The Serotonin Receptors From Molecular Pharmacology to Human Therapeutics

Bryan L. Roth
Published in: Humana press
Release Year: 2019
ISBN: 1-59745-080-9
Pages: 637
Edition: 1st
File Size: 12 MB
File Type: pdf
Language: English

Description of The Serotonin Receptors From Molecular Pharmacology to Human Therapeutics

It has been nearly 20 years since the last Humana Press book devoted to serotonin (5-hydroxytryptamine; 5-HT) receptors has appeared. Since then, the field of 5-HT receptors has undergone a revolution due to the discovery of many additional 5-HT receptors. Although 5-HT was chemically elucidated in 1948 by Page and colleagues (Rapport et al., 1948) and 5-HT receptors initially classified in 1957 (Gaddum and Picarelli, 1957), the complexity of 5-HT pharmacology was not fully appreciated until the late 1970s and early 1980s when many puta- tive 5-HT receptors were identified by radioligand binding studies (e.g., 5-HT1A,  5-HT2, 5-HT1E and so on) (Leysen et al., 1979; Hamon et al., 1980; Peroutka et al., 1981; Leonhardt et al., 1989). The first 5-HT receptors were cloned in 1988 (Fargin et al., 1988; Julius et al., 1988) and the discovery of 14 distinct human 5-HT receptors since then ushered in the era of 5-HT receptor molecular biology (Kroeze et al., 2003). The cloning and sequencing of 5-HT receptors has also revealed the presence of post-transcriptionally modified mRNA species (RNA editing) (Burns et al., 1997) as well as naturally occurring mutations and their relations to various diseases (e.g., single nucleotide polymorphisms; SNPs) (Arranz et al., 1995).
The identification of the amino acid sequences of 5-HT receptors has allowed us to predict how 5-HT and related agonists bind to and activate 5-HT receptors  (Shapiro et al., 2000; Shapiro et al., 2002). The hope has been that this information will lead, eventually, to the development of novel, subtype-selective 5-HT receptor agonists and antagonists (Kroeze et al., 2002). The first several chapters of The Serotonin Receptors: From Molecular Pharmacology to Human Therapeutics are aimed at reviewing our knowledge of the molecular and structural biology of 5-HT receptors, followed by our current understanding of 5-HT receptor pharmacology. The elucidation of the sequences of 5-HT receptors has also facilitated the development of highly selective tools for mapping the distribution of 5-HT receptors. These tools include selective 5-HT receptor antibodies and hybridization probes. The use of these biochemical probes has revealed an unexpected complexity in both the cellular and subcellular distribution of 5-HT receptors.
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