentazocine and (-)-pentazocine antagonize morphine analgesia equally well. This lack of stereospecificity implies an non-opioid mechanism of action. The antagonism of morphine analgesia by (+)-pentazocine is reversed by haloperidol, a potent dopamine D2 and sigma receptor antagonist. The inactivity of the highly selective dopamine D2 receptor antagonist (-)-sulpiride indicates that both (+)-pentazocine and haloperidol are acting through sigma receptors. Haloperidol, but not… CONTINUE READING

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