Stereochemical requirements for pseudoirreversible inhibition of opioid mu receptor binding by the 3‐methylfentanyl congeners, RTI‐46144 and its enantiomers: Evidence for different binding domains

@article{Ni1993StereochemicalRF,
  title={Stereochemical requirements for pseudoirreversible inhibition of opioid mu receptor binding by the 3‐methylfentanyl congeners, RTI‐46144 and its enantiomers: Evidence for different binding domains},
  author={Q. Ni and H. Xu and J. Partilla and P. Stark and F. Carroll and G. Brine and R. Rothman},
  journal={Synapse},
  year={1993},
  volume={15}
}
Fentanyl and its congeners are of interest not only because of their clinical applications, but also because certain members of this series of opioid analgesics exhibit unique properties, such as acting as pseudoirreversible inhibitors of μ receptor binding, both in vitro and in vivo. Previous studies showed that pretreatment of membranes with (+)‐cis‐3‐methylfentanyl resulted in a lower affinity interaction of [3H]ohmefentanyl with the μ binding site, as well as an increased dissociation rate… Expand
Fentanyl analogs: structure-activity-relationship study.
Ligand-induced changes in surface mu-opioid receptor number: relationship to G protein activation?

References

SHOWING 1-10 OF 24 REFERENCES
Differentiation of opiate and neuroleptic receptor binding in rat brain.
...
1
2
3
...