Deramciclane, a putative anxiolytic drug, is a serotonin 5-HT2C receptor inverse agonist but fails to induce 5-HT2C receptor down-regulation

@article{Plvimki1998DeramciclaneAP,
  title={Deramciclane, a putative anxiolytic drug, is a serotonin 5-HT2C receptor inverse agonist but fails to induce 5-HT2C receptor down-regulation},
  author={E. P{\"a}lvim{\"a}ki and H. Majasuo and M. Kuoppam{\"a}ki and P. M{\"a}nnist{\"o} and E. Syv{\"a}lahti and J. Hietala},
  journal={Psychopharmacology},
  year={1998},
  volume={136},
  pages={99-104}
}
Abstract Deramciclane (EGIS-3886) is a novel anxiolytic agent that binds with high affinity to 5-HT2A/2C receptors. The interactions of deramciclane with the serotonin 5-HT2C receptor were characterized further using receptor phosphoinositide hydrolysis assays and receptor autoradiography. Deramciclane antagonized 5-HT2C receptor mediated 5-HT-stimulated phosphoinositide hydrolysis with an IC50 value of 168 nM. Deramciclane also decreased basal phosphoinositide hydrolysis by up to 33% (EC50… Expand
Effect of the novel anxiolytic drug deramciclane on cytochrome P450 2D6 activity as measured by desipramine pharmacokinetics
The role of 5-HT2C receptors in affective disorders.
Effect of the novel anxiolytic drug deramciclane on the pharmacokinetics and pharmacodynamics of the CYP3A4 probe drug buspirone
Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors.
Relevance of dorsal raphe nucleus firing in serotonin 5-HT2C receptor blockade-induced augmentation of SSRIs effects
...
1
2
3
4
...

References

SHOWING 1-10 OF 32 REFERENCES
Chronic Citalopram and Fluoxetine Treatments Upregulate 5-HT2C Receptors in the Rat Choroid Plexus
Regulation of 5-HT2 receptors in rat cortex. Studies with a putative selective agonist and an antagonist.
5-HT1C receptor-mediated phosphoinositide hydrolysis in the rat choroid plexus after chronic treatment with clozapine.
Novel regulation of 5-HT1C receptors: down-regulation induced both by 5-HT1C/2 receptor agonists and antagonists.
Repeated administration of SR 46349B, a selective 5-hydroxytryptamine2 antagonist, up-regulates 5-hydroxytryptamine2 receptors in mouse brain.
Behavioral studies with anxiolytic drugs. VI. Effects on punished responding of drugs interacting with serotonin receptor subtypes.
Regulation of 5-HT2 and 5-HT1C serotonin receptor levels. Methodology and mechanisms.
  • B. Roth, M. Hamblin, R. Ciaranello
  • Biology, Medicine
  • Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology
  • 1990
Recent developments in 5HT-related pharmacology of animal models of anxiety
  • C. Gardner
  • Medicine, Psychology
  • Pharmacology Biochemistry and Behavior
  • 1986
Putative selective 5-HT-2 antagonists block serotonin 5-HT-1c receptors in the choroid plexus.
...
1
2
3
4
...