Serotonin Receptors And Their Ligands
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Author | : B. Olivier |
Publisher | : Elsevier |
Total Pages | : 379 |
Release | : 1997-07-10 |
Genre | : Science |
ISBN | : 0080541119 |
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 | : Stephen J. Peroutka |
Publisher | : Wiley-Liss |
Total Pages | : 256 |
Release | : 1991 |
Genre | : Medical |
ISBN | : |
This authoritative work explores the complex biochemical interactions of serotonin and related serotonergic agents with their receptors. It covers the molecular pharmacology of serotonin receptor subclasses, relating serotonin's influence on behavior, neuropsychiatric disease, and electrophysiology to characterizations at the molecular level.
Author | : Elaine Sanders-Bush |
Publisher | : Springer Science & Business Media |
Total Pages | : 394 |
Release | : 2012-12-06 |
Genre | : Medical |
ISBN | : 1461245605 |
Serotonin (5-HT) was isolated and chemically characterized nearly four decades ago, and is now generally accepted to function as a neurotransmitter and neuromodulatory agent. Early research focused on the measurement of concentrations, synthesis, and metabolism of 5-HT, and only recently has the focus shifted to characterization of 5-HT receptors. Gaddum and Picarelli first sug gested in 1957 that the effect of 5-HT in the guinea pig ileum is mediated by two pharmacologically distinguishable receptors; however, the possibility of dual5-HT receptors was not explored systematically or successfully until the past decade. It is now clear that more, perhaps many more, subclasses of 5-HT receptors exist. The purpose of this book is to provide an up-to-date report on 5-HT receptors. This is a difficult task considering the astonishing speed at which research in this field is expanding. As the first of what we can expect to be a steady stream of monographs focusing on 5-HT receptors, the book confirms that we are in an exciting time in the history of 5-HT. For those of us who have been work ing on 5-HT for many years, our dream of equal progress and recognition with the more extensively studied catecholamines is finally being realized. We now have a Serotonin Club that held its first international scientific meeting in 1987, and several more international meetings are in the planning stages.
Author | : John R. Fozard |
Publisher | : Birkhauser |
Total Pages | : 536 |
Release | : 1991 |
Genre | : Medical |
ISBN | : |
Author | : Bryan L. Roth |
Publisher | : Springer Science & Business Media |
Total Pages | : 628 |
Release | : 2008-08-17 |
Genre | : Medical |
ISBN | : 1597450804 |
A comprehensive, state-of-the-art review of our current understanding of the molecular and structural biology of 5-HT receptors and their potential use for drug discovery. The authors describe the anatomical, cellular, and subcellular distribution of 5-HT receptors and demonstrate a powerful approach to elucidating their physiological role using knockout mice in which the 5-HT receptors were deleted. They also review our understanding of the physiological role(s) of 5-HT receptors based mainly on studies performed in genetically engineered mice. Highlights include discussions of the behavioral phenotypes of 5-HT receptor knockout animals, the molecular biology and pharmacology of 5-HT receptors, and insights into the complexity of 5-HT receptor signal transduction.
Author | : G. A. Kennett |
Publisher | : |
Total Pages | : 12 |
Release | : 1997* |
Genre | : Pharmacology |
ISBN | : |
Author | : Leda Ivanova Manasieva |
Publisher | : |
Total Pages | : |
Release | : 2010 |
Genre | : |
ISBN | : |
Author | : Amitabha Chattopadhyay |
Publisher | : CRC Press |
Total Pages | : 230 |
Release | : 2007-05-17 |
Genre | : Medical |
ISBN | : 1420005758 |
A number of developments spanning a multitude of techniques makes this an exciting time for research in serotonin receptors. A comprehensive review of the subject from a multidisciplinary perspective, Serotonin Receptors in Neurobiology is among the first books to include information on serotonin receptor knockout studies. With contributions from l
Author | : Jessica Nicole Worsham |
Publisher | : |
Total Pages | : |
Release | : 2008 |
Genre | : |
ISBN | : |
Drug abuse and addiction are considered to be a result, at least in part, of the rewarding effects produced by increasing dopamine levels. 5-HT3 serotonin receptors have been shown to indirectly affect dopamine levels. Therefore, the effect of the 5-HT3 receptor partial agonist, MD-354, on the actions of psychomotor stimulants was analyzed in mouse locomotor activity assays to determine whether MD-354 is working through a 5-HT3 receptor agonist or antagonist mode of action. Studies with (+)amphetamine and (+)methamphetamine in combination with MD-354 indicated MD-354 is either devoid of action or is behaving similar to the 5-HT3 receptor antagonist, ondansetron. This effect could be occurring centrally; however peripheral effects can not be discounted. In combination with cocaine, MD-354 behaved similar to the 5-HT3 receptor agonist, SR 57227A, known to act both centrally and peripherally. This difference between central and peripheral effects could account for the different modes of action observed with MD-354. Studies also involved synthesis of potentially brain-penetrant carbamate analogs of MD-354, and QSAR to assist in validating a 5-HT3 receptor agonist pharmacophore.
Author | : Umamaheswar Siripurapu |
Publisher | : |
Total Pages | : 250 |
Release | : 2008 |
Genre | : |
ISBN | : |