Effects of the brain-penetrant and selective 5-HT6 receptor antagonist SB-399885 in animal models of anxiety and depression

  title={Effects of the brain-penetrant and selective 5-HT6 receptor antagonist SB-399885 in animal models of anxiety and depression},
  author={Anna Wesołowska and Agnieszka Nikiforuk},

The selective 5-HT(6) receptor antagonist SB-399885 enhances anti-immobility action of antidepressants in rats.

Anxiolytic-like and antidepressant-like effects produced by the selective 5-HT6 receptor antagonist SB-258585 after intrahippocampal administration to rats

The results obtained indicate that the hippocampus is one of the neuroanatomical sites involved in the anxiolytic-like and antidepressant-like activity of the selective 5-HT6 receptor antagonist SB-258585.

Antidepressant-like effects of a novel 5-HT3 receptor antagonist 6z in acute and chronic murine models of depression

6z is a novel 5-HT3 receptor antagonist with potential antidepressant-like activities, which may be related to modulating hypothalamic-pituitary-adrenal axis and attenuating brain oxidative damage.

The 5-HT6 receptor agonist EMD 386088 produces antidepressant and anxiolytic effects in rats after intrahippocampal administration

The results of the present study demonstrate that the 5-HT6 agonist produces antidepressant- and anxiolytic-like effects and that the hippocampus could be one of the brain regions involved in this action.

Agonist E-6837 and antagonist SB-271046 of 5-HT6 receptors both reverse the depressive-like effect induced in mice by subchronic ketamine administration

The current findings suggest an important role for these 5-HT6R ligands as mood modulators in schizophrenia, however, it is necessary to explore the physiological mechanisms involved in this process in greater detail.

Study on the effect of EMD386088, a 5-HT6 receptor partial agonist, in enhancing the anti-immobility action of some antidepressants in rats

The results obtained from the forced swim test in rats indicate that an activation of 5HT6 receptor may facilitate antidepressant-like activity of some antidepressants and the interaction between EMD386088 and imipramine could not have been pharmacokinetic in nature.

The 5-hydroxytryptamine (serotonin) receptor 6 agonist EMD 386088 ameliorates ketamine-induced deficits in attentional set shifting and novel object recognition, but not in the prepulse inhibition in rats

The beneficial effects of the 5-HT6 agonist in ameliorating some of the ketamine-induced deficits relevant to schizophrenia seem likely to represent a useful pharmacological approach to the treatment of cognitive disturbances observed in this disorder.



Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-HT6 receptor antagonist.

A functional correlation between 5-HT(6) receptors and cholinergic neurotransmission could be shown, supporting the therapeutic potential of 5- HT( 6) receptors in the treatment of cognitive deficits.

The Selective 5-HT6 Receptor Antagonist Ro4368554 Restores Memory Performance in Cholinergic and Serotonergic Models of Memory Deficiency in the Rat

Although Ro4368554 did not improve a time-related retention deficit, it reversed a cholinergic and a serotonergic memory deficit, suggesting that both mechanisms may be involved in the facilitation of object memory by Ro4 368554 and, possibly, other 5-HT6 receptor antagonists.

The 5-HT6 Receptor Antagonist SB-271046 Reverses Scopolamine-Disrupted Consolidation of a Passive Avoidance Task and Ameliorates Spatial Task Deficits in Aged Rats

A significant improvement of task recall suggests SB-271046, in addition to inducing symptomatic cognition-enhancing actions, also attenuates age-related decline in neural function.

The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.

The affinities of 14 5-HT6 receptor ligands at this binding site were similar to those found for the recombinant rat and human 5- HT6 receptor, which suggested the presence of 5-hydroxytryptamine6 receptors in porcine striatum.

Role of the cannabinoid system in the effects induced by nicotine on anxiety-like behaviour in mice

Results demonstrate that the endogenous cannabinoid system is involved in the regulation of nicotine anxiety-like behaviour in mice and provide new findings to support the use of cannabinoid antagonists in the treatment of tobacco addiction.

Nicotine and nicotinic receptor antagonists potentiate the antidepressant‐like effects of imipramine and citalopram

The present results demonstrate an unexpected interaction between nAChR ligands and imipramine and citalopram in the tail‐suspension test and the interaction betweennA ChR antagonists and antidepressants appeared synergistic.