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      The Concise Guide to Pharmacology 2013/14: Ligand-Gated Ion Channels

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          Abstract

          The Concise Guide to PHARMACOLOGY 2013/14 provides concise overviews of the key properties of over 2000 human drug targets with their pharmacology, plus links to an open access knowledgebase of drug targets and their ligands ( www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. The full contents can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.12444/full.

          Ligand-gated ion channels are one of the seven major pharmacological targets into which the Guide is divided, with the others being G protein-coupled receptors, ion channels, catalytic receptors, nuclear hormone receptors, transporters and enzymes. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. A new landscape format has easy to use tables comparing related targets.

          It is a condensed version of material contemporary to late 2013, which is presented in greater detail and constantly updated on the website www.guidetopharmacology.org, superseding data presented in previous Guides to Receptors and Channels. It is produced in conjunction with NC-IUPHAR and provides the official IUPHAR classification and nomenclature for human drug targets, where appropriate. It consolidates information previously curated and displayed separately in IUPHAR-DB and the Guide to Receptors and Channels, providing a permanent, citable, point-in-time record that will survive database updates.

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          Most cited references292

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          Mammalian nicotinic acetylcholine receptors: from structure to function.

          The classical studies of nicotine by Langley at the turn of the 20th century introduced the concept of a "receptive substance," from which the idea of a "receptor" came to light. Subsequent studies aided by the Torpedo electric organ, a rich source of muscle-type nicotinic receptors (nAChRs), and the discovery of alpha-bungarotoxin, a snake toxin that binds pseudo-irreversibly to the muscle nAChR, resulted in the muscle nAChR being the best characterized ligand-gated ion channel hitherto. With the advancement of functional and genetic studies in the late 1980s, the existence of nAChRs in the mammalian brain was confirmed and the realization that the numerous nAChR subtypes contribute to the psychoactive properties of nicotine and other drugs of abuse and to the neuropathology of various diseases, including Alzheimer's, Parkinson's, and schizophrenia, has since emerged. This review provides a comprehensive overview of these findings and the more recent revelations of the impact that the rich diversity in function and expression of this receptor family has on neuronal and nonneuronal cells throughout the body. Despite these numerous developments, our understanding of the contributions of specific neuronal nAChR subtypes to the many facets of physiology throughout the body remains in its infancy.
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            The glutamate receptor ion channels.

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              GABA A receptors: subtypes provide diversity of function and pharmacology.

              This mini-review attempts to update experimental evidence on the existence of GABA(A) receptor pharmacological subtypes and to produce a list of those native receptors that exist. GABA(A) receptors are chloride channels that mediate inhibitory neurotransmission. They are members of the Cys-loop pentameric ligand-gated ion channel (LGIC) superfamily and share structural and functional homology with other members of that family. They are assembled from a family of 19 homologous subunit gene products and form numerous receptor subtypes with properties that depend upon subunit composition, mostly hetero-oligomeric. These vary in their regulation and developmental expression, and importantly, in brain regional, cellular, and subcellular localization, and thus their role in brain circuits and behaviors. We propose several criteria for including a receptor hetero-oligomeric subtype candidate on a list of native subtypes, and a working GABA(A) receptor list. These criteria can be applied to all the members of the LGIC superfamily. The list is divided into three categories of native receptor subtypes: "Identified", "Existence with High Probability", and "Tentative", and currently includes 26 members, but will undoubtedly grow, with future information. This list was first presented by Olsen & Sieghart (in press).
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                Author and article information

                Journal
                Br J Pharmacol
                Br. J. Pharmacol
                bph
                British Journal of Pharmacology
                John Wiley & Sons, Ltd (Chichester, UK )
                0007-1188
                1476-5381
                December 2013
                17 December 2013
                : 170
                : 8
                : 1582-1606
                Affiliations
                [1 ]School of Life Sciences, University of Nottingham Medical School Nottingham, NG7 2UH, UK
                [2 ]The University/BHF Centre for Cardiovascular Science, University of Edinburgh Edinburgh, EH16 4TJ, UK
                [3 ]Spedding Research Solutions SARL Le Vésinet, 78110, France
                [4 ]Neuroscience Division, Medical Education Institute, Ninewells Hospital and Medical School, University of Dundee Dundee, DD1 9SY, UK
                Author notes
                Article
                10.1111/bph.12446
                3892288
                24528238
                ff37a6c9-c686-485a-81da-0937b25dd16d
                Copyright © 2013 The British Pharmacological Society
                History
                Categories
                Article
                The Concise Guide to Pharmacology 2013/14.
                This issue was published by Wiley with financial contributions from the British Pharmacological Society, the International Union of Basic and Clinical Pharmacology, the Wellcome Trust (099156/Z/12/Z]), which supports the website, and the University of Edinburgh, who host the guidetopharmacology.org website

                Pharmacology & Pharmaceutical medicine
                Pharmacology & Pharmaceutical medicine

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