Serotonin 5-HT1A Receptors as Targets for Agents to Treat Psychiatric Disorders: Rationale and Current Status of Research

  title={Serotonin 5-HT1A Receptors as Targets for Agents to Treat Psychiatric Disorders: Rationale and Current Status of Research},
  author={Pau Celada and Anal{\'i}a Bortolozzi and Francesc Casa{\~n}as Artigas},
  journal={CNS Drugs},
Psychiatric disorders represent a large economic burden in modern societies. However, pharmacological treatments are still far from optimal. Drugs used in the treatment of major depressive disorder (MDD) and anxiety disorders (selective serotonin [5-HT] reuptake inhibitors [SSRIs] and serotonin-noradrenaline reuptake inhibitors [SNRIs]) are pharmacological refinements of first-generation tricyclic drugs, discovered by serendipity, and show low efficacy and slowness of onset. Moreover… 

Functional Selectivity and Antidepressant Activity of Serotonin 1A Receptor Ligands

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The novel antidepressants vortioxetine, vilazodone and milnacipran/levomilnacIPran are featured with regard to their serotonin receptor targets which may account for their specific effects on certain symptoms of depression as well as a characteristic side-effect profile.

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This newly identified binding mechanism underlying vilazodone's partial agonism to the 5-HT1A receptor will provide valuable information for medicinal chemists working in the field of rational design of novel SPARIs for MDD treatment.

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It is proposed that TRD may not represent a simple serotonin deficit state but rather an excess of midbrain peri-raphe serotonin and subsequent deficit at key fronto-limbic projection sites, with ultimate compromise in serotonin-mediated neuroplasticity.

Chronic Treatment with the 5-HT1A Receptor Partial Agonist Tandospirone Increases Hippocampal Neurogenesis

The results strongly suggest that 5-HT1A receptor partial agonists would be useful and beneficial in the treatment of depressive and anxiety disorders through increased hippocampal neurogenesis.



Serotonin receptors involved in antidepressant effects.

  • F. Artigas
  • Biology, Psychology
    Pharmacology & therapeutics
  • 2013

5-HT1A receptor function in major depressive disorder

The role of serotonin receptor subtypes in treating depression: a review of animal studies

The involvement of 5- HT receptors in the antidepressant-like effects of SSRIs is complex and involves the orchestration of stimulation and blockade at different 5-HT receptor subtypes.

The 5-HT1A receptor in schizophrenia: a promising target for novel atypical neuroleptics?

There is now a sufficient rationale to examine thoroughly the role of the 5-HT1A receptor in schizophrenia and antipsychotic drug treatment, and the anticataleptic activity of 5- HT1A agonist augmentation of neuroleptics in the treatment of schizophrenia.

Therapeutic Role of 5‐HT1A Receptors in The Treatment of Schizophrenia and Parkinson's Disease

  • Y. Ohno
  • Psychology, Medicine
    CNS neuroscience & therapeutics
  • 2011
Evidence that 5‐HT1A receptors seem to be a promising target for alleviating antipsychotic‐induced extrapyramidal side effects (EPS) and cognitive/affective disorders in schizophrenia and Parkinson's disease should encourage discovery of new 5‐ HT1A ligands, which can resolve the unmet clinical needs in the current therapy.

Is there a role for 5-HT1A agonists in the treatment of depression?

Modifying 5-HT1A Receptor Gene Expression as a New Target for Antidepressant Therapy

Down-regulation of 5-HT1A autoreceptor expression, not simply desensitization of receptor signaling, appears to be required to enhance and accelerate antidepressant action.

Improving the treatment of schizophrenia: focus on serotonin (5-HT)(1A) receptors.

  • M. Millan
  • Psychology, Biology
    The Journal of pharmacology and experimental therapeutics
  • 2000
Clinical studies of antipsychotics interacting with 5-HT(1A) receptors are required to establish their genuine pertinence to the-hopefully improved-treatment of schizophrenia.

Serotonin 5-HT1a Receptor Agonists as Antidepressants

For 20 years serotonin 5-HT1A receptor agonists have been evaluated for effectiveness in treating depressive disorders and depressive symptoms occurring in a range of diagnostic categories, including major and minor depression, mixed states of anxiety and depression, and mixed syndromes of depression and alcohol dependence.

Serotonin 5-HT1A receptor binding in people with panic disorder: positron emission tomography study.

  • J. NashP. Sargent D. Nutt
  • Medicine, Biology
    The British journal of psychiatry : the journal of mental science
  • 2008
Panic disorder is associated with reduced 5-HT(1A) receptor availability, which is also known to have a key role in depression.