Advanced search
Publication Cover
Expert Opinion on Investigational Drugs Volume 18, 2009 - Issue 10
Submit an article Journal homepage
1,008
Views
113
CrossRef citations to date
0
Altmetric
Reviews

Histamine H3 and H4 receptors as novel drug targets

Ekaterini Tiligada University of Athens, Medical School, Department of Pharmacology, M Asias 75, 11527 Athens, Greece +30 2107462575; +30 2107462554; [email protected]
, PhD,
Evangelia Zampeli University of Athens, Medical School, Department of Pharmacology, M Asias 75, 11527 Athens, Greece +30 2107462575; +30 2107462554; [email protected]
, MD,
Kerstin Sander Johann Wolfgang Goethe-University, Institute of Pharmaceutical Chemistry, Biozentrum, ZAFES/LiFF/CMP, Frankfurt/Main, Germany
, BPharm &
Holger Stark Johann Wolfgang Goethe-University, Institute of Pharmaceutical Chemistry, Biozentrum, ZAFES/LiFF/CMP, Frankfurt/Main, Germany
, PhD
Pages 1519-1531 | Published online: 17 Sep 2009

Bibliography

  • Lim HD, van Rijn RM, Ling P, et al. Evaluation of histamine H1-, H2-, and H3- receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther 2005;314:1310-21
  • Pollard H, Moreau J, Arrang JM, Schwartz JC. A detailed autoradiographic mapping of histamine H3 receptors in rat brain areas. Neuroscience 1993;52:169-89
  • Bertaccini G, Coruzzi G, Adami M, et al. Histamine H3 receptors: an overview. Ital J Gastroenterol 1991;23:378-85
  • Arrang JM, Garbarg M, Schwartz JC. Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. Nature 1983;302:832-7
  • Arrang JM, Morisset S, Gbahou F. Constitutive activity of the histamine H3 receptor. Trends Pharmacol Sci 2007;28:350-7
  • Sander K, Kottke T, Stark H. Histamine H3 receptor antagonists go to clinics. Biol Pharm Bull 2008;31:2163-81
  • Celanire S, Lebon F, Stark H. Drug discovery: from hits to clinical candidates. In: Vohora DS, editor, The third histamine receptor: selective ligands as potential therapeutic agents in CNS disorders.: Taylor & Francis CRC Press, Inc., Boca Raton, FL, USA 2008
  • Ligneau X, Morisset S, Tardivel-Lacombe J, et al. Distinct pharmacology of rat and human histamine H3 receptors: role of two amino acids in the third transmembrane domain. Br J Pharmacol 2000;131:1247-50
  • Strakhova MI, Fox GB, Carr TL, et al. Cloning and characterization of the monkey histamine H3 receptor isoforms. Eur J Pharmacol 2008;601:8-15
  • Bakker RA. Histamine H3 receptor isoforms. Inflamm Res 2004;53:509-16
  • Fernandez-Novoa L, Cacabelos R. Histamine function in brain disorders. Behav Brain Res 2001;124:213-33
  • Alvarez EO. The role of histamine on cognition. Behav Brain Res 2009;199:183-9
  • Munari L, Passani MB, Benetti F, et al. ABT-239, an H3 receptor antagonist, reveals heterogeneity among histaminergic neurons. XXXVIIIth Meeting of the European Histamine Research Society. Fulda, Germany 13 – 16 May 2009 O3
  • Blandina P, Efoudebe M, Cenni G, et al. Acetylcholine, histamine, and cognition: two sides of the same coin. Learn Mem 2004;11:1-8
  • Passani MB, Blandina P. The neuronal histaminergic system in cognition. Curr Med Chem Cent Nerv Syst Agents 2004;4:17-26
  • Bacciottini L, Passani MB, Mannaioni PF, Blandina P. Interactions between histaminergic and cholinergic systems in learning and memory. Behav Brain Res 2001;124:183-94
  • Fox GB, Esbenshade TA, Pan JB, et al. Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist. J Pharmacol Exp Ther 2005;313:176-90
  • Bonaventure P, Letavic M, Dugovic C, et al. Histamine H3 receptor antagonists: from target identification to drug leads. Biochem Pharmacol 2007;73:1084-96
  • GSK-pipeline. 2009. Available from: http://www.gsk.com/investors/ product_pipeline/docs/ gsk-pipeline-feb09.pdf
  • An imaging study to investigate the distribution of GSK 239512 in the brain. Available from: http://www.clinicaltrials.gov
  • Drahl C. Curtain rises on potential drugs. ACS meeting news: medicinal chemists disclose candidates for treating neurological, metabolic, and other disorders. Chem Eng News 2009;87:31-3
  • Humbert-Claude M, Morisset S, Gbahou F, Arrang JM. Histamine H3 and dopamine D2 receptor-mediated [35S]GTPgamma[S] binding in rat striatum: evidence for additive effects but lack of interactions. Biochem Pharmacol 2007;73:1172-81
  • Ferrada C, Ferre S, Casado V, et al. Interactions between histamine H3 and dopamine D2 receptors and the implications for striatal function. Neuropharmacology 2008;55:190-7
  • Ferrada C, Moreno E, Casado V, et al. Marked changes in signal transduction upon heteromerization of dopamine D1 and histamine H3 receptors. Br J Pharmacol 2009;157:64-75
  • Jin CY, Anichtchik O, Panula P. Altered histamine H3 receptor radioligand binding in post-mortem brain samples from subjects with psychiatric diseases. Br J Pharmacol 2009;157:118-29
  • Pietro NCD, Seamans JK. Dopamine and serotonin interactions in the prefrontal cortex: insights on antipsychotic drugs and their mechanism of action. Pharmacopsychiatry 2007;40:S27-33
  • Morisset S, Sahm UG, Traiffort E, et al. Atypical neuroleptics enhance histamine turnover in brain via 5-hydroxytryptamine2A receptor blockade. J Pharmacol Exp Ther 1999;288:590-6
  • Southam E, Cilia J, Gartlon JE, et al. Preclinical investigations into the antipsychotic potential of the novel histamine H3 receptor antagonist GSK 207040. Psychopharmacol 2009;201:483-94
  • Ligneau X, Landais L, Perrin D, et al. Brain histamine and schizophrenia: potential therapeutic applications of H3 receptor inverse agonists studied with BF2.649. Biochem Pharmacol 2007;73:1215-24
  • Ferrer International S.A. Monohydrochloride salt of 1-[3-[3-(4-chlorophenyl) propoxy]propyl]-piperidine. WO2006084833A1; 2006
  • A randomized, double blind, placebo controlled, study to demonstrate the cognitive enhancing effects of BF2.649 in people with schizophrenia and schizoaffective disorder. Available from: http://www.clinicaltrials.gov
  • von Coburg Y, Kottke T, Weizel L, et al. Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. Bioorg Med Chem Lett 2009;19:538-42
  • Ito C. Histamine H3 receptor inverse agonists as novel antipsychotics. Cent Nerv Syst Agents Med Chem 2009;9:132-6
  • Stevens DR, Eriksson KS, Brown RE, Haas HL. The mechanism of spontaneous firing in histamine neurons. Behav Brain Res 2001;124:105-12
  • Jones BE. From waking to sleeping: neuronal and chemical substrates. Trends Pharmacol Sci 2005;26:578-86
  • Saras A, Gisselmann G, Vogt-Eisele AK, et al. Histamine action on vertebrate GABAA receptors: direct channel gating and potentiation of GABA responses. J Biol Chem 2008;283:10470-5
  • Brown RE, Sergeeva OA, Eriksson KS, Haas HL. Convergent excitation of dorsal raphe serotonin neurons by multiple arousal systems (orexin/hypocretin, histamine and noradrenaline). J Neurosci 2002;22:8850-9
  • Hong ZY, Huang ZL, Qu WM, Eguchi N. Orexin A promotes histamine, but not norepinephrine or serotonin, release in frontal cortex of mice. Acta Pharmacol Sin 2005;26:155-9
  • Huang ZL, Qu WM, Li WD, et al. Arousal effect of orexin A depends on activation of the histaminergic system. Proc Natl Acad Sci USA 2001;98:9965-70
  • Stevens DR, Kuramasu A, Haas HL. GABAB receptor-mediated control of GABAergic inhibition in rat histaminergic neurons in vitro. Eur J Neurosci 1999;11:1148-54
  • Dauvilliers Y, Arnulf I, Mignot E. Narcolepsy with cataplexy. Lancet 2007;369:499-511
  • John J, Wu MF, Boehmer LN, Siegel JM. Cataplexy-active neurons in the hypothalamus: implications for the role of histamine in sleep and waking behavior. Neuron 2004;42:619-34
  • Parmentier R, Anaclet C, Guhennec C, et al. The brain H3 receptor as a novel therapeutic target for vigilance and sleep-wake disorders. Biochem Pharmacol 2007;73:1157-71
  • Guo RX, Anaclet C, Roberts JC, et al. Differential effects of acute and repeat dosing with the H3 antagonist GSK189254 on the sleep-wake cycle and narcoleptic episodes in Ox-/- mice. Br J Pharmacol 2009;157:104-17
  • Lin JS, Dauvilliers Y, Arnulf I, et al. An inverse agonist of the histamine H3 receptor improves wakefulness in narcolepsy: studies in orexin-/- mice and patients. Neurobiol Dis 2008;30:74-83
  • Ligneau X, Perrin D, Landais L, et al. BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: preclinical pharmacology. J Pharmacol Exp Ther 2007;320:365-75
  • A phase II randomized, double-blind, double-dummy, placebo and comparator-controlled, parallel group, multi-center study to investigate the safety and efficacy of a single dose of JNJ-17216498 administered to subjects with narcolepsy. Available from: http://www.clinicaltrials.gov
  • An open label, dose escalation study with a double blind randomised placebo controlled withdrawal to examine the effects of the histamine H3 antagonist GSK189254 in patients with narcolepsy. Available from: http://www.clinicaltrials.gov
  • Randomized, dose-finding study of BF 2.649 5, 10 20 and 40 mg/d in comparison to placebo in excessive daytime sleepiness in Parkinson's disease patients (PD). Available from: http://www.clinicaltrials.gov
  • Morimoto K, Fahnestock M, Racine RJ. Kindling and status epilepticus models of epilepsy: rewiring the brain. Prog Neurobiol 2004;73:1-60
  • Tuomisto L, Tacke U. Is histamine an anticonvulsive inhibitory transmitter? Neuropharmacol 1986;25:955-8
  • Kamei C, Ishizawa K, Kakinoki H, Fukunaga M. Histaminergic mechanisms in amygdaloid-kindled seizures in rats. Epilepsy Res 1998;30:187-94
  • Dai H, Fu Q, Shen Y, et al. The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neurons. Eur J Pharmacol 2007;563:117-23
  • Yawata I, Tanaka K, Nakagawa Y, et al. Role of histaminergic neurons in development of epileptic seizures in EL mice. Brain Res Mol Brain Res 2004;132:13-7
  • Vohora D, Pal SN, Pillai KK. Histamine and selective H3 receptor ligands: a possible role in the mechanism and management of epilepsy. Pharmacol Biochem Behav 2001;68:735-41
  • Baron R, Schwarz K, Kleinert A, et al. Histamine-induced itch converts into pain in neuropathic hyperalgesia. Neuroreport 2001;12:3475-8
  • Moalem G, Tracey DJ. Immune and inflammatory mechanisms in neuropathic pain. Brain Res Rev 2006;51:240-64
  • White FA, Jung H, Miller RJ. Chemokines and the pathophysiology of neuropathic pain. Proc Natl Acad Sci USA 2007;104:20151-8
  • Medhurst SJ, Collins SD, Billinton A, et al. Novel histamine H3 receptor antagonists GSK 189254 and GSK 334429 are efficacious in surgically-induced and virally-induced rat models of neuropathic pain. Pain 2008;138:61-9
  • Cannon KE, Chazot PL, Hann V, et al. Immunohistochemical localization of histamine H3 receptors in rodent skin, dorsal root ganglia, superior cervical ganglia, and spinal cord: potential antinociceptive targets. Pain 2007;129:76-92
  • Rouleau A, Garbarg M, Ligneau X, et al. Bioavailability, antinociceptive and antiinflammatory properties of BP 2-94, a histamine H3 receptor agonist prodrug. J Pharmacol Exp Ther 1997;281:1085-94
  • Rouleau A, Stark H, Schunack W, Schwartz JC. Anti-inflammatory and antinociceptive properties of BP-294, a histamine H3 receptor agonist prodrug. J Pharmacol Exp Ther 2000;295:219-25
  • Fozard JR. BP-294 Ste Civile Bioprojet. Curr Opin Investig Drugs 2000;1:86-9
  • Cannon KE, Nalwalk JW, Stadel R, et al. Activation of spinal histamine H3 receptors inhibits mechanical nociception. Eur J Pharmacol 2003;470:139-47
  • Smith FM, Haskelberg H, Tracey DJ, Moalem-Taylor G. Role of histamine H3 and H4 receptors in mechanical hyperalgesia following peripheral nerve injury. Neuroimmunomodulation 2007;14:317-25
  • Farzin D, Asghari L, Nowrouzi M. Rodent antinociception following acute treatment with different histamine receptor agonists and antagonists. Pharmacol Biochem Behav 2002;72:751-60
  • Coruzzi G, Adami M, Guaita E, et al. Antiinflammatory and antinociceptive effects of the selective histamine H4 receptor antagonists JNJ-7777120 and VUF 6002 in a rat model of carrageenan-induced acute inflammation. Eur J Pharmacol 2007;563:240-4
  • Liu H, Altenbach RJ, Carr TL, et al. cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11, 11a-octahydrobenzofuro[2,3-h] quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. J Med Chem 2008;51:7094-8
  • Cowart MD, Altenbach RJ, Liu H, et al. Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. J Med Chem 2008;51:6547-57
  • Zampeli E, Tiligada E. The role of histamine H4 receptor in immune and inflammatory disorders. Br J Pharmacol 2009;157:24-33
  • Leurs R, Chazot PL, Shenton FC, et al. Molecular and biochemical pharmacology of the histamine H4 receptor. Br J Pharmacol 2009;157:14-23
  • Sander K, Kottke T, Proschak E, et al. Development of diaminopyrimidines as histamine H4 receptor ligands: virtual screening and scaffold optimization. XXXVIIIth Meeting of the European Histamine Research Society. Fulda, Germany 13 – 16 May 2009. O26
  • Jablonowski JA, Grice CA, Chai W, et al. The first potent and selective non-imidazole human histamine H4 receptor antagonists. J Med Chem 2003;46:3957-60
  • Kiss R, Kiss B, Konczol A, et al. Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening. J Med Chem 2008;51:3145-53
  • Tanrikulu Y, Proschak E, Werner T, et al. Homology model adjustment and ligand screening with a pseudoreceptor of the human histamine H4 receptor. ChemMedChem 2009;4:820-7
  • Igel P, Schneider E, Schnell D, et al. NG-Acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the NG-substituent. J Med Chem 2009;52:2623-7
  • Thurmond RL, Gelfand EW, Dunford PJ. The role of histamine H1 and H4 receptors in allergic inflammation: the search for new antihistamines. Nat Rev Drug Discov 2008;7:41-53
  • O'Reilly M, Alpert R, Jenkinson S, et al. Identification of a histamine H4 receptor on human eosinophils–role in eosinophil chemotaxis. J Recept Signal Transduct Res 2002;22:431-48
  • Thurmond RL, Desai PJ, Dunford PJ, et al. A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther 2004;309:404-13
  • Hofstra CL, Desai PJ, Thurmond RL, Fung-Leung WP. Histamine H4 receptor mediates chemotaxis and calcium mobilization of mast cells. J Pharmacol Exp Ther 2003;305:1212-21
  • Dunford PJ, O'Donnell N, Riley JP, et al. The histamine H4 receptor mediates allergic airway inflammation by regulating the activation of CD4+ T cells. J Immunol 2006;176:7062-70
  • Morgan RK, McAllister B, Cross L, et al. Histamine 4 receptor activation induces recruitment of FoxP3+ T cells and inhibits allergic asthma in a murine model. J Immunol 2007;178:8081-9
  • Dijkstra D, Leurs R, Chazot P, et al. Histamine downregulates monocyte CCL2 production through the histamine H4 receptor. J Allergy Clin Immunol 2007;120:300-7
  • Zampeli E, Thurmond RL, Tiligada E. The histamine H4 receptor antagonist JNJ-7777120 induces increases in the histamine content of the rat conjunctiva. Inflamm Res 2009;58:285-91
  • Yu S, Stahl E, Li Q, Ouyang A. Antigen inhalation induces mast cells and eosinophils infiltration in the guinea pig esophageal epithelium involving histamine-mediated pathway. Life Sci 2008;82:324-30
  • Bell JK, McQueen DS, Rees JL. Involvement of histamine H4 and H1 receptors in scratching induced by histamine receptor agonists in Balb C mice. Br J Pharmacol 2004;142:374-80
  • Bäumer W, Wendorff S, Gutzmer R, et al. Histamine H4 receptors modulate dendritic cell migration through skin: immunomodulatory role of histamine. Allergy 2008;63:1387-94
  • Dunford PJ, Williams KN, Desai PJ, et al. Histamine H4 receptor antagonists are superior to traditional antihistamines in the attenuation of experimental pruritus. J Allergy Clin Immunol 2007;119:176-83
  • Rossbach K, Wendorff S, Sander K, et al. Histamine H4 receptor antagonism reduces hapten-induced scratching behaviour but not inflammation. Exp Dermatol 2009;18:57-63
  • Grzybowska-Kowalczyk A, Wojtecka-Lukasik E, Maslinska D, et al. Distribution pattern of histamine H4 receptor in human synovial tissue from patients with rheumatoid arthritis. Inflamm Res 2007;56(Suppl 1):S59-60
  • Ikawa Y, Suzuki M, Shiono S, et al. Histamine H4 receptor expression in human synovial cells obtained from patients suffering from rheumatoid arthritis. Biol Pharm Bull 2005;28:2016-8
  • Ohki E, Suzuki M, Aoe T, et al. Expression of histamine H4 receptor in synovial cells from rheumatoid arthritic patients. Biol Pharm Bull 2007;30:2217-20
  • Grzybowska-Kowalczyk A, Maslinska D, Wojciechowska M, et al. Expression of histamine H4 receptor in human osteoarthritic synovial tissue. Inflamm Res 2008;57(Suppl 1):S63-4
  • Zampeli E, Thurmond RL, Tiligada E. Effect of the H4R antagonist JNJ7777120 on the cartilage histamine content in rats with adjuvant arthritis. Fund Clin Pharmacol 2008;22:S10
  • Kyriakidis K, Zampeli E, Tiligada E. Effect of the H4 receptor antagonist JNJ7777120 on histamine levels of peripheral blood vessels in rats with adjuvant arthritis. XXXVIIIth Meeting of the European Histamine Research Society. Fulda, Germany 13 – 16 May 2009. O28
  • Boer K, Helinger E, Helinger A, et al. Decreased expression of histamine H1 and H4 receptors suggests disturbance of local regulation in human colorectal tumours by histamine. Eur J Cell Biol 2008;87:227-36
  • Medina V, Cricco G, Nunez M, et al. Histamine-mediated signaling processes in human malignant mammary cells. Cancer Biol Ther 2006;5:1462-71
  • Medina V, Croci M, Crescenti E, et al. The role of histamine in human mammary carcinogenesis: H3 and H4 receptors as potential therapeutic targets for breast cancer treatment. Cancer Biol Ther 2008;7:28-35
  • Rivera ES, Massari N, Medina VA, et al. Histamine-mediated biological responses in WM35 human melanoma cells. XXXVIIIth Meeting of the European Histamine Research Society. Fulda, Germany 13 – 16 May 2009. P30
  • Davenas E, Rouleau A, Morisset S, Arrang JM. Autoregulation of McA-RH7777 hepatoma cell proliferation by histamine H3 receptors. J Pharmacol Exp Ther 2008;326:406-13

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Order Reprints Request Corporate Permissions

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

Request Academic Permissions

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.

Related research

People also read lists articles that other readers of this article have read.

Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine.

Cited by lists all citing articles based on Crossref citations.
Articles with the Crossref icon will open in a new tab.