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The serotonin 2 receptor (5-HT2 receptor) is a G protein-coupled receptor that plays key roles in neurotransmission and various physiological processes. It is comprised of three main subtypes: 5-HT2A, 5-HT2B, and 5-HT2C receptors. These receptors are involved in cognition, mood regulation, cardiac function, appetite control, and vasoconstriction. Drugs targeting this receptor family include psychedelics, antidepressants, and antipsychotics. Abnormalities in 5-HT2 receptor function are associated with psychiatric conditions such as depression, schizophrenia, and addiction, as well as cardiovascular side effects.
Agonists (e.g., LSD, psilocybin) stimulate the receptor. Antagonists (e.g., atypical antipsychotics) block the receptor. Activation leads to stimulation of phospholipase C (PLC), resulting in increased production of IP₃/DAG, intracellular calcium release, and activation of protein kinase C. Chronic administration of SSRIs and atypical antipsychotics leads to adaptive downregulation.
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