5-HT2 receptors are major targets for a wide array of psychoactive drugs, ranging from nonclassical antipsychotic drugs, anxiolytics and antidepressants, which have a 5-HT2 antagonistic action, to hallucinogens, which are agonists of the 5-HT2 receptors. The 5-HT2 receptors form a closely related subgroup of G-protein-coupled receptors and show the typical heptahelical structure of an integral membrane protein monomer. They are currently classified as 5-HT2A, 5-HT2B, and 5-HT2C subtypes, based on their close structural homology, pharmacology and signal transduction pathways. The amino acid sequence of the 5-HT2 receptors shares a high degree (>70%) of identity within the transmembrane segments and consequently, it is not surprising that many compounds bind with high affinity to all these three receptor subtypes. The high degree of sequence homology has considerably hampered the identification of selective 5-HT2C antagonists and especially, agonists (Di Giovanni et al. 2006).

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