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Histamine Receptors and Signaling

  • Hargita Hegyesi
  • Zsuzsa Darvas
  • Robin L. Thurmond
  • András Falus
Part of the Springer Series in Biophysics book series (BIOPHYSICS, volume 8)

Keywords

Mast Cell Allergic Rhinitis Histamine Receptor Glia Maturation Factor Bovine Adrenal Chromaffin Cell 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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References

  1. Amin K, Ludviksdottir D, Janson C, Nettelbladt O, Bjornsson E, Roomans GM, Boman G, Seveus L, Venge P (2000) Inflammation and structural changes in the airways of patients with atopic and nonatopic asthma. BHR Group. Am J Resp Crit Care Med 162:2295–2301PubMedGoogle Scholar
  2. Apodaca R, Dvorak CA, Xiao W, Barbier AJ, Boggs JD, Wilson SJ, Lovenberg TW, Carruthers NI (2003) A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines. J Med Chem 46:3938–3944CrossRefPubMedGoogle Scholar
  3. Arias-Montano JA, Floran B, Garcia M, Aceves J, Young JM (2001) Histamine H3 receptor-mediated inhibition of depolarization-induced, dopamine D1 receptor-dependent release of [3H]-γ-aminobutyric acid from rat striatal slices. Br J Pharmacol 133:165–171CrossRefPubMedGoogle Scholar
  4. Arrang JM, Garbarg M, Schwartz JC (1983) Autoinhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. Nature 302:832–837CrossRefPubMedGoogle Scholar
  5. Arrang JM, Garbarg M, Lancelot JC, Lecomte JM, Pollard H, Robba M, Schunack W, Schwartz JC (1987) Highly potent and selective ligands for histamine H3-receptors. Nature 327:117–123CrossRefPubMedGoogle Scholar
  6. Attoub S, Moizo L, Sobhani I, Laigneau J-P, Lewin MJM, Bado A (2001) The H3 receptor is involved in cholecystokinin inhibition of food intake in rats. Life Sci 69:469–478CrossRefPubMedGoogle Scholar
  7. Azzolina A, Guarneri P, Lampiasi N (2002) Involvement of p38 and JNK MAPKs pathways in substance P-induced production of TNF-alpha by peritoneal mast cells. Cytokine 18:72–80CrossRefPubMedGoogle Scholar
  8. Bakker RA, Schoonus SB, Smit MJ, Timmerman H, Leurs R (2001) Histamine H(1)-receptor activation of nuclear factor-kappa B: roles for G beta gamma-and G alpha(q/11)-subunits in constitutive and agonist-mediated signalling. Mol Pharmacol 60:1133–1142PubMedGoogle Scholar
  9. Bakker RA, Casarosa P, Timmerman H, Smit MJ, Leurs R (2004) Constitutively active Gq/11-coupled receptors enable signaling by co-expressed G(i/o)-coupled receptors. J Biol Chem 279:5152–5161CrossRefPubMedGoogle Scholar
  10. Bell JK, McQueen DS, Rees JL (2004) Involvement of histamine H4 and H1 receptors in scratching induced by histamine receptor agonists in Balb C mice. Br J Pharmacol 142(2):374–380CrossRefPubMedGoogle Scholar
  11. Blandina P, Giorgetti M, Bartolini L, Cecchi M, Timmerman H, Leurs R, Pepeu G, Giovannini MG (1996) Inhibition of cortical acetylcholine release and cognitive performance by histamine H3 receptor activation in rats. Br J Pharmacol 119:1656–1664PubMedGoogle Scholar
  12. Blandizzi C, Colucci R, Tognetti M, De Paolis B, Del Tacca M (2001) H3 receptor-mediated inhibition of intestinal acetylcholine release: pharmacological characterization of signal transduction pathways. Naunyn-Schmiedeberg’s Arch Pharmacol 363:193–202CrossRefGoogle Scholar
  13. Bowrey PF, King J, Magarey C, Schwartz P, Marr P, Bolton E, Morris DL (2000) Histamine, mast cells and tumour cell proliferation in breast cancer: does preoperative cimetidine administration have an effect? Br J Cancer 82:167–170CrossRefPubMedGoogle Scholar
  14. Buckland KF, Williams TJ, Conroy DM (2003) Histamine induces cytoskeletal changes in human eosinophils via the H4 receptor. Br J Pharmacol 140:1117–1127CrossRefPubMedGoogle Scholar
  15. Casarosa P, Bakker RA, Verzijl D, Navis M, Timmerman H, Leurs R, Smit MJ (2001) Constitutive signaling of the human cytomegalovirus-encoded chemokine receptor US28. J Biol Chem 276:1133–1137CrossRefPubMedGoogle Scholar
  16. Celuch SM (1995) Possible participation of histamine H3 receptors in the modulation of noradrenaline release from rat spinal cord slices. Eur J Pharmacol 287:127–133CrossRefPubMedGoogle Scholar
  17. Chai W, Breitenbucher JG, Kwok A, Li X, Wong V, Carruthers NI, Lovenberg TW, Mazur C, Wilson SJ, Axe FU, Jones TK (2003) Non-imidazole heterocyclic histamine H3 receptor antagonists. Bioorg Med Chem Lett 13:1767–1770CrossRefPubMedGoogle Scholar
  18. Chen J, Liu C, Lovenberg TW (2003) Molecular and pharmacological characterization of the mouse histamine H3 receptor. Eur J Pharmacol 467:57–65CrossRefPubMedGoogle Scholar
  19. Clapham J, Kilpatrick GJ (1992) Histamine H3 receptors modulate the release of [3H]acetylcholine from slices of rat entorhinal cortex: evidence for the possible existence of H3 receptor subtypes. Br J Pharmacol 107:919–923PubMedGoogle Scholar
  20. Clark EA, Hill SJ (1996) Sensitivity of histamine H3 receptor agonist-stimulated [35S]GTP gamma[S] binding to pertussis toxin. Eur J Pharmacol 296:223–225CrossRefPubMedGoogle Scholar
  21. Clark RAF, Gallin JI, Kaplan AP (1975) Selective eosinophil chemotactic activity of histamine. J Exp Med 142:1462–1476CrossRefPubMedGoogle Scholar
  22. Clark RAF, Sandler JA, Gallin JI, Kaplan AP (1977) Histamine modulation of eosinophil migration. J Immunol 118:137–145PubMedGoogle Scholar
  23. Coge F, Guenin S-P, Audinot V, Renouard-Try A, Beauverger P, Macia C, Ouvry C, Nagel N, Rique H, Boutin JA, Galizzi J-P (2001a) Genomic organization and characterization of splice variants of the human histamine H3 receptor. Biochem J 355:279–288CrossRefPubMedGoogle Scholar
  24. Coge F, Guenin S-P, Rique H, Boutin JA, Galizzi J-P (2001b) Structure and expression of the human histamine H4-receptor gene. Biochem Biophys Res Commun 284:301–309CrossRefPubMedGoogle Scholar
  25. Crimi E, Chiaramondia M, Milanese M, Rossi GA, Brusasco V (1991) Increased numbers of mast cells in bronchial mucosa after the late-phase asthmatic response to allergen. Am Rev Resp Dis 144:1282–1286PubMedGoogle Scholar
  26. Curran MP, Scott LJ, Perry CM (2004) Cetirizine: a review of its use in allergic disorders. Drugs 64:523–561PubMedGoogle Scholar
  27. Davio C, Cricco G, Bergoc R, Andrade N, Rivera E (1993) H1 and H2 histamine receptors in human mammary carcinomas. Agents Actions Spec Conf Issue 38:71–74Google Scholar
  28. Del Valle J, Gantz I (1997) Novel insights into histamine H2 receptor biology. Am J Physiol 273:G987–G996PubMedGoogle Scholar
  29. Drutel G, Peitsaro N, Karlstedt K, Wieland K, Smit MJ, Timmerman H, Panula P, Leurs R (2001) Identification of rat H3 receptor isoforms with different brain expression and signaling properties. Mol Pharmacol 59:1–8PubMedGoogle Scholar
  30. Elz S, Kramer K, Pertz HH, Detert H, Laak AM, Kuhne R, Schunack W (2000) Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists. J Med Chem 43:1071–1084CrossRefPubMedGoogle Scholar
  31. Endou M, Levi R (1995) Histamine in the heart. Eur J Clin Invest 25(Suppl 1): 5–11PubMedGoogle Scholar
  32. Endou M, Poli E, Levi R (1994) Histamine H3-receptor signaling in the heart: possible involvement of Gi/Go proteins and N-type Ca++ channels. J Pharmacol Exp Ther 269:221–229PubMedGoogle Scholar
  33. Esbenshade TA, Krueger KM, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Fox GB, Faghih R, Bennani YL, Williams M, Hancock AA (2003) Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects. J Pharmacol Exp Ther 305:887–896CrossRefPubMedGoogle Scholar
  34. Faghih R, Dwight W, Black L, Liu H, Gentles R, Phelan K, Esbenshade TA, Ireland L, Miller TR, Kang C-H, Krueger KM, Fox GB, Hancock AA, Bennani YL (2002a) Structure—activity relationships of non-imidazole H3 receptor ligands. Part 2: binding preference for δ-amino acids motifs. Bioorg Med Chem Letters 12:2035–2037CrossRefGoogle Scholar
  35. Faghih R, Dwight W, Vasudevan A, Dinges J, Conner SE, Esbenshade TA, Bennani YL, Hancock AA (2002b) Aminoalkoxybiphenylnitriles as histamine-3 receptor ligands. Bioorg Med Chem Lett 12:3077–3079CrossRefPubMedGoogle Scholar
  36. Faghih R, Dwight W, Pan JB, Fox GB, Krueger KM, Esbenshade TA, McVey JM, Marsh K, Bennani YL, Hancock AA (2003) Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists. Bioorg Med Chem Lett 13:1325–1328CrossRefPubMedGoogle Scholar
  37. Fink K, Schlicker E, Neise A, Gothert M (1990) Involvement of presynaptic H3 receptors in the inhibitory effect of histamine on serotonin release in the rat brain cortex. Naunyn-Schmiedeberg’s Arch Pharmacol 342:513–519Google Scholar
  38. Fokkens WJ, Godthelp T, Holm AF, Blom H, Mulder PG, Vroom TM, Rijntjes E (1992) Dynamics of mast cells in the nasal mucosa of patients with allergic rhinitis and non-allergic controls: a biopsy study. Clin Exp Allergy 22:701–710PubMedGoogle Scholar
  39. Fox GB, Pan JB, Esbenshade TA, Bennani YL, Black LA, Faghih R, Hancock AA, Decker MW (2002) Effects of histamine H3 receptor ligands GT-2331 and ciproxifan in a repeated acquisition avoidance response in the spontaneously hypertensive rat pup. Behav Brain Res 131:151–161CrossRefPubMedGoogle Scholar
  40. Gantner F, Sakai K, Tusche MW, Cruikshank WW, Center DM, Bacon KB (2002) Histamine H4 and H2 receptors control histamine-induced interleukin-16 release from human CD8+ T cells. J Pharmacol Exp Ther 303:300–307CrossRefPubMedGoogle Scholar
  41. Gantz I, Munzert G, Tashiro T, Schaffer M, Wang L, DelValle J, Yamada T (1991) Molecular cloning of the human histamine H2 receptor. Biochem Biophys Res Commun 178:1386–1392CrossRefPubMedGoogle Scholar
  42. Garbarg M, Schwartz JC (1988) Synergism between histamine H1-and H2-receptors in the cAMP response in guinea pig brain slices: effects of phorbol esters and calcium. Mol Pharmacol 33:38–43PubMedGoogle Scholar
  43. Gauvreau GM, Lee JM, Watson RM, Irani AM, Schwartz LB, O’Byrne PM (2000) Increased numbers of both airway basophils and mast cells in sputum after allergen inhalation challenge of atopic asthmatics. Am J Resp Crit Care Med 161:1473–1478PubMedGoogle Scholar
  44. Gfesser GA, Zhang H, Dinges J, Fox GB, Pan JB, Esbenshade TA, Yao BB, Witte D, Miller TR, Kang C-H, Krueger KM, Bennani YL, Hancock AA, Faghih R (2004) Structure-activity relationships of non-imidazole H3 receptor ligands. Part 3: 5-substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists. Bioorg Med Chem Lett 14:673–676CrossRefPubMedGoogle Scholar
  45. Giovannini MG, Bartolini L, Bacciottini L, Greco L, Blandina P (1999) Effects of histamine H3 receptor agonists and antagonists on cognitive performance and scopolamine-induced amnesia. Behav Brain Res 104:147–155CrossRefPubMedGoogle Scholar
  46. Griffiths J, Marley PD (2001) Ca2+-dependent activation of tyrosine hydroxylase involves MEK1. Neuroreport 12:2679–2683CrossRefPubMedGoogle Scholar
  47. Hagermark O (1992) Peripheral and central mediators of itch. Skin Pharmacol 5:1–8PubMedGoogle Scholar
  48. Hashimoto T, Harusawa S, Araki L, Zuiderveld Obbe P, Smit Martine J, Imazu T, Takashima S, Yamamoto Y, Sakamoto Y, Kurihara T, Leurs R, Bakker Remko A, Yamatodani A (2003) A selective human H(4)-receptor agonist: (-)-2-cyano-1-methyl-3-[(2R,5R)-5-[1H-imidazol-4(5)-yl]tetrahydrofuran-2-y] methylguanidine. J Med Chem 46:3162–3165CrossRefPubMedGoogle Scholar
  49. Hattori Y, Gando S, Endou M, Kanno M (1991) Characterization of histamine receptors modulating inotropic and biochemical activities in rabbit left atria. Eur J Pharmacol 196:29–36CrossRefPubMedGoogle Scholar
  50. Henz BM, Metzenauer P, O’Keefe E, Zuberbier T (1998) Differential effects of new-generation H1-receptor antagonists in pruritic dermatoses. Allergy 53:180–183PubMedGoogle Scholar
  51. Hill SJ, Young JM, Marrian DH (1977) Specific binding of 3H-mepyramine to histamine H1 receptors in intestinal smooth muscle. Nature 270:361–363CrossRefPubMedGoogle Scholar
  52. Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R, Haas HL (1997) International Union of Pharmacology. XIII. Classification of histamine receptors. Pharmacol Rev 49:253–278PubMedGoogle Scholar
  53. Hofstra CL, Desai PJ, Thurmond RL, Fung-Leung W-P (2003) Histamine H4 receptor mediates chemotaxis and calcium mobilization of mast cells. J Pharmacol Exp Ther 305:1212–1221CrossRefPubMedGoogle Scholar
  54. Hough LB (2001) Genomics meets histamine receptors: new subtypes, new receptors. Mol Pharmacol 59:415–419PubMedGoogle Scholar
  55. Howarth PH, Salagean M, Dokic D (2000) Allergic rhinitis: not purely a histamine-related disease. Allergy 55(Suppl 64):7–16CrossRefPubMedGoogle Scholar
  56. Igaz P, Fitzimons CP, Szalai C, Falus A (2002) Histamine genomics in silico: polymorphisms of the human genes involved in the synthesis, action and degradation of histamine. Am J Pharmacogenom 2:67–72Google Scholar
  57. Imamura M, Lander HM, Levi R (1996) Activation of histamine H3-receptors inhibits carriermediated norepinephrine release during protracted myocardial ischemia: comparison with adenosine A1-receptors and A2-adrenoceptors. Circ Res 78:475–481PubMedGoogle Scholar
  58. Inoue I, Yanai K, Kitamura D, Taniuchi I, Kobayashi T, Niimura K, Watanabe T (1996) Impaired locomotor activity and exploratory behavior in mice lacking histamine H1 receptors. Proc Nat Acad Sci USA 93:13316–13320CrossRefPubMedGoogle Scholar
  59. Itoh E, Fujimiya M, Inui A (1999) Thioperamide, a histamine H3 receptor antagonist, powerfully suppresses peptide YY-induced food intake in rats. Biol Psychiatry 45:475–481CrossRefPubMedGoogle Scholar
  60. Jablonowski JA, Carruthers NI, Thurmond RL (2004) Histamine H4 receptor and potential therapeutic uses for H4 ligands. Mini Rev Med Chem 4(9):993–1000PubMedGoogle Scholar
  61. Jang I-S, Rhee J-S, Watanabe T, Akaike N, Akaike N (2001) Histaminergic modulation of GABAergic transmission in rat ventromedial hypothalamic neurons. J Physiol 534:791–803CrossRefPubMedGoogle Scholar
  62. Kassel O, De Blay F, Duvernelle C, Olgart C, Israel-Biet D, Krieger P, Moreau L, Muller C, Pauli G, Frossard N (2001) Local increase in the number of mast cells and expression of nerve growth factor in the bronchus of asthmatic patients after repeated inhalation of allergen at low-dose. Clin Exp Allergy 31:1432–1440CrossRefPubMedGoogle Scholar
  63. Kilpatrick GJ, Michel AD (1991) Characterization of the binding of the histamine H3 receptors agonist [3H](R)-alpha-methyl histamine to homogenates of rat and guinea pig cortex. Agents Actions Suppl 33:69–75PubMedGoogle Scholar
  64. Kirby JG, Hargreave FE, Gleich GJ, O’Byrne PM (1987) Bronchoalveolar cell profiles of asthmatic and nonasthmatic subjects. Am Rev Resp Dis 136:379–383PubMedGoogle Scholar
  65. Kobayashi T, Tonai S, Ishihara Y, Koga R, Okabe S, Watanabe T (2000) Functional and morphological regulation of the gastric mucosa in histamine H2 receptor-deficient mice. J Clin Invest 105:1741–1749PubMedGoogle Scholar
  66. Korte A, Myers J, Shih NY, Egan RW, Clark MA (1990) Characterization and tissue distribution of H3 histamine receptors in guinea pigs by Na-methylhistamine. Biochem Biophys Res Commun 168:979–986CrossRefPubMedGoogle Scholar
  67. Koyama M, Heerdt PM, Levi R (2003a) Increased severity of reperfusion arrhythmias in mouse hearts lacking histamine H3-receptors. Biochem Biophys Res Commun 306:792–796CrossRefPubMedGoogle Scholar
  68. Koyama M, Seyedi N, Fung-Leung W-P, Lovenberg TW, Levi R (2003b) Norepinephrine release from the ischemic heart is greatly enhanced in mice lacking histamine H3 receptors. Mol Pharmacol 63:378–382CrossRefPubMedGoogle Scholar
  69. Krishnaswamy G, Kelley J, Johnson D, Youngberg G, Stone W, Huang SK, Bieber J, Chi DS (2001) The human mast cell: functions in physiology and disease. Front Biosci 6:1109–1127Google Scholar
  70. Kubo Y, Nakano K (1999) Regulation of histamine synthesis in mouse CD4+ and CD8+ T lymphocytes. Inflamm Res 48:149–153CrossRefPubMedGoogle Scholar
  71. Lacey JV Jr, Sherman ME, Hartge P, Schatzkin A, Schairer C (2004) Medication use and risk of ovarian carcinoma: a prospective study. Int J Cancer 108:281–286CrossRefPubMedGoogle Scholar
  72. Larsen JS (2001) Do antihistamines have a role in asthma therapy? Pharmacotherapy 21 (3 Pt 2):28S–33SCrossRefPubMedGoogle Scholar
  73. Lee JJ, Parsons ME (2000) Signaling mechanisms coupled to presynaptic A1-and H3-receptors in the inhibition of cholinergic contractile responses of the guinea pig ileum. J Pharmacol Exp Ther 295:607–613PubMedGoogle Scholar
  74. Leurs R, Traiffort E, Arrang JM, Tardivel-Lacombe J, Ruat M, Schwartz JC (1994) Guinea pig histamine H1 receptor. II. Stable expression in Chinese hamster ovary cells reveals the interaction with three major signal transduction pathways. J Neurochem 2:519–527Google Scholar
  75. Leurs R, Smit MJ, Timmerman H (1995) Molecular pharmacological aspects of histamine receptors. Pharmacol Ther 66:413–463CrossRefPubMedGoogle Scholar
  76. Levi R, Smith NCE (2000) Histamine H3-receptors: a new frontier in myocardial ischemia. J Pharmacol Exp Ther 292:825–830PubMedGoogle Scholar
  77. Li D, Wen JF, Jin JY, Jin H, Ann HS, Kim SZ, Kim SH, Lee HS, Cho KW (2003) Histamine inhibits atrial myocytic ANP release via H2 receptor-cAMP-protein kinase signalling Am J Physiol-Regul Integr Comp Physiol 285(2):R380–R393PubMedGoogle Scholar
  78. Lin JS, Sakai K, Vanni-Mercier G, Arrang JM, Garbarg M, Schwartz JC, Jouvet M (1990) Involvement of histaminergic neurons in arousal mechanisms demonstrated with H3-receptor ligands in the cat. Brain Res 523:325–330CrossRefPubMedGoogle Scholar
  79. Ling P, Ngo K, Nguyen S, Thurmond RL, Edwards JP, Karlsson L, Fung-Leung W-P (2004) Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule up-regulation. Br J Pharmacol 142(1):161–171CrossRefPubMedGoogle Scholar
  80. Linney ID, Buck IM, Harper EA, Kalindjian SB, Pether MJ, Shankley NP, Watt GF, Wright PT (2000) Design, synthesis, and structure-activity relationships of novel non-imidazole histamine H3 receptor antagonists. J Med Chem 43:2362–2370CrossRefPubMedGoogle Scholar
  81. Liu C, Ma XJ, Lovenberg TW (2000) Alternative splicing of the histamine H3 receptor mRNA at the third cytoplasmic loop is not detectable in humans. Mol Brain Res 83:145–150CrossRefPubMedGoogle Scholar
  82. Liu C, Ma X-J, Jiang X, Wilson SJ, Hofstra CL, Blevitt J, Pyati J, Li X, Chai W, Carruthers N, Lovenberg TW (2001a) Cloning and pharmacological characterization of a fourth histamine receptor (H4) expressed in bone marrow. Mol Pharmacol 59:420–426PubMedGoogle Scholar
  83. Liu C, Wilson SJ, Kuei C, Lovenberg TW (2001b) Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation. J Pharmacol Exp Ther 299:121–130PubMedGoogle Scholar
  84. Longhurst PA, McNeill JH (1982) Rabbit atrial histamine receptors and cyclic AMP. Can J Physiol Pharmacol 60:1730–1732PubMedGoogle Scholar
  85. Lordan JL, Holgate ST (2002) H1-antihistamines in asthma. Clin Allergy Immunol 17:221–248PubMedGoogle Scholar
  86. Lovenberg TW, Roland BL, Wilson SJ, Jiang X, Pyati J, Huvar A, Jackson MR, Erlander MG (1999) Cloning and functional expression of the human histamine H3 receptor. Mol Pharmacol 55:1101–1107PubMedGoogle Scholar
  87. Lovenberg TW, Pyati J, Chang H, Wilson SJ, Erlander MG (2000) Cloning of rat histamine H3 receptor reveals distinct species pharmacological profiles. J Pharmacol Exp Ther 293:771–778PubMedGoogle Scholar
  88. Marone G, Casolaro V, Patella V, Florio G, Triggiani M (1997) Molecular and cellular biology of mast cells and basophils. Int Arch Allergy Appl Immunol 114:207–217Google Scholar
  89. Martinez-Mir MI, Pollard H, Moreau J, Arrang JM, Ruat M, Traiffort E, Schwartz JC, Palacios JM (1990) Three histamine receptors (H1, H2 and H3) visualized in the brain of human and non-human primates. Brain Res 526:322–327CrossRefPubMedGoogle Scholar
  90. Masaki TH, Yoshimatsu S, Chiba T, Watanabe T, Sakata T (2001) Targeted disruption of histamine H1-receptor attenuates regulatory effects of leptin on feeding, adiposity, and UCP family in mice. Diabetes 50:385–391PubMedGoogle Scholar
  91. Megson AC, Walker EM, Hill SJ (2001) Role of protein kinase Calpha in signaling from the histamine H(1) receptor to the nucleus. Mol Pharmacol 59:1012–1021PubMedGoogle Scholar
  92. Meier G, Ligneau X, Pertz HH, Ganellin CR, Schwartz J-C, Schunack W, Stark H (2002) Piperidine-hydrocarbon compounds as novel non-imidazole histamine H3-receptor antagonists. Bioorg Med Chem 10:2535–2542CrossRefPubMedGoogle Scholar
  93. Miko T, Ligneau X, Pertz HH, Ganellin CR, Arrang J-M, Schwartz J-C, Schunack W, Stark H (2003) Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl) piperidines and related compounds. J Med Chem 46:1523–1530CrossRefPubMedGoogle Scholar
  94. Mobarakeh JI, Sakurada S, Katsuyama S, Kutsuwa M, Kuramasu A, Lin ZY, Watanabe T, Hashimoto Y, Yanai K (2000) Role of histamine H1 receptor in pain perception: a study of the receptor gene knockout mice. Eur J Pharmacol 391:81–89CrossRefPubMedGoogle Scholar
  95. Molina-Hernandez A, Nunez A, Arias-Montano JA (2000) Histamine H3-receptor activation inhibits dopamine synthesis in rat striatum. Neuroreport 11:163–166PubMedGoogle Scholar
  96. Molina-Hernandez A, Nunez A, Sierra J-J, Arias-Montano J-A (2001) Histamine H3 receptor activation inhibits glutamate release from rat striatal synaptosomes. Neuropharmacology 41:928–934CrossRefPubMedGoogle Scholar
  97. Monti JM, Jantos H, Boussard M, Altier H, Orellana C, Olivera S (1991) Effects of selective activation or blockade of the histamine H3 receptor on sleep and wakefulness. Eur J Pharmacol 205:283–287CrossRefPubMedGoogle Scholar
  98. Morisset S, Rouleau A, Lineau X, Gbahou F, Tardivel-Lacombe J, Stark H, Schunack W, Ganellin CR, Schwartz JC, Arrang J-M (2000) High constitutive activity of native H3 receptors regulates histamine neurons in brain. Nature 408:860–864CrossRefPubMedGoogle Scholar
  99. Morse KL, Behan J, Laz TM, West RE Jr, Greenfeder SA, Anthes JC, Umland S, Wan Y, Hipkin RW, Gonsiorek W, Shin N, Gustafson EL, Qiao X, Wang S, Hedrick JA, Greene J, Bayne M, Monsma FJ Jr (2001) Cloning and characterization of a novel human histamine receptor. J Pharmacol Exp Ther 296:1058–1066PubMedGoogle Scholar
  100. Nagahara A, Wang L, Del Valle J, Todisco A (1998) Regulation of c-Jun NH2-terminal kinases in isolated canine gastric parietal cells. Am J Physiol 275:G740–G748PubMedGoogle Scholar
  101. Nakamura T, Itadani H, Hidaka Y, Ohta M, Tanaka K (2000) Molecular cloning and characterization of a new human histamine receptor, HH4R. Biochem Biophys Res Commun 279:615–620CrossRefPubMedGoogle Scholar
  102. Nguyen T, Shapiro DA, George SR, Setola V, Lee DK, Cheng R, Rauser L, Lee SP, Lynch KR, Roth BL, O’Dowd BF (2001) Discovery of a novel member of the histamine receptor family. Mol Pharmacol 59:427–433PubMedGoogle Scholar
  103. Oda T, Morikawa N, Saito Y, Masuho Y, Matsumoto S-I (2000) Molecular cloning and characterization of a novel type of histamine receptor preferentially expressed in leukocytes. J Biol Chem 275:36781–36786CrossRefPubMedGoogle Scholar
  104. Ohkubo T, Shibata M, Inoue M, Kaya H, Takahashi H (1995) Regulation of substance P release mediated via prejunctional histamine H3 receptors. Eur J Pharmacol 273:83–88CrossRefPubMedGoogle Scholar
  105. Orange PR, Heath PR, Wright SR, Pearson RC (1996) Allelic variations of the human histamine H2 receptor gene. Neuroreport 7:1293–1296PubMedGoogle Scholar
  106. O’Reilly M, Alpert R, Jenkinson S, Gladue RP, Foo S, Trim S, Peter B, Trevethick M, Fidock M (2002) Identification of a histamine H4 receptor on human eosinophils — role in eosinophil chemotaxis. J Recept Signal Tr R 22:431–448CrossRefGoogle Scholar
  107. Osna N, Elliott K, Khan MM (2001) Regulation of interleukin-10 secretion by histamine in TH2 cells and splenocytes. Int Immunopharmacol 1:85–96CrossRefPubMedGoogle Scholar
  108. Packard KA, Khan MM (2003) Effects of histamine on Th1/Th2 cytokine balance. Int Immunopharmacol 3:909–920CrossRefPubMedGoogle Scholar
  109. Peterson LJ, Hansen U, Kristensen JK, Nielsen H, Skov PS, Nielsen HJ (1998) Studies on mast cells and histamine release in psoriasis: the effect of ranitidine. Acta Dermatol Venereol (Stockholm) 78:190–193CrossRefGoogle Scholar
  110. Poli E, Pozzoli C, Coruzzi G, Bertaccini G (1993) Histamine H3-receptor-induced inhibition of duodenal cholinergic transmission is independent of intracellular cyclic AMP and GMP. Gen Pharmacol 24:1273–1278PubMedGoogle Scholar
  111. Poli E, Pozzoli C, Coruzzi G, Bertaccini G (1994) Signal transducing mechanisms coupled to histamine H3 receptors and alpha-2 adrenoceptors in the guinea pig duodenum: possible involvement of N-type Ca++ channels. J Pharmacol Exp Ther 270:788–794PubMedGoogle Scholar
  112. Pollard H, Moreau J, Arrang JM, Schwartz JC (1993) A detailed autoradiographic mapping of histamine H3 receptors in rat brain areas. Neuroscience 52:169–189CrossRefPubMedGoogle Scholar
  113. Poluektova LY, Huggler GK, Patterson EB, Khan MM (1999) Involvement of protein kinase A in histamine-mediated inhibition of IL-2mRNA expression in mouse splenocytes. Immunopharmacology 41:77–87CrossRefPubMedGoogle Scholar
  114. Raible DG, Schulman ES, DiMuzio J, Cardillo R, Post TJ (1992) Mast cell mediators prostaglandin-D2 and histamine activate human eosinophils. J Immunol 148:3536–3542PubMedGoogle Scholar
  115. Raible DG, Lenahan T, Fayvilevich Y, Kosinski R, Schulman ES (1994) Pharmacologic characterization of a novel histamine receptor on human eosinophils. Am J Res Crit Care Med 149:1506–1511Google Scholar
  116. Robinson AJ, Dickenson JM (2001) Activation of the p38 and p42/p44 mitogen-activated protein kinase families by the histamine H(1) receptor in DDT(1)MF-2 cells. Br J Pharmacol 133:1378–1386CrossRefPubMedGoogle Scholar
  117. Sasaki Y, Ihara K, Ahmed S, Yamawaki K, Kusuhara K, Nakayama H, Nishima S, Hara T (2000) Lack of association between atopic asthma and polymorphisms of the histamine H1 receptor, histamine H2 receptor, and histamine N-methyltransferase genes. Immunogenetics 51:238–240CrossRefPubMedGoogle Scholar
  118. Schlicker E, Betz R, Gothert M (1988) Histamine H3 receptor-mediated inhibition of serotonin release in the rat brain cortex. Naunyn-Schmiedeberg’s Arch Pharmacol 337:588–590Google Scholar
  119. Schlicker E, Fink K, Detzner M, Gothert M (1993) Histamine inhibits dopamine release in the mouse striatum via presynaptic H3 receptors. J Neural Transm Gen Sect 93:1–10CrossRefPubMedGoogle Scholar
  120. Schlicker E, Kathmann M, Detzner M, Exner HJ, Gothert M (1994) H3 receptor-mediated inhibition of noradrenaline release: an investigation into the involvement of Ca2+ and K+ ions, G protein and adenylate cyclase. Naunyn-Schmiedeberg’s Arch Pharmacol 350:34–41Google Scholar
  121. Schwartz JC, Morisset S, Rouleau A, Ligneau X, Gbahou F, Tardivel-Lacombe J, Stark H, Schunack W, Ganellin CR, Arrang JM (2003) Therapeutic implications of constitutive activity of receptors: the example of the histamine H3 receptor. J Neural Transm Suppl 64:1–16PubMedGoogle Scholar
  122. Shah C, McAtee L, Breitenbucher JG, Rudolph D, Li X, Lovenberg TW, Mazur C, Wilson SJ, Carruthers NI (2002) Novel human histamine H3 receptor antagonists. Bioorg Med Chem Lett 12:3309–3312CrossRefPubMedGoogle Scholar
  123. Shahrestanifar M, Fan X, Manning DR (1999) Lysophosphatidic acid activates NF-kappaB in fibroblasts. A requirement for multiple inputs. J Biol Chem 274:3828–3833CrossRefPubMedGoogle Scholar
  124. Shin N, Coates E, Murgolo NJ, Morse KL, Bayne M, Strader CD, Monsma FJ Jr (2002) Molecular modeling and site-specific mutagenesis of the histamine-binding site of the histamine H4 receptor. Mol Pharmacol 62:38–47CrossRefPubMedGoogle Scholar
  125. Silver RB, Mackins CJ, Smith NCE, Koritchneva IL, Lefkowitz K, Lovenberg TW, Levi R (2001) Coupling of histamine H3 receptors to neuronal Na+/H+ exchange: a novel protective mechanism in myocardial ischemia. Proc Natl Acad Sci USA 98:2855–2859CrossRefPubMedGoogle Scholar
  126. Simons FE, Sussman GL, Simons KJ (1995) Effect of H2-antagonist cimetidine on the pharmacokinetics and pharmacodynamics of the H1-receptor antagonists hydroxyzine and cetirizine in patients with chronic urticaria. J Allergy Clin Immun 95:685–693CrossRefPubMedGoogle Scholar
  127. Slater A, Smallman LA, Drake-Lee AB (1996) Increase in epithelial mast cell numbers in the nasal mucosa of patients with perennial allergic rhinitis. J Laryngol Otol 110:929–933PubMedGoogle Scholar
  128. Smit MJ, Hoffmann M, Timmerman H, Leurs R (1999) Molecular properties and signalling pathways of the histamine H1 receptor. Clin Exp Allergy 29(Suppl 3):19–28PubMedGoogle Scholar
  129. Sonobe Y, Nakane H, Watanabe T, Nakano K (2004) Regulation of Con A-dependent cytokine production from CD4+ and CD8+ T lymphocytes by autosecretion of histamine. Inflamm Res 53:87–92CrossRefPubMedGoogle Scholar
  130. Stark H (2003) Recent advances in histamine H3/H4 receptor ligands. Expert Opin Ther Pat 13:851–865CrossRefGoogle Scholar
  131. Takagishi T, Sasaguri Y, Nakano R, Arima N, Tanimoto A, Fukui H, Morimatsu M (1995) Expression of the histamine H1 receptor gene in relation to atherosclerosis. Am J Pathol 146:981–988PubMedGoogle Scholar
  132. Takahashi K, Suwa H, Ishikawa T, Kotani H (2002) Targeted disruption of H3 receptors results in changes in brain histamine tone leading to an obese phenotype. J Clin Invest 110:1791–1799CrossRefPubMedGoogle Scholar
  133. Takeshita K, Sakai K, Bacon KB, Gantner F (2003) Critical role of histamine H4 receptor in leukotriene B4 production and mast cell-dependent neutrophil recruitment induced by zymosan in vivo. J Pharmacol Exp Ther 307:1072–1078CrossRefPubMedGoogle Scholar
  134. Tardivel-Lacombe J, Morisset S, Gbahou F, Schwartz JC, Arrang J-M (2001) Chromosomal mapping and organization of the human histamine H3 receptor gene. Neuroreport 12:321–324CrossRefPubMedGoogle Scholar
  135. Thurmond RL, Desai PJ, Dunford PJ, Fung-Leung W-P, Hofstra CL, Jiang W, Nguyen S, Riley JP, Sun S, Williams KN, Edwards JP, Karlsson L (2004) A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther 309:404–413CrossRefPubMedGoogle Scholar
  136. Toyota H, Dugovic C, Koehl M, Laposky AD, Weber C, Ngo K, Wu Y, Lee DH, Yanai K, Sakurai E, Watanabe T, Liu C, Chen J, Barbier AJ, Turek FW, Fung-Leung WP, Lovenberg TW (2002) Behavioral characterization of mice lacking histamine H3 receptors. Mol Pharmacol 62:389–397CrossRefPubMedGoogle Scholar
  137. Turner SC, Esbenshade TA, Bennani YL, Hancock AA (2003) A new class of histamine H3-receptor antagonists: synthesis and structure-activity relationships of 7,8,9,10-tetrahydro-6-Hcyclohepta[ß]quinolines. Bioorg Med Chem Lett 13:2131–2135CrossRefPubMedGoogle Scholar
  138. van der Goot H, Timmerman H (2000) Selective ligands as tools to study histamine receptors. Eur J Med Chem 35:5–20CrossRefPubMedGoogle Scholar
  139. Vasudevan A, Conner SE, Gentles RG, Faghih R, Liu H, Dwight W, Ireland L, Kang CH, Esbenshade TA, Bennani YL, Hancock AA (2002) Synthesis and evaluation of potent pyrrolidine H3 antagonists. Bioorg Med Chem Lett 12:3055–3058CrossRefPubMedGoogle Scholar
  140. Wadee AA, Anderson R, Sher R (1980) In vitro effects of histamine on eosinophil migration. Int Arch Allergy Appl Immunol 63:322–329PubMedGoogle Scholar
  141. Walczynski K, Guryn R, Zuiderveld OP, Timmerman H (1999) Non-imidazole histamine H3 ligands. Part 2. New 2-substituted benzothiazoles as histamine H3 antagonists. Arch Pharm 332:389–398CrossRefGoogle Scholar
  142. Walsh GM (2002) Second-generation antihistamines in asthma therapy: is there a protective effect? Am J Resp Med 1:27–34Google Scholar
  143. Weiger T, Stevens DR, Wunder L, Haas HL (1997) Histamine H1 receptors in C6 glial cells are coupled to calcium-dependent potassium channels via release of calcium from internal stores. Naunyn-Schmiedeberg’s Arch Pharmacol 355:559–565Google Scholar
  144. Wellendorph P, Goodman MW, Burstein ES, Nash NR, Brann MR, Weiner DM (2002) Molecular cloning and pharmacology of functionally distinct isoforms of the human histamine H3 receptor. Neuropharmacology 42:929–940CrossRefPubMedGoogle Scholar
  145. Wellner-Kienitz MC, Bender K, Meyer T, Pott L (2003) Coupling to Gs and G(q/11) of histamine H2 receptors heterologously expressed in adult rat atrial myocytes. Biochim Biophys Acta 1642:67–77CrossRefPubMedGoogle Scholar
  146. Wiedemann P, Boenisch H, Oerters F, Bruess M (2002) Structure of the human histamine H3 receptor gene (HRH3) and identification of naturally occurring variations. J Neural Transm 109:443–453CrossRefPubMedGoogle Scholar
  147. Wieland K, Bongers G, Yamamoto Y, Hashimoto T, Yamatodani A, Menge WMBP, Timmerman H, Lovenberg TW, Leurs R (2001) Constitutive activity of histamine H3 receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H3 antagonists. J Pharmacol Exp Ther 299:908–914PubMedGoogle Scholar
  148. Woolley DE (2003) The mast cell in inflammatory arthritis. New Engl J Med 348:1709–1711CrossRefPubMedGoogle Scholar
  149. Xie P, Browning DD, Hay N, Mackman N, Ye RD (2000) Activation of NF-kappa B by bradykinin through a Galpha(q)-and Gbeta gamma-dependent pathway that involves phosphoinositide 3-kinase and Akt. J Biol Chem 275:24907–24914CrossRefPubMedGoogle Scholar
  150. Yamasaki T, Tamai I, Matsumura Y (2001) Activation of histamine H3 receptors inhibits renal noradrenergic neurotransmission in anesthetized dogs. Am J Physiol 280:R1450–R1456Google Scholar
  151. Yanai K, Son LZ, Endou M, Sakurai E, Nakagawasai O, Tadano T, Kisara K, Inoue I, Watanabe T (1998) Behavioural characterization and amounts of brain monoamines and their metabolites in mice lacking histamine H1 receptors. Neuroscience 87:479–487CrossRefPubMedGoogle Scholar
  152. Zaheer A, Lim R (1998) Overexpression of glia maturation factor (GMF) in PC12 pheochromocytoma cells activates p38 MAP kinase, MAPKAP kinase-2, and tyrosine hydroxylase. Biochem Biophys Res Commun 250:278–282CrossRefPubMedGoogle Scholar
  153. Zhu Y, Michalovich D, Wu H-L, Tan KB, Dytko GM, Mannan IJ, Boyce R, Alston J, Tierney LA, Li X, Herrity NC, Vawter L, Sarau HM, Ames RS, Davenport CM, Hieble JP, Wilson S, Bergsma DJ, Fitzgerald LR (2001) Cloning, expression, and pharmacological characterization of a novel human histamine receptor. Mol Pharmacol 59:434–441PubMedGoogle Scholar

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© Springer-Verlag Berlin Heidelberg 2005

Authors and Affiliations

  • Hargita Hegyesi
  • Zsuzsa Darvas
  • Robin L. Thurmond
  • András Falus

There are no affiliations available

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