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.
Author(s): Oliver B., van Wijngaarden I. and Soudijn W. (Eds.)
Series: Pharmacochemistry Library 27
Publisher: Elsevier, Academic Press
Year: 1997
Language: English
Pages: 3-367
Content:
Preface
Page vii
5-Hydroxytryptamine receptor subtypes Original Research Article
Pages 3-13
Stephen J. Peroutka
5-HT1A receptor ligands Original Research Article
Pages 17-43
I. van Wijngaarden, W. Soudijn, M.Th.M. Tulp
Structural characteristics of 5-HT1A receptors and their ligands Original Research Article
Pages 45-64
W. Kuipers
5-HT1A receptor coupling to G-proteins
Pages 65-66
W. Soudijn
Ligand binding assays Original Research Article
Pages 67-71
M.Th.M. Tulp, I. van Wijngaarden
5-HT1A behavioural models Original Research Article
Pages 73-79
J. Mos, B. Olivier
Therapeutic applications 5-HT1A receptor ligands Original Research Article
Pages 81-83
I. van Wijngaarden
5-HT1B receptor ligands Original Research Article
Pages 87-95
I. van Wijngaarden, W. Soudijn
5-HT1B Receptors
Pages 97-98
W. Kuipers
5-HT1D receptors Original Research Article
Pages 101-138
D.N. Middlemiss, M.S. Beer, V.G. Matassa
5-HT1E and 5-HT1F receptors Original Research Article
Pages 141-157
G. McAllister, J.L. Castro
5-HT2A, 5-HT2B and 5-HT2C receptor ligands Original Research Article
Pages 161-197
I. van Wijngaarden, W. Soudijn
The 5-HT2-type receptor family Original Research Article
Pages 199-214
E. Ronken, B. Olivier
5-HT2 receptor antagonists: (potential) therapeutics Original Research Article
Pages 215-217
W. Soudijn
5-HT3 receptors Original Research Article
Pages 221-258
H. Gozlan
5-HT4 receptors Original Research Article
Pages 261-308
A. Dumuis, H. Ansanay, C. Waeber, M. Sebben, L. Fagni, J. Bockaert
The 5-HT5, 5-HT6 and 5-HT7 receptors Original Research Article
Pages 311-323
R. Grailhe, U. Boschert, R. Hen
5-HT transporter Original Research Article
Pages 327-361
W. Soudijn, I. van Wijngaarden
Index
Pages 363-367
