Risperidone Irreversibly Binds to and Inactivates the h5-HT7 Serotonin Receptor

@article{Smith2006RisperidoneIB,
  title={Risperidone Irreversibly Binds to and Inactivates the h5-HT7 Serotonin Receptor},
  author={C. Smith and T. Rahman and Nicole Toohey and J. Mazurkiewicz and K. Herrick-Davis and M. Teitler},
  journal={Molecular Pharmacology},
  year={2006},
  volume={70},
  pages={1264 - 1270}
}
Risperidone displays a novel mechanism of antagonism of the h5-HT7 receptor. Pretreatment of the cells with 5 or 20 nM risperidone, followed by removal of the drug from the media, renders the 5-HT7 receptors unresponsive to 10 μM 5-HT for at least 24 h. Thus, risperidone seems to be producing a rapid, long-lasting inactivation of the h5-HT7 receptor. Whole-cell radioligand binding studies indicate that risperidone interacts in an irreversible or pseudo-irreversible manner with the h5-HT7… Expand
56 Citations
Cellular mechanisms of the 5-HT7 receptor-mediated signaling
  • 50
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 25 REFERENCES
Biochemical profile of risperidone, a new antipsychotic.
  • 385
Persistent Binding and Functional Antagonism by Xanomeline at the Muscarinic M5 Receptor
  • 29
  • PDF
Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs
  • 25
Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
  • 634
Constitutive activity of G-protein coupled receptors: emphasis on serotonin receptors.
  • 45
Desensitization of G protein-coupled receptors and neuronal functions.
  • 778
  • PDF
Historical review: a brief history and personal retrospective of seven-transmembrane receptors.
  • R. Lefkowitz
  • Biology, Medicine
  • Trends in pharmacological sciences
  • 2004
  • 386
Classification of typical and atypical antipsychotic drugs on the basis of dopamine D-1, D-2 and serotonin2 pKi values.
  • 1,271
...
1
2
3
...