Abstract

The Concise Guide to PHARMACOLOGY 2021/22 is the fifth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of nearly 1900 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide constitutes over 500 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/bph.15539. Ion channels are one of the six major pharmacological targets into which the Guide is divided, with the others being: G protein-coupled receptors, nuclear hormone receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2021, and supersedes data presented in the 2019/20, 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the Nomenclature and Standards Committee of the International Union of Basic and Clinical Pharmacology (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.

Highlights

  • Background currentKCNK2, O95069KCNK3, O14649 arachidonic acid [824]GI-530159 [640], BL-1249 halothane [579](pEC50 5.3) [865], chloroform Concentration range: 8×10−3M [823], halothane [823], isoflurane [823]norfluoxetine [513]

  • The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2021, and supersedes data presented in the 2019/20, 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the Nomenclature and Standards Committee of the International Union of Basic and Clinical Pharmacology (NC-IUPHAR), providing official IUPHAR classification and nomenclature for human drug targets, where appropriate

  • Expressed heteromultimers form ion channels with differences in kinetics, ion selectivity, pHsensitivity and sensitivity to blockers that resemble some of the native proton activated currents recorded from neurones [43, 61, 292, 620]

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Summary

Conflict of interest

The authors state that there are no conflicts of interest to disclose. Overview: Ion channels are pore-forming proteins that allow the flow of ions across membranes, either plasma membranes, or the membranes of intracellular organelles [407]. 5-Hydroxytryptamine (serotonin) receptors [430]) is a ligand-gated ion channel of the Cys-loop family that includes the zinc-activated channels, nicotinic acetylcholine, GABAA and strychnine-sensitive glycine receptors. Expressed heteromultimers form ion channels with differences in kinetics, ion selectivity, pHsensitivity and sensitivity to blockers that resemble some of the native proton activated currents recorded from neurones [43, 61, 292, 620]. Overview: The GABAA receptor is a ligand-gated ion channel of the Cys-loop family that includes the nicotinic acetylcholine, 5-HT3 and strychnine-sensitive glycine receptors. Several high-resolution cryo-electron microscopy structures have been described in which the full-length human α1β3γ2L GABAA receptor in lipid nanodiscs is bound to the channel-blocker picrotoxin, the competitive antagonist bicuculline, the agonist GABA (γ-aminobutyric acid), and the classical benzodiazepines alprazolam and diazepam [687].

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