The Concise Guide to PHARMACOLOGY 2015/16 provides concise overviews of the key properties of over 1750 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.13349/full. Voltage-gated ion channels are one of the eight major pharmacological targets into which the Guide is divided, with the others being: G protein-coupled receptors, ligand-gated ion channels, other ion channels, 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 Concise Guide is published in landscape format in order to facilitate comparison of related targets. It is a condensed version of material contemporary to late 2015, which is presented in greater detail and constantly updated on the website www.guidetopharmacology.org, superseding data presented in the previous Guides to Receptors & Channels and the Concise Guide to PHARMACOLOGY 2013/14. 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 GRAC and provides a permanent, citable, point-in-time record that will survive database updates.
Conflict of interestThe authors state that there are no conflicts of interest to declare. This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
Family structure
5905CatSper and Two-Pore channels 5907Cyclic nucleotide-regulated channels 5909Potassium channels 5910Calcium-activated potassium channels Functional Characteristics Organelle voltage-gated Na -selective channel (Na K Ca 2 ); Required for the generation of action potential-like long depolarization in lysosomes. Voltage-dependence of activation is sensitive to luminal pH (determined from lysosomal recordings). 1 2 @ pH4.6 = +91 mV; 1 2 @ pH6.5 = +2.6 mV. Maximum activity requires PI(3,5)P 2 and reduced [ATP] Organelle voltage-independent Na -selective channel (Na K Ca 2 ). Sensitive to the levels of PI(3,5)P 2 . Activated by decreases in [ATP] [59,218, 299]. Moreover, targeted disruption of Catsper1, 2, 3, 4, or AE genes results in an identical phenotype in which spermatozoa fail to exhibit the hyperactive movement (whip-like flagellar beats) necessary for penetration of the egg cumulus and zona pellucida and subsequent fertilization. Such disruptions are associated with a deficit in alkalinization and depolarization-evoked Ca 2 entry into spermatozoa [47,59, 299]. Thus, it is likely that the CatSper pore is forme...