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 Alain P. Gobert and Françoise Lejeune and Anne Dekeyne and Adrian Newman-Tancredi and Valérie Pasteau and Jean Michel Rivet and Didier Cussac},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2003},
  volume={306},
  pages={954 - 964}
}
  • M. Millan, A. Gobert, D. Cussac
  • Published 1 September 2003
  • Biology, Chemistry
  • Journal of Pharmacology and Experimental Therapeutics
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… 
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