These proceedings cover the most recent advances on histamine research from basic science to clinical medicine. Histamine is an endogenous compound that is synthesized, stored, and released primarily by mast cells and after release exerts profound effects on many tissues and organs. It is one of the cellular mediators of the immediate hypersensitivity reaction and the acute inflammatory responses, as well as primary stimulant of gastric acid secretion. A central neurotransmitter role for histamine has been also established. Histamine research has been very dynamic since it discovery in 1910. Among recent important advances are:: Generation of Histamine H1, H2, H3 receptors and histidine decraboxylase (HDC) knockout mice; Clarification of the constitutive activity of the H1, H2 and H3 receptors; Characterisation of H3 receptor isoforms with distinct signaling properties; and Characterisation and cloning of the H4 receptor.
Regulation of mast cell differentiation (Y. Kitamura et al.). The histamine H3 receptor: gene organization, mutiple isoforms, constitutive activity and molecular pharmacology (J.-M. Arrang et al.).
CNS overviews.
The discovery of potent non-imidazole H3-receptor histamine antagonists (C.R. Ganellin et al.). Histaminergic and cholinergic transmission in cognitive processes (A. Philipu, H. Prast, M.M. Kraus). Physiology and pharmacology of histaminergic neurons (H.L. Haas et al.). Histaminergic modulation of basal forebrain cholinergic neurons (M.B. Passani et al.). The interaction between the histaminergic system and the NO-cGMP pathway: A functional neuroanatomical study in the mammillary region and cerebral cortex of the rat (H.W.M. Steinbusch et al.).
The Histamine H3 receptor and its ligands: from gene to clininc.
Molecular identification of the human and rat histamine H3- receptors: New pharmacological and functional insight (T.W. Lovenberg et al.). Clonining functional characterisation and CNS expression of H3 receptor isoforms (R. Leurs et al.). Partial agonists for the histamine H3 receptor with high in vivo activity (W. Schunack et al.). Structure-activity relationship of histamine H3-ligands: Organic synthesis imidazole C-nucleoside derivatives (S. Harusawa et al.).
Histamine H1 antagonists.
Role of protein kinase C-á in signalling from the histamine H1-receptor to the c-fos promoter (S.J. Hill, A.C. Megson, E.M. Walker). Molecular basis for the cardiovascular adverse effects of first- and second-generation antihistamines (M. Taglialatela et al.). The skin reactivity to histamine: The traps of the investigation (J.-P. Rihoux, A. Campbell).
Safety and efficiency of histamine H1 antagonists.
Efficacy and safety of H1-receptor antagonists in the treatment of allergic disorders: an overview (F. Estelle, R. Simons). Histaminergic neurons and sleep-wake regulation (J.S. Lin, G. Vanni-Mersier, R. Parmentier). Brain penetration of ebastine evaluated in human by positron emission tomography PET (M. Tagawa et al.).
Signal transduction.
Pathways of histamine H1receptor-induced Ca2+ entry in an human astrocytoma cells (M.M.-P. Wong, J.M. Young). Qualitative structure activity relationship for inverse agonism of histamine H2 receptor (A.E. Alewijnse et al.). Constitutive signalling of the human histamine H1 receptor (R.A. Bakker et al.). H1-Histamine receptor communicates to G14 with a relatively higher affinity than to G11 (N. Nakahata et al.). Pathological significance of over-production of histamine and altered transcriptional regulation of H1- and H2- receptors during septic shock (N.Matsuda et al.). Histamine receptors in the chick cerebral cortex: effects on cyclic AMP formation and characterization by radioreceptor binding (J.B. Zawilska, A. Wolan-Tambor, J.Zwak). Histaminergic effect on apoptosis of small intestinal mucosa after ischemia-reperfusion in the rat (K. Fujimoto et al.).
Hypothalamus and histamine neurons.
Changes in circadian rhythmicity and melatonin balance in rats with portacaval anastomosis (PCA)-relation with histamine (L. Tuomisto et al.). Histamine is a transmitter to maintain tonic firing of mesopontine tegmental cholinergic neurons during wakefulness (Y. Koyama, K. Tkahashi, Y. Kayama). Effects of leptin on feeding in histamine H1-receptor knockout mice (T. Masaki et al.). Chronic histamine treatment improves impaired energy intake and hyperinsulinia in diet-induced obese mice (H. Yoshimatsu et al.). Neurotransmitter inputs to the tuberomammillary neurons (K.S. Eriksson et al.). The difference of leptin-histamine signaling in the hypothalamus of obese animal models (H. Yoshimatsu et al.). A possible involvement of the chorda tympani in the enhancement of the hypothalamic histamine release by leptin (T. Morimoto-Ishizuka et al.).
H2 receptors and diseases.
Functional and morphological abnormality of gastric mucosa in histamine H2 receptor (H2R)- deficientm mice (T. Watanabe et al.).
New perspectives for histamine-mediated CNS functions.
A third legacy for burimamide: Discovery and characterization of improgan and a new class of non-opioid analgesics derived from histamine antagonist (L.B. Hough et al.). Involvement of central histamine in amygdaloid kindled seizures in rats (C. Kamei). The role of histamine in a hypocretin orexin-deficient sleep disorder, narcolepsy (S. Nishino at al.). Central histamine and behavioral respiration (I. Homma et al.). Peripheral neuronal histamine down regulates sympathetic activity and arterial pressure (H. Campos). Changes in brain histamine H1 reseptors in chronic hepatic encephalopathy (V. Lozeva et al.). Activation of central histminergic system induced by histamine H3-receptor antagonists on anxiety and learning in mice (K. Onodera et al.).
Mast cells, ECL cells and others.
Role of Histamine and mast cells in metabolic encephalopathy (P.J. Langlais). Mast cell degranulation in the rat small intestine: role of endothelin-A receptors (M. Boros, L. Szalay, J. Kaszaki) Altered response of (isolated) placental vessels to histamine in diabetes complicated pregnancy (D. Szukiewicz et al.). Gastric submucosal microdialysis: A method to monitor ECL-cell histamine mobilization from rat stomach (M. Kitano et al.). The interaction between histamine H3receptors and dopamine D1 receptors in the regulation of [3H]-ă-aminobutyric acid relaese in rat striatum (J.-A. Arias-Montano et al.). Immunohistochemical localization of histamine N-methyltransferase in the bovine central nervous system (M. Nishibori et al.).
Histidine decarboxylase.
Histidine decarboxylase activity in hematopoietic progenitors as a marker for basophil potentiality. Evidence for the existance of a common progenitor for megakaryocytes and basophils (M. Dy et al.). Endogenous histamine and allergic eosinophol infiltration into the airways (A. Korai et al.). Role of histamine in gastric acid secrection: L-hisidine decarboxylase deficient mice (S. Tanaka et al.).
Histamine and allergic disease.
Histamine as a mediator of allergic airway disease (S. Holgate). Histamine and skin allergic diseases (T. Koga, F. Kohda, M. Furue). Effects of a selective H1-receptor antagonist, epinastine, on airway inflammation in asthmatics (K. Kimura et al.).
Mast cells and inflammation.
Suppression of MAP kinase pathways in mast cells by glucocorticolds; mechanisms and consequences (M.A. Beaven, D.S. Cissel, T.R. Hundley). Antiasthmatic Indonesian Medicinal plants: Their tracheospasmolytic activity against histamine induced contractions (S. Wahyuono et al.). Mast cells in rhinitis (R. Pawankar et al.).
Poster Sessions.
Molecular biology and application.
Characterization of splicing variants of histamine H3 receptor (K. Tanaka et al.). Molecular cloning and characterization of a new subtype histamine receptor, H4 (T. Nakamura et al.). Genomic structure of histamine N-methyl-transferase in mammals (M. Takemura et al.). In situ hybridization analysis of gene expression of histamine H1 receptor in murine dorsal root and trigeminal ganglia (M. Itoh et al.). L-Histamine decarboxylase protein and activity in rat brain microvascular endothelial cells (E. Sakurai et al.).
Allergy, inflammation and immunology.
Participation of histamine H1 and H2 receptors in the induction of scratching behavior of ICR mice caused by IgE-mediated passive cutaneous anaphylaxis (N. Inagaki et al.). Immediate-type allergic reaction and helper T cell fuction in histamine H1 receptor- and H2 receptor-deficient mice (T. Kobayashi et al.). IL-18 production induced by histamine in human PBMCs through H2 receptor stimulation (H. Kohka et al.). Regulatory mechanism of eosinophil peroxidase release from guinea pig eosinophils (Y. Kirino, M. Mio, C. Kamei). Induction of VEGF expression by histamine in the granulation tissue in rats (A.K. Ghosh, N. Hirasawa, K. Ohuchi). Induction of histidine decarboxylase in the neointimal smooth muscle cells of balloon-injured porcine coronary arteries (Y.-Il. Fang et al.). Localization of histamine N-methyltransferase in guinea pig tissues: an immunohistochemical study (A. Tahara et al.).
Signal transduction.
Agonist-mediated regulation of histamine H1 receptors and Ca2+ signaling: Ca2+/calmodulin-mediated regulation of receptor function and distribution (S. Hishinuma). Involvement of protein kinase C in regulation of histamine H1 receptor expression in U373 astrocytoma cells (R. Ishikawa et al.). Glucose overload attenuates histamine H2 receptor-mediated Ca2+ mobilization due to protein kinase C production in bovine cerebral endothelial cells (M. Oike, C. Kimura, Y. Ito). Studies of histamine H1 receptor down-regulation using mutant receptors lacking putative phosphorylation sites (M. Ogawa et al.). Mechanism underlying histamine-induced desensitization of amylase secretion in rat parotid glands (H. Ishida et al.). Regulation of histidine decarboxylase protein expression in macrophages: Involvement of MAP kinases and inhibition by dexamethasone (A. Murakami et al.).
Mast cells.
Functional maturation of mouse cultured mast cells to a connective tissue mast cell-like phenotype in vitro (Y. Taketomi et et.). Functional differences between the connective tissue and mucosal mast cells on the contraction of isolated rat trachea (Z. Ikawati et al.). Rho GTPases regulate degranulation and cytokine release from RBL-2H3 cells (I. Hide et al.). Effect of lipid peroxide on histamine release from rat peritoneal mast cells (M. Akagi et al.). Effects of ultraviolet light UV on histamine release from rat peritoneal mast cells (M. Mio et al.). Placental mast cells and histamine in pregnancy complicated by intrauterine growth retardation (IUGR): relation to the development of villous microvessels (D. Szukiewicz et al.). Involvement of mast cells in inflammation sites of colitis induced by dextran sulfate sodium (Y. Iba, Y. Sugimoto, C. Kamei). Development of histamine sensor using recombinant histamine oxidase (S. Iwaki et al.).
H3 receptors and ligands.
Histamine H3 receptor mRNA expression in adult rat brain: cloning of receptor isoforms with differential expression patterns (K.Karlstedt et al.). Histamine H3 receptor-mediated regulation of glutamatergic synaptic transmission in the hippocampus and striatum (R.E. Brown et al.). Peripherally administered ciproxifan elevates hypothalamic histamine levels and potently reduces food intake in the Sprague Dawley rat (C. Bjenning et al.). Peripherally administered histamine H3 antagonist potently reduces snacking behavior in the obes Zucker rat (C. Bjenning, W. Liu, K. Rimvall). Auditory evoked potentials in rats: Effects of anticonvulsants and thioperamide (S. Lensu et al.). Histamine H3-receptor activation modulates glutamate release from rat striatal synaptosomes (A. Molina-Hernandez, A. Nunez, J.-A. Aria-Montano).
CNS-1.
Mechanism for the inhibition of amygdaloid kindled seizures induced by histamine in rats (C. Okuma, T. Hirai, C. Kamei). The role of endogenous histamine in learning and memory in rats (C. Kamei, Y. Sugimoto, Z. Chen) Effects of immunosuppressive drugs on food and kaolin intakes, and hypothalamic histamine turnover in rats (R. Oishi et al.). Glucagon-like peptide 1 modulates histaminergic action in the central regulation of food intake in rats (Y. Kuros et al.). Histamine-induced itch-scratch response and cutaneous nerve firing in mice: comparison with serotonin (H. Nojima, T. Maekawa, Y. Kuraishi). Intrathecal histamine elicites a scratching, biting and licking behavior in mice (T. Orita et al.). The role of brain histamine in visceral pain and emotion: Analysis through functional neuroimaging in human barins (M. Kano et al.).
CNS-2.
Involvement of histamine receptors in p-hydroxyamphetamine-induced head-twitch behavior (T. Tadano et al.). The role of histaminergic neuron system in the methamphetamine induced behavioral sensitization: A study using histamine related gene knockout mice (Y. Kubota et al.). Brain histamine as protective system for the formation of neural sensitization (C. Ito, M. Sato, T. Watanabe). The changes of histamine concentrations in the plasma and brain in response to acute stress (Z.-B. Yang et al.). Anti-stress effects of chicken essence in food-deprived activity stress: Possible involvement of histaminergic neurons (Z.-B. Yang et al.). Decreased histamine H1 receptors in the rat brain subjected to food-deprived activity stress (M. Endou et al.). Central histamine influences respiration in the POA/AH (M. Iwase et al.). Central histamine is a contributory factor in temperature-induced polypnea in conscious mice (M. Izumizaki et al.). Histamine release in the medulla oblongata influences tracheal tone and blood pressure (M. Kanamaru, M. Iwase, I. Homma). The effects of histamine receptor antagonists on the induction of metallothionein mRNA after lipopolysaccharide injection in the mouse spleen (N. Sogawa et al.).
CNS-3.
Evidence for the presence of histamine reuptake system in the brain and its characterization (E. Sakurai et al.). The effects of sleepiness on the brain activity during spatial cognition tasks: A human PET study (H. Mochizuki et al.).
Index of authors
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