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={M. Millan and A. Gobert and F. Lejeune and A. Dekeyne and A. Newman-Tancredi and V. Pasteau and J.‐M. Rivet and D. Cussac}, journal={Journal of Pharmacology and Experimental Therapeutics}, year={2003}, volume={306}, pages={954 - 964} }
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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References
SHOWING 1-10 OF 74 REFERENCES
5-HT2C receptor agonists: pharmacological characteristics and therapeutic potential.
- Chemistry, Medicine
- The Journal of pharmacology and experimental therapeutics
- 1998
- 310
5-HT2C receptors mediate penile erections in rats: actions of novel and selective agonists and antagonists.
- Chemistry, Medicine
- European journal of pharmacology
- 1997
- 116
Melatonin modulates the sensitivity of 5-hydroxytryptamine-2 receptor-mediated sleep—wakefulness regulation in the rat
- Biology, Medicine
- Neuroscience Letters
- 1989
- 43
Serotonin 5-HT2c agonists mimic the effect of light pulses on circadian rhythms
- Biology, Medicine
- Brain Research
- 1998
- 101
Melatonin agonists modulate 5-HT2A receptor-mediated neurotransmission: behavioral and biochemical studies in the rat.
- Biology, Medicine
- The Journal of pharmacology and experimental therapeutics
- 1995
- 60
Differential activation of Gq/11 and Gi(3) proteins at 5-hydroxytryptamine(2C) receptors revealed by antibody capture assays: influence of receptor reserve and relationship to agonist-directed trafficking.
- Medicine, Chemistry
- Molecular pharmacology
- 2002
- 105
- PDF
Evidence for accelerated desensitisation of 5-HT2C receptors following combined treatment with fluoxetine and the 5-HT1A receptor antagonist, WAY 100,635, in the rat
- Medicine
- Neuropharmacology
- 2000
- 73
Determination of the dose of agomelatine, a melatoninergic agonist and selective 5-HT2C antagonist, in the treatment of major depressive disorder: a placebo-controlled dose range study
- Medicine, Psychology
- International clinical psychopharmacology
- 2002
- 348
- Highly Influential
Characterization of phospholipase C activity at h5-HT2C compared with h5-HT2B receptors: influence of novel ligands upon membrane-bound levels of [3H]phosphatidylinositols
- Medicine, Chemistry
- Naunyn-Schmiedeberg's Archives of Pharmacology
- 2002
- 77