Brain 5-HT2A receptor occupancy of deramciclane in humans after a single oral administration – a positron emission tomography study

@article{Kanerva1999Brain5R,
  title={Brain 5-HT2A receptor occupancy of deramciclane in humans after a single oral administration – a positron emission tomography study},
  author={Harri Kanerva and Harry Vilkman and Kjell N{\aa}gren and Olavi Kilkku and Mikko Kuoppam{\"a}ki and Erkka Syv{\"a}lahti and Jarmo Hietala},
  journal={Psychopharmacology},
  year={1999},
  volume={145},
  pages={76-81}
}
Rationale: Deramciclane fumarate is a new 5-HT2A and 5-HT2C receptor antagonist with putative anxiolytic effects. In the present study the binding of deramciclane to serotonin 5-HT2A receptors in frontal cortex of healthy male volunteers was studied using [11C]-N-methyl spiperone ([11C]-NMSP) and positron emission tomography. Methods: The receptor occupancy percentage was assessed by the means of inhibition of [11C]-NMSP from the 5-HT2A receptors in the frontal cortex. Single oral doses of 20… Expand
Effect of the novel anxiolytic drug deramciclane on the pharmacokinetics and pharmacodynamics of the CYP3A4 probe drug buspirone
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Influence of food on the oral bioavailability of deramciclane from film-coated tablet in healthy male volunteers.
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The 24 and 31% increase in C(max) and AUC(0-infinity) of deramciclane, respectively, under fed condition is modest and probably has no clinical significance since it is relatively small compared to the inter-individual variability of these parameters. Expand
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TLDR
Here, the profiles of novel serotonin antagonists currently in preclinical development are reviewed and their therapeutic potential is assessed. Expand
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TLDR
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