Serotonin Receptors and their Ligands

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B. Olivier, I. van Wijngaarden, W. Soudijn
Elsevier, 10 июл. 1997 г. - Всего страниц: 364
An international group of authors have produced an overview of the progress made in the medicinal chemistry of compounds (selectively) acting at serotonin receptors or serotonin transporters either as agonists, partial agonists or antagonists.

Structure - affinity relationships and structure - activity relationships of agonists, partial agonists, and antagonists of 5-HT receptors and uptake sites, are discussed. Structure, sequence homology and the effect of site-directed mutations of 5-HT receptors and the reuptake site on the binding of ligands show the tremendous impact of molecular biology on medicinal chemistry research. Also discussed is the pharmacology and (potential) clinical applications of ligands for the 5-HT receptors and the reuptake site. By developing elegant techniques of cloning and expression of serotonin receptor subtypes, their mutants and chimeras, a unique opportunity was offered to study the binding mode of serotoninergic ligands to their receptors and transporters.

The distribution, structure and homologies of serotonin receptor subtypes and the structure of the serotonin transporter are also taken into account.

The (potential) therapeutic applications of ligands of the different subtypes are described.

Altogether an excellent addition to the Pharmacochemical Library series.

 

Содержание

CHAPTER 2 5HT1A RECEPTORS Chapter 2
15
CHAPTER 3 5HT1B RECEPTORS Chapter 3
85
CHAPTER 4 5HT1D RECEPTORS Chapter 4
99
CHAPTER 5 5HT1E 5HT1F RECEPTORS Chapter 5
139
CHAPTER 6 5HT2A 5HT2B and 5HT2C RECEPTORS Chapter 6
159
CHAPTER 7 5HT3 RECEPTORS Chapter 7
219
CHAPTER 8 5HT4 RECEPTORS Chapter 8
259
CHAPTER 9 5HT5 5HT6 and 5HT7 RECEPTORS Chapter 9
309
CHAPTER 10 5HT TRANSPORTER Chapter 10
325
Index
363
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Стр. 4 - Indeed, the multiplicity of 5-HT receptor subtypes, both within and between species, has exceeded most of the predictions that might have been made on the basis of pharmacological data.
Стр. 8 - Finally, for all 5-HT receptors identified, the interspecies variation is minimal (ie, >90% identity between species homologs) as indicated by the very short branches linking these subtypes in the phylogenetic tree.

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