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.

Table of Contents

Preface. Chapter 1. Serotonin Receptor Subtypes. 5-Hydroxytryptamine receptor subtypes (S.J. Peroutka). Chapter 2. 5-HT1A Receptors. 5-HTIA Receptor ligands (I. van Wijngaarden, W. Soudijn, M.Th.M. Tulp). Structural characteristics of 5-HTIA receptors and their ligands (W. Kuipers). 5-HTIA Receptor coupling to G-proteins (W. Soudijn). Ligand binding assays (M.Th.M. Tulp, I. van Wijngaarden). 5-HTIA Behavioural models (J. Mos, B. Olivier). Therapeutic applications 5-HTIA receptor ligands (I. van Wijngaarden). Chapter 3. 5-HTIB Receptors. 5-HTIB Receptor ligands (I. van Wijngaarden, W. Soudijn). 5-HTIB Receptors (W. Kuipers). Chapter 4. 5-HTID Receptors. 5-HTID Receptors (D.N. Middlemiss, M.S. Beer, V.G. Matassa). Chapter 5. 5-HTIE, 5-HTIF Receptors. 5-HTIE and 5-HTIF Receptors (G. McAllister, J.L. Castro). Chapter 6. 5-HT2A, 5-HT2B and 5-HT2c Receptors. 5-HT2A, 5-HT2B and 5-HT2c Receptor ligands (I. van Wijngaarden, W. Soudijn). The 5-HT2,-type receptor family(E. Ronken, B. Olivier). 5-HT2 Receptor antagonists: (potential) therapeutics (W. Soudijn). Chapter 7. 5-HT3 Receptors. 5-HT3 Receptors (H. Gozlan). Chapter 8. 5-HT4 Receptors. 5-HT4 Receptors (A. Dumuis, H. Ansanay, C. Waeber, M. Sebben, L. Fagni, J. Bockaert). Chapter 9. 5-HT5, 5-HT6 and 5-HT7 Receptors. The 5-HT5, 5-HT6 and 5-HT7 Receptors (R. Grailhe, U. Boschert, R. Hen). Chapter 10. 5-HT Transporter. 5-HT Transporter (W. Soudijn, I. van Wijngaarden). Index.


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© 1997
Elsevier Science
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