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Serotonin (5-hydroxytryptamine, 5-HT), like many other mammalian neurotransmitters, plays a wide variety of roles in human health and disease. The diversity of 5-HT receptors, represented by at least seven protein families, offers a fascinating system in which to study the mechanisms by which receptor diversity is generated and regulated. This month's review article by Sanders-Bush et al. details these mechanisms. Cover image: Computational model of the 5-HT 2C receptor, highlighting two tyrosine residues implicated in receptor conformational regulation. [Published with permission; from Prioleau et al., J. Biol. Chem. 277, 36577-36584. Copyright (2002) JBC.]