5-HT2A Receptors and Pain

  • Christine Courteix
  • Amandine Dupuis
  • Pierre-Yves Martin
  • Benoit Sion
Part of the The Receptors book series (REC, volume 32)


Serotonin (5-hydroxytryptamine, 5-HT) is a key modulator of spinal nociceptive transmission. Among 5-HT receptors, the 5-HT2A subtype plays a critical role in the modulation of nociceptive information. Both pro- and antinociceptive effects of 5-HT2A receptor activation have been reported but converging evidence indicates an excitatory role for peripheral 5-HT2A receptors on pain transmission in acute, sub-chronic and chronic pain conditions. The central effects of 5-HT2A agonists which produce either anti-hyperalgesic or anti-allodynic effect seem to depend on the pathophysiology of pain. Neverthless, some data indicate that 5-HT acting drugs such as selective serotonin reuptake inhibitor (SSRI) antidepressants involve the 5-HT2A receptor to produce analgesia and that restoring 5-HT2A receptor functionality may contribute to enhance the analgesic efficacy of SSRI in metabolic and traumatic neuropathic pain.


Serotonin 5-HT2A receptor Chronic pain Acute pain PDZ-proteins Antidepressants 


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Copyright information

© Springer International Publishing AG 2018

Authors and Affiliations

  • Christine Courteix
    • 1
    • 2
  • Amandine Dupuis
    • 1
    • 2
  • Pierre-Yves Martin
    • 1
    • 2
  • Benoit Sion
    • 1
    • 2
  1. 1.INSERM U1107, NEURO-DOLClermont-FerrandFrance
  2. 2.Laboratoire de Physiologie, UFR Pharmacie, Université Clermont AuvergneClermont-FerrandFrance

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