The Functional Roles of Histamine Receptors

463 Pages·2022·11.185 MB·English

by  Kazuhiko Yanai, Maria Beatrice Passani

Current Topics in Behavioral Neurosciences 59
Kazuhiko Yanai
Maria Beatrice Passani   Editors
The Functional
Roles
of Histamine
Receptors
Current Topics in Behavioral Neurosciences
Volume 59
SeriesEditors
Mark A. Geyer, Department of Psychiatry, University of California San Diego, La
Jolla,CA,USA
Charles A. Marsden, Queen’s Medical Centre, University of Nottingham, Notting-
ham,UK
Bart A. Ellenbroek, School of Psychology, Victoria University of Wellington,
Wellington,NewZealand
Thomas R. E. Barnes, The Centre for Mental Health, Imperial College London,
London,UK
SusanL.Andersen,HarvardMedicalSchool,McLeanHospital,Belmont,MA,USA
MartinP.Paulus,LaureateInstituteforBrainResearch,Tulsa,OK,USA
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hamMedicalSchoolQueen’sMedicalCentre,Nottingham,UK
ProfessorBartA.Ellenbroek
School of Psychology, Victoria University of Wellington, Wellington, New
Zealand
(cid:129)
Kazuhiko Yanai Maria Beatrice Passani
Editors
The Functional Roles
of Histamine Receptors
Editors
KazuhikoYanai MariaBeatricePassani
Departmentof Pharmacology DepartmentofHealthScience
TohokuUniversitySchoolofMedicine UniversityofFlorence
Sendai,Japan Firenze,Italy
ISSN1866-3370 ISSN1866-3389 (electronic)
CurrentTopicsinBehavioralNeurosciences
ISBN978-3-031-16996-0 ISBN978-3-031-16997-7 (eBook)
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Preface
Research in the field of histamine receptors over the past 100 years went hand-in-
hand with the development of modern pharmacology. Advances in histamine
research led by outstanding scientists were so incisive that the clinical approach to
treatallergiesandgastrointestinalailmentswasrevolutionized.Maybenootherfield
ofpharmacologywashonouredbyfourNobellaureates,namelyAdolfWindausfor
thechemicalsynthesisofhistamine,SirHenryH.Dalewhodescribedthephysiol-
ogyofhistamine,DanielBovetforhisdiscoveryofH receptorantagonistsandSir
1
James W. Black for his discovery of the H receptor and synthesis of selective
2
antagonists.
In the following decades, histamine pharmacology witnessed a rapid growth of
H and H receptor antagonists with an improved profile for the treatment of
1 2
conditions such as allergic rhinitis, conjunctivitis, urticaria and peptic ulcer. The
pharmacologicaltreatmentofpepticulcerandgastro-oesophagealrefluxwasindeed
arevolutionasitendedthesurgicalintervention.
Several of the older antihistamines are still marketed for skin applications or
desired for their sedative effects. It was indeed the sedative action of these com-
pounds that intrigued the scientists and lead them to suggest, as early as the 1970,
that histamine was present in the brain. Indeed, it was. Neuroanatomical and
classical pharmacological studies confirmed that histaminergic neurons form a
small cluster in the posterior hypothalamus and have extensive projections in the
brain.AnewreceptorintheCNSwasalsoidentifiedwithinthesameyears:theH
3
receptor. These findings ignited an explosion of interest on the function of brain
histamine,bothbytheacademiaandtheindustry.
Several selective ligands for the H receptor have been synthesised and have
3
helped elucidate the role of histamine in the healthy and diseased brain. Clinical
trials abounded in the early 2000 exploiting H receptor antagonists for their
3
procognitiveeffectsinAlzheimer’s,Parkinson’s,ADHDpatients.Theclinicaltrials
failed though,whichdecreed thedownfallofH receptorpharmacology. Onlyone
3
v
vi Preface
H receptor antagonist for the treatment of narcolepsy was approved by the Euro-
3
peanMedicineAgencyin2016andFDAin2019andreachedbothmarkets.
Interest in histamine pharmacology was in the meantime resurrected by the
discovery of another histamine receptor, number 4, using genomics-based reverse
pharmacological approaches for screening orphan GPCRs. This receptor is prefer-
entiallyexpressedbyimmunecellsanditsdiscoveryraisedhopesforitstranslational
exploitation as a new therapeutic target for unmet medical needs ranging from
asthma to cancer. However, several drawbacks emerged and dramatically slowed
downresearchinthefield.
Allalongthehistoryofhistaminepharmacology,clinicalandpreclinicalstudies
progressed hand-in-hand. Despite the raises and falls, histamine research is all but
dead.Forinstance,abetterunderstandingofreceptorintra-andinterspecieshetero-
geneity will certainly improve and accelerate the translation of experimental data
into clinical practice. Also, the plethora of data on brain histamine is hinting at a
fundamentalroleofthissystemasahubthatreceivesinternalandperipheralstimuli
to allocate thenecessary excitation tospecific brain circuits that preside theappro-
priatebehaviouralresponses.
The development of new histaminergic ligands is an on-going process that
constantlyprovidesnewpreclinicaltools(e.g.photoswitchablecompoundstomod-
ulate histamine function with calibrated wavelengths) to elucidate the functional
complexityofhistaminenetworksinhuman(patho)physiology.
In our book, we will try to cover the salient aspects of histamine receptors
function and pharmacology IN THE CENTRAL NERVOUS SYSTEM, hopefully
givingafullaccountofthepreclinicalandclinicalprogressinthelastdecadesand
theexcitingperspectiveforthefuture.Wewilltrytocovertheclinicalareasthatare
in major need of new therapeutic approaches and that may take advantage of new
histaminergiccompoundsforapersonalisedmedicine.
Sendai,Japan KazuhikoYanai
Firenze,Italy MariaBeatricePassani
Contents
PartI PharmacologyandMedicinalChemistry
NewChemicalBiologyToolsfortheHistamineReceptorFamily. . . . . . 3
YangZheng,GáborWágner,NielsHauwert,XiaoyuanMa,
HenryF.Vischer,andRobLeurs
ChemicalProbesforHistamineReceptorSubtypes. . . . . . . . . . . . . . . . 29
MarkusFalkenstein,MilicaElek,andHolgerStark
Patho-PharmacologicalResearchofAnti-allergicNatural
ProductsTargetingAntihistamine-Sensitiveand-Insensitive
AllergicMechanisms. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 77
HiroyukiFukui,HiroyukiMizuguchi,YoshiakiKitamura,
andNoriakiTakeda
MolecularSignalingandTranscriptionalRegulationofHistamineH
1
ReceptorGene. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 91
HiroyukiMizuguchi,YoshiakiKitamura,NoriakiTakeda,
andHiroyukiFukui
PartII ClinicalPharmacology
HistamineNeuroimaginginStress-RelatedDisorders. . . . . . . . . . . . . . . 113
ShinFukudo,MichikoKano,YasuhiroSato,TomohikoMuratsubaki,
MotoyoriKanazawa,ManabuTashiro,andKazuhikoYanai
Histamine-4Receptor:EmergingTargetfortheTreatment
ofNeurologicalDiseases. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 131
LingShan,GerardJ.M.Martens,andDickF.Swaab
ImagingHistamineH3ReceptorswithPositronEmission
Tomography. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 147
PabloMartínRusjanandBernardLeFoll
vii
viii Contents
TherapeuticPotentialofHistamineH3ReceptorsinSubstanceUse
Disorders. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 169
PatriciaDiCiano,ChristianS.Hendershot,andBernardLeFoll
EfficacyandSafetyofNon-brainPenetratingH -Antihistamines
1
fortheTreatmentofAllergicDiseases. . . . . . . . . . . . . . . . . . . . . . . . . . 193
KazuhikoYanai,TakeoYoshikawa,andMartinK.Church
PartIII TheImmuneandInflammatoryResponseintheBrain
TheHistamineandMultipleSclerosisAlliance:PleiotropicActions
andFunctionalValidation. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 217
CinziaVolonté,SavinaApolloni,andSusannaAmadio
HistamineandMicroglia. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 241
TomomitsuIida,KazuhikoYanai,andTakeoYoshikawa
HistamineintheCrosstalkBetweenInnateImmuneCellsand
Neurons:RelevanceforBrainHomeostasisandDisease. . . . . . . . . . . . . 261
LilianaBernardino
PartIV Neuropharmacology:HistamineandBehaviour
TheHistamineSysteminZebrafishBrain:Organization,Receptors,
andBehavioralRoles. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 291
PerttiPanula,Yu-ChiaChen,DiegoBaronio,SerenaLewis,
andMariaSundvik
DifferentPeasintheSamePod:TheHistaminergicNeuronal
Heterogeneity. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 303
GustavoProvensi,M.BeatricePassani,andPatrizioBlandina
Histamine:AKeyNeuromodulatorofMemoryConsolidation
andRetrieval. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 329
HiroshiNomura,RintaroShimizume,andYujiIkegaya
TargetingHistamineandHistamineReceptorsforthePrecise
RegulationofFeeding. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 355
YanrongZhengandZhongChen
ADuetBetweenHistamineandOleoylethanolamideintheControl
ofHomeostaticandCognitiveProcesses. . . . . . . . . . . . . . . . . . . . . . . . . 389
GustavoProvensi,AlessiaCosta,BarbaraRani,PatrizioBlandina,
andM.BeatricePassani
Contents ix
PartV Neuropharmacology:HistamineandSleep
HistamineasanAlertSignalintheBrain. . . . . . . . . . . . . . . . . . . . . . . . 413
TakatoshiMochizuki
BrainMastCellsinSleepandBehavioralRegulation. . . . . . . . . . . . . . . 427
SeijiNishino,NoriakiSakai,NaoyaNishino,andTaisukeOno
TheRoleoftheCentralHistaminergicSysteminBehavioralState
Control. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 447
EldaArrigoniandPatrickM.Fuller