2023
The Concise Guide to PHARMACOLOGY 2023/24: Ion channels
Alexander S, Mathie A, Peters J, Veale E, Striessnig J, Kelly E, Armstrong J, Faccenda E, Harding S, Davies J, Aldrich R, Attali B, Baggetta A, Becirovic E, Biel M, Bill R, Caceres A, Catterall W, Conner A, Davies P, De Clerq K, Delling M, Di Virgilio F, Falzoni S, Fenske S, Fortuny-Gomez A, Fountain S, George C, Goldstein S, Grimm C, Grissmer S, Ha K, Hammelmann V, Hanukoglu I, Hu M, Ijzerman A, Jabba S, Jarvis M, Jensen A, Jordt S, Kaczmarek L, Kellenberger S, Kennedy C, King B, Kitchen P, Liu Q, Lynch J, Meades J, Mehlfeld V, Nicke A, Offermanns S, Perez-Reyes E, Plant L, Rash L, Ren D, Salman M, Sieghart W, Sivilotti L, Smart T, Snutch T, Tian J, Trimmer J, Van den Eynde C, Vriens J, Wei A, Winn B, Wulff H, Xu H, Yang F, Fang W, Yue L, Zhang X, Zhu M. The Concise Guide to PHARMACOLOGY 2023/24: Ion channels. British Journal Of Pharmacology 2023, 180: s145-s222. PMID: 38123150, PMCID: PMC11339754, DOI: 10.1111/bph.16178.Peer-Reviewed Original ResearchConceptsBest available pharmacological toolsOpen access knowledgebase sourceOfficial IUPHAR classificationAvailable pharmacological toolsDrug targetsG protein-coupled receptorsIon channelsProtein-coupled receptorsNomenclature guidanceClinical pharmacologyMajor pharmacological targetCatalytic receptorsSelective pharmacologyNuclear hormone receptorsPharmacological targetsPharmacological toolsHormone receptorsPrevious GuidesReceptorsLandscape formatHuman drug targetsPharmacologyConcise guideBiennial publicationRelated targetsTransient Receptor Potential channels (TRP) in GtoPdb v.2023.2
Blair N, Caceres A, Carvacho I, Chaudhuri D, Clapham D, De Clerq K, Delling M, Doerner J, Fan L, Grimm C, Ha K, Hu M, Jabba S, Jordt S, Julius D, Kahle K, Liu B, Liu Q, McKemy D, Nilius B, Oancea E, Owsianik G, Riccio A, Sah R, Stotz S, Tian J, Tong D, Vriens J, Wu L, Xu H, Yang F, Yang W, Yue L, Zhu M. Transient Receptor Potential channels (TRP) in GtoPdb v.2023.2. IUPHAR/BPS Guide To Pharmacology CITE 2023, 2023 DOI: 10.2218/gtopdb/f78/2023.2.Peer-Reviewed Original ResearchTransient receptor potential channelsCongenital stationary night blindnessTRPC channelsAdenosine diphosphate riboseStore-operated channelsMost TRP channelsTRP channelsNMDA receptorsCation channelsIntracellular ATP levelsExtra-synaptic NMDA receptorsMetabotropic glutamate receptor 6Activation of GoHuman TRPM1 mutationsReabsorption of calciumTRPC4/C5Ion channelsExpression of S100A9Dendritic cell migrationBile duct diseaseIntracellular calcium storesActivity of TRPV1Layer 5 neuronsSynaptic NMDA receptorsMouse prefrontal cortexTransient Receptor Potential channels (TRP) in GtoPdb v.2023.1
Blair N, Carvacho I, Chaudhuri D, Clapham D, De Clerq K, Delling M, Doerner J, Fan L, Grimm C, Ha K, Hu M, Jordt S, Julius D, Kahle K, Liu B, Liu Q, McKemy D, Nilius B, Oancea E, Owsianik G, Riccio A, Sah R, Stotz S, Tian J, Tong D, Vriens J, Wu L, Xu H, Yang F, Yang W, Yue L, Zhu M. Transient Receptor Potential channels (TRP) in GtoPdb v.2023.1. IUPHAR/BPS Guide To Pharmacology CITE 2023, 2023 DOI: 10.2218/gtopdb/f78/2023.1.Peer-Reviewed Original ResearchTransient receptor potential channelsCongenital stationary night blindnessTRPC channelsAdenosine diphosphate riboseStore-operated channelsMost TRP channelsTRP channelsNMDA receptorsCation channelsIntracellular ATP levelsExtra-synaptic NMDA receptorsMetabotropic glutamate receptor 6Activation of GoHuman TRPM1 mutationsReabsorption of calciumTRPC4/C5Ion channelsExpression of S100A9Dendritic cell migrationBile duct diseaseIntracellular calcium storesActivity of TRPV1Layer 5 neuronsSynaptic NMDA receptorsMouse prefrontal cortex
2022
Transient Receptor Potential channels (TRP) in GtoPdb v.2022.1
Blair N, Carvacho I, Chaudhuri D, Clapham D, DeCaen P, Delling M, Doerner J, Fan L, Grimm C, Ha K, Jordt S, Julius D, Kahle K, Liu B, McKemy D, Nilius B, Oancea E, Owsianik G, Riccio A, Sah R, Stotz S, Tian J, Tong D, Van den Eynde C, Vriens J, Wu L, Xu H, Yue L, Zhang X, Zhu M. Transient Receptor Potential channels (TRP) in GtoPdb v.2022.1. IUPHAR/BPS Guide To Pharmacology CITE 2022, 2022 DOI: 10.2218/gtopdb/f78/2022.1.Peer-Reviewed Original ResearchTransient receptor potential channelsCongenital stationary night blindnessTRPC channelsStore-operated channelsMost TRP channelsTRP channelsCation channelsMetabotropic glutamate receptor 6Activation of GoHuman TRPM1 mutationsReabsorption of calciumTRPC4/C5Ion channelsDendritic cell migrationLow extracellular sodiumIntracellular calcium storesActivity of TRPV1Layer 5 neuronsMouse prefrontal cortexMucolipidosis type IVGlutamate receptor 6Store-operated mechanismsMain olfactory epitheliumBroad-spectrum agentsPancreatic beta cells
2021
Transient Receptor Potential channels (TRP) in GtoPdb v.2021.3
Blair N, Carvacho I, Chaudhuri D, Clapham D, DeCaen P, Delling M, Doerner J, Fan L, Ha K, Jordt S, Julius D, Kahle K, Liu B, McKemy D, Nilius B, Oancea E, Owsianik G, Riccio A, Sah R, Stotz S, Tian J, Tong D, Van den Eynde C, Vriens J, Wu L, Xu H, Yue L, Zhang X, Zhu M. Transient Receptor Potential channels (TRP) in GtoPdb v.2021.3. IUPHAR/BPS Guide To Pharmacology CITE 2021, 2021 DOI: 10.2218/gtopdb/f78/2021.3.Peer-Reviewed Original ResearchTransient receptor potential channelsCongenital stationary night blindnessTRPC channelsStore-operated channelsMost TRP channelsTRP channelsCation channelsMetabotropic glutamate receptor 6Activation of GoHuman TRPM1 mutationsReabsorption of calciumTRPC4/C5Ion channelsDendritic cell migrationLow extracellular sodiumIntracellular calcium storesActivity of TRPV1Layer 5 neuronsMouse prefrontal cortexMucolipidosis type IVGlutamate receptor 6Main olfactory epitheliumStore-operated mechanismsBroad-spectrum agentsPancreatic beta cells
2019
Transient Receptor Potential channels (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database
Blair N, Carvacho I, Chaudhuri D, Clapham D, DeCaen P, Delling M, Doerner J, Fan L, Ha K, Jordt S, Julius D, Kahle K, Liu B, McKemy D, Nilius B, Oancea E, Owsianik G, Riccio A, Sah R, Stotz S, Tian J, Tong D, Van den Eynde C, Vriens J, Wu L, Xu H, Yue L, Zhang X, Zhu M. Transient Receptor Potential channels (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database. IUPHAR/BPS Guide To Pharmacology CITE 2019, 2019 DOI: 10.2218/gtopdb/f78/2019.4.Peer-Reviewed Original ResearchCongenital stationary night blindnessTRPC channelsStore-operated channelsMost TRP channelsTRP channelsCation channelsMetabotropic glutamate receptor 6Activation of GoHuman TRPM1 mutationsReabsorption of calciumTRPC4/C5Ion channelsDendritic cell migrationIntracellular calcium storesLow extracellular sodiumLayer 5 neuronsTransient receptor potential channelsActivity of TRPV1Mouse prefrontal cortexMucolipidosis type IVGlutamate receptor 6Main olfactory epitheliumStore-operated mechanismsBroad-spectrum agentsPancreatic beta cells
2017
Ankyrin‐rich membrane spanning protein as a novel modulator of transient receptor potential vanilloid 1‐function in nociceptive neurons
Peter J, Kasper C, Kaufholz M, Buschow R, Isensee J, Hucho T, Herberg F, Schwede F, Stein C, Jordt S, Brackmann M, Spahn V. Ankyrin‐rich membrane spanning protein as a novel modulator of transient receptor potential vanilloid 1‐function in nociceptive neurons. European Journal Of Pain 2017, 21: 1072-1086. PMID: 28182310, PMCID: PMC5504413, DOI: 10.1002/ejp.1008.Peer-Reviewed Original ResearchConceptsAnkyrin-rich membranePKA-dependent mannerKinase DHEK-293 cellsSensitivity of TRPV1Immunoprecipitation experimentsDRG neuronsNovel modulatorRodent DRG neuronsIon channelsIon channel TRPV1Excitatory ion channelSmall-diameter dorsal root ganglion neuronsTransient receptor potential vanilloidImportant componentDorsal root ganglion neuronsPeripheral sensory neuronsMouse DRG neuronsChemical stimuliSensory neuronsCellsComplexesMembraneDirect modificationTRPV1 expression
2009
A sensory neuronal ion channel essential for airway inflammation and hyperreactivity in asthma
Caceres AI, Brackmann M, Elia MD, Bessac BF, del Camino D, D'Amours M, Witek JS, Fanger CM, Chong JA, Hayward NJ, Homer RJ, Cohn L, Huang X, Moran MM, Jordt SE. A sensory neuronal ion channel essential for airway inflammation and hyperreactivity in asthma. Proceedings Of The National Academy Of Sciences Of The United States Of America 2009, 106: 9099-9104. PMID: 19458046, PMCID: PMC2684498, DOI: 10.1073/pnas.0900591106.Peer-Reviewed Original ResearchConceptsAsthmatic airway inflammationAirway inflammationAirway hyperreactivityAllergen challengeHC-030031Airway allergen challengeEndogenous TRPA1 agonistsMurine ovalbumin modelImpaired inflammatory responseTreatment of asthmaRole of TRPA1Wild-type miceAirway epithelial functionAllergic inflammatory conditionsPromising pharmacological targetNeuronal ion channelsLipid peroxidation productsIon channelsAllergic asthmaAirway exposureEosinophil infiltrationLeukocyte infiltrationContractile stimuliInflammatory disordersOvalbumin modelTRPA1 Antagonists Block the Noxious Effects of Toxic Industrial Isocyanates and Tear Gases
Bessac B, Sivula M, von Hehn C, Caceres A, Escalera J, Jordt S. TRPA1 Antagonists Block the Noxious Effects of Toxic Industrial Isocyanates and Tear Gases. The FASEB Journal 2009, 23: 580.11-580.11. DOI: 10.1096/fasebj.23.1_supplement.580.11.Peer-Reviewed Original ResearchTransient receptor potential ankyrin 1Tear gas agentsSame neuronal receptorNoxious effectsTear gasesActivation of Ca2Adverse health effectsNocifensive behaviorAirway irritationCutaneous exposureTRPA1 antagonistSensory neuronsAnkyrin 1Neuronal receptorsPharmacological inhibitionGenetic ablationHealth effectsMembrane currentsFrequent exposureNoxious chemicalsExposureIon channelsSimilar responsesCa2Lacrimation
2008
Breathtaking TRP Channels: TRPA1 and TRPV1 in Airway Chemosensation and Reflex Control
Bessac BF, Jordt SE. Breathtaking TRP Channels: TRPA1 and TRPV1 in Airway Chemosensation and Reflex Control. Physiology 2008, 23: 360-370. PMID: 19074743, PMCID: PMC2735846, DOI: 10.1152/physiol.00026.2008.Peer-Reviewed Original ResearchConceptsReactive airways dysfunction syndromeAirway reflex responsesAirways dysfunction syndromeAirway inflammationChronic coughDysfunction syndromeTRP ion channelsReflex responsesReflex controlCapsaicin receptorChemical hypersensitivityTRPA1Reactive oxygen speciesInflammationTRPV1Noxious constituentsIon channelsOxygen speciesNew studiesCOPDCoughAsthmaSyndromeHypersensitivityIrritation
2007
The menthol receptor TRPM8 is the principal detector of environmental cold
Bautista DM, Siemens J, Glazer JM, Tsuruda PR, Basbaum AI, Stucky CL, Jordt SE, Julius D. The menthol receptor TRPM8 is the principal detector of environmental cold. Nature 2007, 448: 204-208. PMID: 17538622, DOI: 10.1038/nature05910.Peer-Reviewed Original ResearchConceptsMenthol receptor TRPM8TRPM8 knockout miceIntact nerve fibersDifferent ion channelsNerve fibersWhole animal testsKnockout miceNoxious coldCold stimuliCold sensationCold transducerInnocuous coolEnvironmental coldTRPM8MiceIon channelsAnimal testsCellular levelPhysiological importanceCold sensitivity
2006
TRPA1 Mediates the Inflammatory Actions of Environmental Irritants and Proalgesic Agents
Bautista DM, Jordt SE, Nikai T, Tsuruda PR, Read AJ, Poblete J, Yamoah EN, Basbaum AI, Julius D. TRPA1 Mediates the Inflammatory Actions of Environmental Irritants and Proalgesic Agents. Cell 2006, 124: 1269-1282. PMID: 16564016, DOI: 10.1016/j.cell.2006.02.023.Peer-Reviewed Original ResearchConceptsTRPA1-deficient miceInflammatory painEnvironmental irritantsInflammatory actionsProalgesic agentsPrimary afferent nociceptorsExcitatory ion channelPain hypersensitivityPungent irritantsAfferent nociceptorsNociceptor excitationAuditory functionThermal nociceptionNoxious coldMice exhibitChemotherapeutic agentsTRPA1PainIrritantsNociceptorsMiceSole targetMustard oilIon channelsInitial detection
2005
Pungent products from garlic activate the sensory ion channel TRPA1
Bautista DM, Movahed P, Hinman A, Axelsson HE, Sterner O, Högestätt ED, Julius D, Jordt SE, Zygmunt PM. Pungent products from garlic activate the sensory ion channel TRPA1. Proceedings Of The National Academy Of Sciences Of The United States Of America 2005, 102: 12248-12252. PMID: 16103371, PMCID: PMC1189336, DOI: 10.1073/pnas.0505356102.Peer-Reviewed Original ResearchConceptsSensory nerve endingsSensory neuronsNerve endingsTRPA1 channelsDiallyl disulfidePrimary sensory neuronsActivation of TRPA1Ion channel TRPA1Excitatory ion channelPain pathwaysPungent ingredientAllium familyVasorelaxant activityTRPA1Health benefitsNeuronsAllium extractsIon channelsAllicinMolecular mechanismsAllyl isothiocyanateEndingsPainVasodilationInflammation
2001
Bradykinin and nerve growth factor release the capsaicin receptor from PtdIns(4,5)P2-mediated inhibition
Chuang H, Prescott E, Kong H, Shields S, Jordt S, Basbaum A, Chao M, Julius D. Bradykinin and nerve growth factor release the capsaicin receptor from PtdIns(4,5)P2-mediated inhibition. Nature 2001, 411: 957-962. PMID: 11418861, DOI: 10.1038/35082088.Peer-Reviewed Original ResearchConceptsPlasma membrane phosphatidylinositolNerve growth factorTyrosine kinase receptorsActivation of PLCGrowth factorTRP channel familyMembrane phosphatidylinositolChannel familyKinase receptorsBiochemical mechanismsMolecular levelBiochemical studiesIon channelsCellular levelChannel activityHeat-activated ion channelExpression of VR1Sensory nerve endingsChemical stimuliSense of painSensory neuronsEndogenous factorsPrimary afferentsNerve endingsCapsaicin receptor