Evidence from opiate binding studies that heroin acts through its metabolites.

@article{Inturrisi1983EvidenceFO,
  title={Evidence from opiate binding studies that heroin acts through its metabolites.},
  author={Charles E. Inturrisi and Misty Schultz and Seung Uoo Shin and Jason G Umans and L O Angel and Eric J. Simon},
  journal={Life sciences},
  year={1983},
  volume={33 Suppl 1},
  pages={
          773-6
        }
}
The relative affinity to opiate receptors of heroin, 6-acetylmorphine and morphine was estimated by determining their ability to displace specifically bound 3H-naltrexone from rat brain opiate binding sites. In vitro hydrolysis of heroin to 6-acetylmorphine was monitored in the binding assay filtrate by use of a quantitative HPLC procedure. The rate of heroin hydrolysis was significantly slower at 0 degrees C than at 37 degrees C. The displacement of 1 nM 3H-naltrexone by unlabeled ligand at… CONTINUE READING

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