Background: The aim of this review was to identify the mechanisms by which serotonin
receptors involved at the central level are able to modulate the nociceptive response. Pain is a defense
mechanism of the body that entails physiological, anatomical, neurochemical, and psychological
changes, and is defined as an unpleasant sensory and emotional experience with potential
risk of tissue damage, comprising the leading cause of appointments with Physicians worldwide.
Treatment for this symptom has generated several neuropharmacological lines of research, due to
the different types of pain and the various drugs employed to treat this condition. Serotonin [5-
HydroxyTryptamine (5-HT)] is a neurotransmitter with seven families (5-HT1–5-HT7) and approximately
15 receptor subtypes. Serotonin modulates neuronal activity; however, this neurotransmitter
is related with a number of physiological processes, such as cardiovascular function,
gastric motility, renal function, etc. On the other hand, several researches reported that serotonin
modulates nociceptive response through 5-HT1, 5-HT2, 5-HT3, and 5-HT7 receptors in the Central
Nervous System (CNS).
Method: In this review, a search was conducted on PubMed, ProQuest, EBSCO, and the Science
Citation Index for studies evaluating the effects of 5-HT1, 5-HT2, 5-HT3, and 5-HT7 receptors in the
CNS on the modulation of different types of pain.
Conclusion We concluded that 5-HT1, 5-HT2, 5-HT3, and 5-HT7 receptors in the CNS modulate the
pain, but this depends on the distribution of the receptors, dose of agonists or antagonists, administration
route, pain type and duration in order to inhibit, excite, or even maintain the nociceptive