The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways.

@article{Millan2003TheNM,
  title={The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways.},
  author={Mark J. Millan and Anthony Gobert and Françoise Lejeune and Anne Dekeyne and Adrian Newman-Tancredi and Val{\'e}rie Pasteau and J.-M. Rivet and Didier Cussac},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2003},
  volume={306 3},
  pages={
          954-64
        }
}
  • Mark J. Millan, Anthony Gobert, +5 authors Didier Cussac
  • Published in
    The Journal of pharmacology…
    2003
  • Chemistry, Medicine
  • Agomelatine (S20098) displayed pKi values of 6.4 and 6.2 at native (porcine) and cloned, human (h)5-hydroxytryptamine (5-HT)2C receptors, respectively. It also interacted with h5-HT2B receptors (6.6), whereas it showed low affinity at native (rat)/cloned, human 5-HT2A (<5.0/5.3) and 5-HT1A (<5.0/5.2) receptors, and negligible (<5.0) affinity for other 5-HT receptors. In antibody capture/scintillation proximity assays, agomelatine concentration dependently and competitively abolished h5-HT2C… CONTINUE READING

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