The 5-HT3 Receptor
5-Hydroxytryptamine (5-HT), also known as serotonin, was initially identified as a potent vasoconstrictor present in blood serum (Rapport et al. 1947), but it has become obvious over the years that 5-HT has a multitude of functions, including activation or inhibition of muscle, exocrine and endocrine glands, central and peripheral neurons, and cells of the hematopoietic and immune systems. 5-HT initiates its actions by binding to specific receptor proteins in the cell membrane. These 5-HT receptors were initially subdivided into D and M subtypes, based on their sensitivity to dibenyline or morphine (Gaddum and Picarelli 1957). This was an oversimplification, and currently 5-HT receptors are divided into seven major families (5-HT1–7) based on transduction and structural characteristics. All of these receptors exert their effects via G proteins, except for the 5-HT3receptor which is a ligand-gated ion channel...
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