The 5-HT (2A) and 5-HT (2C) receptors mediate effects of a large variety of compounds affecting depression, anxiety, hallucinations, dysthymia, sleep patterns, feeding behaviour and neuro-endocrine functions. Binding of such compounds to either 5-HT (2) receptor subtype induces processes that regulate receptor sensitivity.

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Let’s delve into the fascinating world of serotonin receptors. 🧬

1. 5-HT2A Receptor (HTR2A):

   • The 5-HT2A receptor is a subtype of the 5-HT2 receptor family. It belongs to the serotonin receptor group and is a G protein-coupled receptor (GPCR)¹.

   • Location: The 5-HT2A receptor is found on the cell surface but also has several intracellular locations¹.

   • Signaling Cascade: It primarily couples to the Gαq signal transduction pathway¹.

   • Function:

     • Excitatory: It is the main excitatory receptor subtype among the GPCRs for serotonin.

     • Inhibitory: In certain areas like the visual cortex and the orbitofrontal cortex, it may have an inhibitory effect.

   • Psychedelic Connection: The 5-HT2A receptor gained prominence due to its role as a target for serotonergic psychedelic drugs like LSD and psilocybin mushrooms.

   • Antipsychotic Action: It also mediates, at least partly, the action of many antipsychotic drugs, especially the atypical ones.

   • Depression and Suicidal Patients: Suicidal and depressed patients have been found to have more 5-HT2A receptors, suggesting their involvement in depression pathogenesis¹.

2. 5-HT2C Receptor (HTR2C):

   • The 5-HT2C receptor binds the endogenous neurotransmitter serotonin (5-HT)².

   • Location: It is located within postsynaptic structures.

   • Signaling Cascade: Like the 5-HT2A receptor, it also activates phospholipase C (PLC), resulting in depolarization of the host cell³.

   • Function:

     • Involved in various processes, including locomotory behavior, appetite regulation, and fear response.

     • It plays a role in calcium ion homeostasis and phospholipase C-activating signaling pathways.

   • RNA Editing: The 5-HT2C receptor undergoes RNA editing, leading to functional diversity.

   • Expression: It is expressed in various brain regions, including the nucleus accumbens, hypothalamus, and hippocampus².

In summary, both 5-HT2A and 5-HT2C receptors are crucial players in serotonin signaling, impacting various physiological and behavioral processes. 🌟⁴⁵