Receptor-binding properties in vitro and in vivo of ritanserin: A very potent and long acting serotonin-S2 antagonist.

@article{Leysen1985ReceptorbindingPI,
  title={Receptor-binding properties in vitro and in vivo of ritanserin: A very potent and long acting serotonin-S2 antagonist.},
  author={Jos{\'e}e E. Leysen and Walter Gommeren and Paul van Gompel and J. Wynants and Paul M. F. Janssen and Pierre M. Laduron},
  journal={Molecular pharmacology},
  year={1985},
  volume={27 6},
  pages={600-11}
}
In vitro and in vivo receptor-binding properties of the new serotonin antagonist, ritanserin, are reported. In in vitro binding assays, ritanserin shows high affinity binding to serotonin-S2 sites in rat frontal cortex tissue: IC50 = 0.9 nM without drug preincubation and 0.3 nM with 30-min drug preincubation; IC50 values for histamine-H1, dopamine-D2, and adrenergic-alpha 1 and -alpha 2 sites were 39-, 77-, 107-, and 166-fold higher, and at up to 1 microM, the drug did not bind to serotonin-S1… CONTINUE READING