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G Protein-Coupled Receptors www.brjpharmacol.org Volume 164, Supplement 1, November 2011 S1 INTRODUCTION S85 Neuropeptide Y S1 Guide to Receptors and Channels (GRAC), 5th edition S86 Neuropeptides B and W S3 Consultants S87 Neurotensin S88 Opioid and opioid-like S5 G PROTEIN-COUPLED RECEPTORS S90 Orexin S5 Introduction S91 P2Y S8 Orphan G protein-coupled receptors S93 Parathyroid hormone and parathyroid hormone- S16 5-HT (5-Hydroxytryptamine) related peptide S20 Acetylcholine (muscarinic) S94 Platelet-activating factor S22 Adenosine S95 Proteinase-activated S24 α Adrenoceptors, 1 S97 Prostanoid S25 α Adrenoceptors, 2 S100 Prokineticin S26 β Adrenoceptors, S101 Relaxin family peptide S28 Anaphylatoxin S103 Somatostatin S29 Angiotensin S105 Sphingosine 1-phosphate S30 Apelin S107 Tachykinin S31 Bile acid S108 Trace amine-associated S32 Bombesin S109 TRH S33 Bradykinin S110 Urotensin-II S34 Calcitonin, amylin, CGRP and adrenomedullin S111 Vasopressin & oxytocin S36 Calcium-sensing S113 VIP & PACAP S37 Cannabinoid S39 Chemokine S115 LIGAND-GATED ION CHANNELS S42 Cholecystokinin S115 Introduction S43 Corticotropin-releasing factor S116 5-HT3 (5-Hydroxytryptamine3) S44 Dopamine S118 Acetylcholine (nicotinic) S46 Endothelin S122 GABAA (γ-aminobutyric acid) S48 Formylpeptide S126 Glutamate (ionotropic) S49 Free fatty acid S130 Glycine S51 Frizzled S133 P2X S53 GABAB S135 ZAC (Zinc-activated channel) S55 Galanin S137 S57 Ghrelin ION CHANNELS S137 S59 Glucagon, glucagon-like peptide and secretin Introduction S138 S61 Glutamate, metabotropic Acid-sensing (proton-gated) ion channels (ASICs) S141 S65 Glycoprotein hormone Aquaporins S142 S66 Gonadotropin-releasing hormone (GnRH) Calcium (voltage-gated) S144 S68 G protein-coupled estrogen (GPER) CatSper channels S146 S69 GPR18, GPR55 and GPR119 Chloride channels S152 S70 Histamine Connexins and pannexins S153 S71 Hydroxycarboxylic acid family Cyclic nucleotide-gated channels S154 S72 KISS1, neuropeptide FF, prolactin-releasing peptide Epithelial sodium channels (ENaC) S156 and QRFP Hyperpolarisation-activated, cyclic nucleotide-gated S74 Leukotriene, lipoxin, oxoeicosanoid and resolvin (HCN) S157 S76 Lysophosphatidic acid IP3 receptor S158 S78 Melanin-concentrating hormone Potassium S161 S79 Melanocortin Voltage-gated proton channel S162 S80 Melatonin Ryanodine receptor S163 S82 Motilin Sodium leak channel, non-selective S164 S83 Neuromedin U Sodium (voltage-gated) S166 S84 Neuropeptide S Transient receptor potential (TRP) cation channels Contents continued . 1103-104_bph_v164_is1_toc.indd03-104_bph_v164_is1_toc.indd iiiiii 110/25/20110/25/2011 44:57:21:57:21 PPMM Contents continued S175 NUCLEAR RECEPTORS S252 SLC22 family of organic cation and anion S175 Introduction transporters S176 Orphan nuclear receptors S254 SLC23 family of ascorbic acid transporters S179 Liver X and farnesoid X S255 SLC24 family of sodium/potassium/calcium S181 Peroxisome proliferator-activated exchangers S183 Retinoic acid, retinoid X and retinoic acid-related S256 SLC25 family of mitochondrial transporters orphan S259 SLC26 family of anion exchangers S185 Steroid hormone S260 SLC27 family of fatty acid transporters S187 Thyroid hormone S261 SLC28 and SLC29 families of nucleoside transporters S188 Vitamin D, Pregnane X and Constitutive Androstane S263 SLC30 zinc transporter family S263 SLC31 family of copper transporters S189 CATALYTIC RECEPTORS S264 SLC32 vesicular inhibitory amino acid transporter S189 Introduction S264 SLC33 acetylCoA transporter S190 Cytokine receptor family S265 SLC34 family of sodium phosphate co-transporters S194 GDNF family S266 SLC35 family of nucleotide sugar transporters S195 Natriuretic peptide S267 SLC36 family of proton-coupled amino acid S197 Pattern recognition receptors transporters S200 Receptor serine/threonine kinase (RSTK) family S268 SLC37 family of phosphosugar/phosphate (EC 2.7.11.30) exchangers S203 Receptor tyrosine kinases (E.C. 2.7.1.112) S269 SLC38 family of sodium-dependent neutral amino S210 Receptor tyrosine phosphatases (RTP, EC 3.1.3.48) acid transporters S211 Tumour necrosis factor (TNF) family S270 SLC39 family of metal ion transporters S213 TRANSPORTERS S271 SLC40 iron transporter S213 Introduction S272 SLC41 family of divalent cation transporters S214 ATP-binding cassette family S272 SLC42 family of non-erythroid Rhesus glycoprotein S218 F-type and V-type ATPases (EC 3.6.3.14) ammonium transporters S220 P-type ATPases (EC 3.6.3.-) S273 SLC43 family of large neutral amino acid S223 The SLC superfamily of solute carriers transporters S223 SLC1 family of amino acid transporters S273 SLC44 family of choline transporters S226 SLC2 family of hexose and sugar alcohol transporters S274 SLC45 orphans S228 SLC3 and SLC7 families of heteromeric amino acid S275 SLC46 family of folate transporters transporters (HATs) S275 SLC47 family of multidrug and toxin extrusion S229 SLC4 family of bicarbonate transporters transporters S230 SLC5 family of sodium-dependent transporters S276 SLC48 haem transporter S234 SLC6 neurotransmitter transporter family S276 SLCO family of organic anion transporting S239 SLC8 family of sodium/calcium exchangers polypeptides S239 SLC9 family of sodium/hydrogen exchangers S279 ENZYMES S240 SLC10 family of sodium-bile acid co-transporters S279 Introduction S242 SLC11 family of proton-coupled metal ion S280 Adenosine turnover transporters S282 Amino acid hydroxylases (E.C.1.14.16.-) S242 SLC12 family of cation-coupled chloride transporters S283 L-Arginine turnover S243 SLC13 family of sodium-dependent sulphate/ S286 Carboxylases and decarboxylases carboxylate transporters S288 Cyclic nucleotide turnover S244 SLC14 family of facilitative urea transporters S292 Cytochrome P450 (E.C. 1.14.-.-) S245 SLC15 family of peptide transporters S296 Eicosanoid turnover S246 SLC16 family of monocarboxylate transporters S300 Endocannabinoid turnover S247 SLC17 phosphate and organic anion transporter S302 Glycerophospholipid turnover family S306 Haem oxygenase (EC 1.14.99.3) S249 SLC18 family of vesicular amine transporters S307 Hydrogen sulphide synthesis S251 SLC19 family of vitamin transporters S308 Inositol phosphate turnover S251 SLC20 family of sodium-dependent phosphate S310 Protein serine/threonine kinases (E.C. 2.7.1.-) transporters S317 Protein turnover 1103-104_bph_v164_is1_toc.indd03-104_bph_v164_is1_toc.indd iivv 110/25/20110/25/2011 44:57:21:57:21 PPMM Alexander SPH, Mathie A, Peters JA Guide to Receptors and Channels (GRAC), 5th edition S1 Guide to Receptors and Channels (GRAC), 5th editionbph_1649 1..2 Abstract The Fifth Edition of the ‘Guide to Receptors and Channels’ is a compilation of the major pharmacological targets divided into seven sections: G protein-coupled receptors, ligand-gated ion channels, ion channels, catalytic receptors, nuclear receptors, transporters and enzymes. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside suggestions for further reading. Available alongside this publication is a portal at http://www.GuideToPharmacology.org which is produced in close association with NC-IUPHAR and allows free online access to the information presented in the Fifth Edition. Introduction The great proliferation of drug targets in recent years has driven the need to provide a logically-organised synopsis of the nomenclature and pharmacology of these targets. This is the underlying reason for this ‘Guide to Receptors and Channels’, distributed with the British Journal of Pharmacology, and produced in association with NC-IUPHAR, the Nomenclature Committees of the International Union of Basic and Clinical Pharmacology. Thanks to a closer collaboration between the British Pharmacological Society and NC-IUPHAR, a free online portal containing the information presented in the Guide to Receptors and Channels has been established at http://www.GuideToPharmacology.org. The new portal gathers in one place the previously separate information on drug targets of GRAC and IUPHAR-DB, the database produced by NC-IUPHAR. Over time, these will steadily be integrated and the portal will be developed as a one-stop-shop for information on drug targets and other information of assistance to pharmacology and drug development in both academia and industry. The free online portal has been created by the IUPHAR Database Team (Joanna Sharman, Chido Mpamhanga, Adam Pawson, Helen Benson, Vincent Bombail and Tony Harmar) in the Centre for Cardiovascular Science, University of Edinburgh. Our intent is to produce an authoritative but user-friendly publication, which allows a rapid overview of the key properties of a wide range of established or potential pharmacological targets. The aim is to provide information succinctly, so that a newcomer to a particular target group can identify the main elements ‘at a glance’. It is not our goal to produce all-inclusive reviews of the targets presented; references to these are included in the Further Reading sections of the entries or, for many targets, the website of NC-IUPHAR (http://www.iuphar-db.org) provides extensive information. The ‘Guide to Receptors and Channels’ presents each entry, typically a circumscribed target class family on, wherever possible, a single page, so as to allow easy access and rapid oversight. Targets have been selected for inclusion where there is sufficient pharmacological information to allow clear definition or where, in our view, there is clear interest in this molecular class from the pharmacological community. Our philosophy has been to present data
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