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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
- M. Millan, A. Gobert, D. Cussac
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 September 2003
In contrast to melatonin, agomelatine behaves as an antagonist at 5- HT2B and 5-HT2C receptors: blockade of the latter reinforces frontocortical adrenergic and dopaminergic transmission.
Serotonin (5-HT)2C receptors tonically inhibit dopamine (DA) and noradrenaline (NA), but not 5-HT, release in the frontal cortex in vivo
Anxiolytic properties of agomelatine, an antidepressant with melatoninergic and serotonergic properties: role of 5-HT2C receptor blockade
In contrast to melatonin, and reflecting blockade of 5-HT2C receptors, agomelatine is active in several models of anxiolytic properties in rodents and differs from that of benzodiazepines from which it may also be distinguished by its contrasting influence on corticolimbic monoaminergic pathways.
A comparative in vitro and in vivo pharmacological characterization of the novel dopamine D3 receptor antagonists (+)-S 14297, nafadotride, GR 103,691 and U 99194.
- V. Audinot, A. Newman-Tancredi, M. Millan
- BiologyThe Journal of pharmacology and experimental…
- 1 October 1998
Both (+)-S 14297 and GR 103,691 are markedly selective ligands that permit the characterization of actions at hD3 vs. hD2 receptors in vitro, but both are of greater utility for the evaluation of their functional significance in vivo.
Agonist and antagonist actions of yohimbine as compared to fluparoxan at α2‐adrenergic receptors (AR)s, serotonin (5‐HT)1A, 5‐HT1B, 5‐HT1D and dopamine D2 and D3 receptors. Significance for the…
The α2‐AR antagonist properties of yohimbine increase DA and NAD levels both alone and in association with fluoxetine, whereas fluparoxan selectively enhances hippocampal noradrenaline (NAD) turnover and enhances striatal dopamine turnover and suppresses striatal turnover of 5‐HT.
Pro-cognitive effects of 5-HT6 receptor antagonists in the social recognition procedure in rats: implication of the frontal cortex
Results indicate that 5-HT6 receptors modulate social recognition by actions in the FCX and underpin their pertinence as targets for the treatment of psychiatric disorders in which cognitive function is compromised.
Discriminative stimulus properties of the novel serotonin (5-HT)2C receptor agonist, RO60-0175: a pharmacological analysis
Citalopram reduces social interaction in rats by activation of serotonin (5-HT)2C receptors
S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: II. Functional and behavioral profile compared with GR218,231 and L741,626.
- M. Millan, A. Dekeyne, J. Rivet, T. Dubuffet, G. Lavielle, M. Brocco
- Biology, PsychologyThe Journal of pharmacology and experimental…
- 1 June 2000
D(2)-receptors are principally involved in these paradigms, although D(3)-receptionors may contribute to induction of hypothermia and PEs, and S33084 was inactive in models of potential antipsychotic and extrapyramidal activity and failed to modify spontaneous locomotor behavior.
S32006, a novel 5-HT2C receptor antagonist displaying broad-based antidepressant and anxiolytic properties in rodent models
In vitro and in vivo, the novel benzourea derivative, S32006 is a potent 5-HT2C receptor antagonist, and possesses antidepressant and anxiolytic properties in diverse rodent models.