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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
TLDR
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.
Serotonin2C receptors tonically suppress the activity of mesocortical dopaminergic and adrenergic, but not serotonergic, pathways: A combined dialysis and electrophysiological analysis in the rat
TLDR
5‐HT2C receptors exert a tonic, suppressive influence on the activity of mesocortical — as well as mesolimbic and nigrostriatal — dopaminergic pathways, likely via indirect actions expressed at the level of their cell bodies.
(1-(2,5-dimethoxy-4 iodophenyl)-2-aminopropane)-induced head-twitches in the rat are mediated by 5-hydroxytryptamine (5-HT) 2A receptors: modulation by novel 5-HT2A/2C antagonists, D1 antagonists and
TLDR
It is demonstrated that 5-HT2A receptors mediate HTW in rats and that both D1 and D2 receptors as well as (postsynaptic) 5- HT1A receptors play a role in their expression.
Anxiolytic properties of agomelatine, an antidepressant with melatoninergic and serotonergic properties: role of 5-HT2C receptor blockade
TLDR
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.
TLDR
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.
The transient receptor potential protein (Trp), a putative store‐operated Ca2+ channel essential for phosphoinositide‐mediated photoreception, forms a signaling complex with NorpA, InaC and InaD.
TLDR
It is suggested that the organization of signal transducing proteins into a multiprotein complex provides the structural basis for an efficient and fast activation and regulation of Ca2+ entry through the Trp channel.
Contrasting mechanisms of action and sensitivity to antipsychotics of phencyclidine versus amphetamine: importance of nucleus accumbens 5‐HT2A sites for PCP‐induced locomotion in the rat
TLDR
PCP‐induced locomotion (PLOC) was potently blocked by the selective serotonin (5‐HT)2A vs. D2 antagonists, SR46349, MDL100,907, ritanserin and fananserin, which barely affected amphetamine‐induced Locomotion (ALOC), which is, correspondingly, more potents blocked than ALOC by antipsychotics displaying marked affinity at 5‐HT2A receptors.
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
TLDR
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.
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