Opiate receptor binding-effect relationship: Sufentanil and etorphine produce analgesia at the μ-site with low fractional receptor occupancy

@article{Rosenbaum1984OpiateRB,
  title={Opiate receptor binding-effect relationship: Sufentanil and etorphine produce analgesia at the μ-site with low fractional receptor occupancy},
  author={Jan S. Rosenbaum and Nick H G Holford and Wolfgang Sadee},
  journal={Brain Research},
  year={1984},
  volume={291},
  pages={317-324}
}
The analgesic activity of the opiate agonists etorphine and sufentanil and the antagonistic effects of diprenorphine and naloxone have been related to the occupancy of 3 classes of opiate binding sites previously defined in vivo in order to establish their pharmacological significance. Sufentanil binds specifically in vivo to the first type of site (site 1), exhibiting approximately 1100-fold selectivity over site 2, whereas etorphine displays approximately 20-fold selectivity for site 1 over… CONTINUE READING