5-HT7 Receptor Inhibition and Inactivation Induce Antidepressantlike Behavior and Sleep Pattern

  title={5-HT7 Receptor Inhibition and Inactivation Induce Antidepressantlike Behavior and Sleep Pattern},
  author={Peter B. Hedlund and Salvador Huitrón-Reséndiz and Steven J. Henriksen and J. Gregor Sutcliffe},
  journal={Biological Psychiatry},

5-HT7 receptor modulation of sleep patterns

Findings support a role for 5-HT7 receptors in the DRN in the mechanisms underlying REM sleep formation and speculate that such ligands might exhibit utility in disorders where disrupted REM sleep is a feature.

Inactivation of the 5-HT7 receptor partially blocks PCP-induced disruption of prepulse inhibition

A partial role for the 5-HT 7 receptor is indicated in the glutamatergic PPI model of sensorimotor gating deficits in schizophrenia that is sensitive to atypical antipsychotic drugs and schizophrenia, and no involvement of this receptor in the dopaminergic PPI models that are sensitive to typical antipsychotics are indicated.

The role of serotonin 5-HT7 receptor in regulating sleep and wakefulness

The results suggest that the on-off (activation/blockade), two-state ligand-receptor interaction model is not tenable for the 5-HT7 receptor.

The 5-HT7 receptor as a mediator and modulator of antidepressant-like behavior

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.

Biochemical and Behavioral Evidence for Antidepressant-Like Effects of 5-HT6 Receptor Stimulation

5-HT6 receptor stimulation may be a mechanism initiating some of the biochemical and behavioral outcomes of 5-HT reuptake inhibitors, such as fluoxetine, which indicates that selective 5- HT6 receptor agonists may represent a novel antidepressant drug class.

Selective agonists for serotonin 7 (5-HT7) receptor and their applications in preclinical models: an overview

The data indicate that 5-HT7 receptor agonists can have neuroprotective effects against N-methyl-d-aspartate-induced toxicity, modulate neuronal plasticity in rats, enhance morphine-induced antinociception and alleviate hyperalgesia consecutive to nerve lesion in neuropathic animals.



Elevated anxiety and antidepressant-like responses in serotonin 5-HT1A receptor mutant mice.

  • L. HeislerH. Chu L. Tecott
  • Biology, Psychology
    Proceedings of the National Academy of Sciences of the United States of America
  • 1998
Results indicate that the targeted disruption of the 5-HT1A receptor gene leads to heritable perturbations in the serotonergic regulation of emotional state.

Serotonin receptor 1A knockout: an animal model of anxiety-related disorder.

  • S. RambozR. Oosting R. Hen
  • Biology, Psychology
    Proceedings of the National Academy of Sciences of the United States of America
  • 1998
It is demonstrated that mice without 5-HT1A receptors display decreased exploratory activity and increased fear of aversive environments (open or elevated spaces) and suggested that reductions in 5- HT1A receptor density due to genetic defects or environmental stressors might result in heightened anxiety.

Antidepressant-like behavioral effects in 5-hydroxytryptamine(1A) and 5-hydroxytryptamine(1B) receptor mutant mice.

The results suggest that 5-HT(1A) and 5- HT(1B) receptors have different roles in the modulation of the response to antidepressant drugs in the TST, suggesting mediation by enhanced catecholamine function.

5-HT1A/1B Receptor-Mediated Effects of the Selective Serotonin Reuptake Inhibitor, Citalopram, on Sleep: Studies in 5-HT1A and 5-HT1B Knockout Mice

Data indicate that the action of the SSRI citalopram on sleep in the mouse is essentially mediated by 5-HT1A receptors, which provides further support to the clinical strategy of antidepressant augmentation by5- HT1A antagonists, because the latter would also counteract the direct sleep-inhibitory side-effects of SSRIs.

No hypothermic response to serotonin in 5-HT7 receptor knockout mice

The results show that 5-HT-induced hypothermia is mediated by the 5- HT7 receptor, and that oleamide may act through an independent mechanism as well as at an allosteric5-HT7 receptor site to regulate body temperature.

Involvement of 5-HT1A Receptors in Homeostatic and Stress-Induced Adaptive Regulations of Paradoxical Sleep: Studies in 5-HT1A Knock-Out Mice

It is demonstrated that 5-HT1A receptors play key roles in the control of spontaneous sleep–wakefulness cycles, as well as in homeostatic regulation and stress-induced adaptive changes of paradoxical sleep.

Blockade of serotonin 5-HT1B and 5-HT2A receptors suppresses the induction of locomotor activity by 5-HT reuptake inhibitors, citalopram and fluvoxamine, in NMRI mice exposed to a novel environment: a comparison to other 5-HT receptor subtypes

The locomotor response to SSRIs of mice exposed to a novel environment is mediated via 5-HT1B and5-HT2A receptors, and the significance of these observations to the clinical actions ofSSRIs will be of interest to elucidate.