Novel antagonists of 5-HT6 and/or 5-HT7 receptors affect the brain monoamines metabolism and enhance the anti-immobility activity of different antidepressants in rats

  title={Novel antagonists of 5-HT6 and/or 5-HT7 receptors affect the brain monoamines metabolism and enhance the anti-immobility activity of different antidepressants in rats},
  author={A. Partyka and M. Jastrzębska-Więsek and L. Antkiewicz-Michaluk and J. Michaluk and A. Wesołowska},
  journal={Behavioural Brain Research},
HighlightsPZ‐668, PZ‐1433, and ADN‐1184 showed anti‐immobility action in MED = 0.1 mg/kg.5‐HT6 and/or 5‐HT7 antagonists affected brain monoamine metabolism in different way.5‐HT6 and/or 5‐HT7 antagonists potentiated the effects of different antidepressants. Abstract The aim of the present study was to investigate and compare the ability of three novel 5‐HT6 and/or 5‐HT7 receptor antagonists as follows: PZ‐668—a preferential 5‐HT6 antagonist; PZ‐1433—a preferential 5‐HT7 antagonist; and ADN‐1184… Expand
2 Citations
The pronociceptive role of 5-HT6 receptors in ventrolateral orbital cortex in a rat formalin test model
The results suggested that 5-HT6 receptors play a pronociceptive role in the VLO in the rat formalin test due to its activation of AC - PKA pathway, and cerebral cortical 5- HT6 receptors could be a new target to develop analgesic drugs. Expand


Evidence that central 5‐HT2A and 5‐HT2B/C receptors regulate 5‐HT cell firing in the dorsal raphe nucleus of the anaesthetised rat
Recordings of 5‐HT neurones in the dorsal raphe nucleus of anaesthetised rats indicate that the inhibition of 5-HT cell firing induced by systemic administration of DOI and DOB is mediated predominantly by the5‐HT2A receptor‐subtype, but that 5‐ HT2B/C receptors also play a minor role. Expand
The Selective 5-HT2A Receptor Antagonist M100907 Enhances Antidepressant-Like Behavioral Effects of the SSRI Fluoxetine
The results will be discussed in the context that the combined blockade of 5-HT2A receptors and serotonin transporters (SERT) may result in greater efficacy in treating neuropsychiatric syndromes than blocking either site alone. Expand
5-HT6 receptor antagonist SB-399885 potentiates haloperidol and risperidone-induced dopamine efflux in the medial prefrontal cortex or hippocampus
The results suggest that the combined blockade of 5-HT6 and D2 receptors may contribute to the potentiation of haloperidol- and risperidone-induced DA efflux in the mPFC or HIP. Expand
Study into a possible mechanism responsible for the antidepressant-like activity of the selective 5-HT6 receptor antagonist SB-399885 in rats.
The results described in the present paper indicate that the anti-immobility activity of SB-399885 is not connected with 5-HT innervation, and that D(1)- and D(2-like receptors and alpha(2)-adrenoceptors are involved in this action. Expand
The selective 5-HT(6) receptor antagonist SB-399885 enhances anti-immobility action of antidepressants in rats.
The obtained results indicate that the blockade of 5-HT(6) receptors may facilitate the anti-immobility effect of imipramine, desipramsine, bupropion or moclobemide in the forced swim test. Expand
Selective Blockade of 5-Hydroxytryptamine (5-HT)7 Receptors Enhances 5-HT Transmission, Antidepressant-Like Behavior, and Rapid Eye Movement Sleep Suppression Induced by Citalopram in Rodents
Results indicate that selective blockade of 5-HT7 receptors may enhance the antidepressant efficacy of citalopram and may provide a novel therapy to alleviate sleep disturbances associated with depression. Expand
5-HT6 receptor antagonism potentiates the behavioral and neurochemical effects of amphetamine but not cocaine
The effects of a novel 5-HT(6) receptor antagonist, SB 258510A, on psychostimulant-induced motor activity, self-administration, and increases in extracellular dopamine in the nucleus accumbens and frontal cortex of male Wistar rats are characterized. Expand
Pharmacological Blockade of 5-HT7 Receptors as a Putative Fast Acting Antidepressant Strategy
Findings indicate that the 5-HT7 receptor antagonists may represent a new class of antidepressants with faster therapeutic action than the commonly prescribed antidepressant fluoxetine. Expand
Enhancement of the anti-immobility action of antidepressants by a selective 5-HT7 receptor antagonist in the forced swimming test in mice.
The obtained results indicate that blockade of 5-HT7 receptors may facilitate the anti-immobility effect of antidepressants in mice. Expand
Investigation of the SSRI augmentation properties of 5-HT2 receptor antagonists using in vivo microdialysis
Results confirm recent findings that 5-HT(2) receptor antagonists augment the effect of citalopram on extracellular 5-hydroxytryptamine (5-HT) neurones, and indicate the involvement of 5- HT(2C) and possibly 5-ht(2A) receptors. Expand