HRH3

Summary

Gene Symbol: HRH3
Description: histamine receptor H3
Alias: GPCR97, HH3R, histamine H3 receptor, G protein-coupled receptor 97, H3R
Species: human

Top Publications

  1. ncbi Autoinhibition of histamine synthesis mediated by presynaptic H3-receptors
    J M Arrang
    Unite 109 de Neurobiologie et Pharmacologie, Centre Paul Broca de l INSERM, Paris, France
    Neuroscience 23:149-57. 1987
  2. ncbi Histamine H1 and H2 receptor antagonists accelerate skin barrier repair and prevent epidermal hyperplasia induced by barrier disruption in a dry environment
    Y Ashida
    Skin Biology Research Laboratories, Life Science Research Center, Shiseido Research Center, 2 12 1 Fukuura, Kanazawa Ku, Yokohama 236 8643, Japan
    J Invest Dermatol 116:261-5. 2001
  3. ncbi Molecular cloning and pharmacology of functionally distinct isoforms of the human histamine H(3) receptor
    P Wellendorph
    ACADIA Pharmaceuticals Inc, San Diego, CA 92121, USA
    Neuropharmacology 42:929-40. 2002
  4. ncbi Influence of a selective histamine H3 receptor antagonist on hypothalamic neural activity, food intake and body weight
    K Malmlof
    Department of Pharmacology Research, Novo Nordisk A S, Måløv, Denmark
    Int J Obes (Lond) 29:1402-12. 2005
  5. ncbi Cloning and functional expression of the human histamine H3 receptor
    T W Lovenberg
    R W Johnson Pharmaceutical Research Institute, San Diego, California, USA
    Mol Pharmacol 55:1101-7. 1999
  6. doi A pharmacogenetic study of risperidone on histamine H3 receptor gene (HRH3) in Chinese Han schizophrenia patients
    Zhiyun Wei
    Bio X Institutes, Key Laboratory for the Genetics of Developmental and Neuropsychiatric Disorders, Ministry of Education, Shanghai Jiao Tong University, Shanghai, China
    J Psychopharmacol 26:813-8. 2012
  7. pmc The gastric H3 receptor: a review
    M J Lewin
    INSERM, , Paris, France
    Yale J Biol Med 65:607-11; discussion 621-3. 1992
  8. ncbi Role of capsaicin-sensitive nerves and histamine H1, H2, and H3 receptors in the gastroprotective effect of histamine against stress ulcers in rats
    Artur Dembinski
    Department of Physiology, Jagiellonian University Medical School, 16 Grzegorzecka Street, Krakow 31 531, Poland
    Eur J Pharmacol 508:211-21. 2005
  9. pmc Characterization of the binding of the first selective radiolabelled histamine H3-receptor antagonist, [125I]-iodophenpropit, to rat brain
    F P Jansen
    Leiden Amsterdam Center for Drug Research, Department of Pharmacochemistry, Faculty of Chemistry, Vrije Universiteit, The Netherlands
    Br J Pharmacol 113:355-62. 1994
  10. pmc Plasticity of histamine H3 receptor expression and binding in the vestibular nuclei after labyrinthectomy in rat
    Adrian F Lozada
    Department of Biology, Abo Akademi University, BioCity, Artillerigatan 6A, FIN 20520 Turku, Finland
    BMC Neurosci 5:32. 2004

Research Grants

  1. Histamine Receptor Norepinephrine in Cardiac Dysfunction
    Roberto Levi; Fiscal Year: 2013
  2. DANIEL DEXTER SAVAGE; Fiscal Year: 2015
  3. Development of Cyclopropyl Metal Carbene Based Methods for Organic Synthesis
    Weiping Tang; Fiscal Year: 2013
  4. Susceptibilty and Resistance Loci in Mouse EAE
    Cory Teuscher; Fiscal Year: 2008
  5. IMMUNOREGULATORY LOCI IN ORGAN SPECIFIC AUTOIMMUNITY
    Cory Teuscher; Fiscal Year: 2001
  6. Voltammetric analysis of striatal dopamine dynamics
    Fu Ming Zhou; Fiscal Year: 2006
  7. Androgens and apoE4 induced cognitive impairments
    Jacob Raber; Fiscal Year: 2005
  8. Genetics of Suscptibility to Anthrax Toxin in vivo
    Cory Teuscher; Fiscal Year: 2008
  9. AUTOIMMUNE DISEASE AND NEONATAL TOLERANCE
    Cory Teuscher; Fiscal Year: 2009
  10. Ang II and Norepinephrine in Cardiac Sympathetic Nerves
    Roberto Levi; Fiscal Year: 2009

Detail Information

Publications189 found, 100 shown here

  1. ncbi Autoinhibition of histamine synthesis mediated by presynaptic H3-receptors
    J M Arrang
    Unite 109 de Neurobiologie et Pharmacologie, Centre Paul Broca de l INSERM, Paris, France
    Neuroscience 23:149-57. 1987
    ..A relationship between the two regulatory processes, possibly via intracellular calcium, seems likely but remains to be investigated at the molecular level...
  2. ncbi Histamine H1 and H2 receptor antagonists accelerate skin barrier repair and prevent epidermal hyperplasia induced by barrier disruption in a dry environment
    Y Ashida
    Skin Biology Research Laboratories, Life Science Research Center, Shiseido Research Center, 2 12 1 Fukuura, Kanazawa Ku, Yokohama 236 8643, Japan
    J Invest Dermatol 116:261-5. 2001
    ..The histamine H1 receptor antagonists diphenhydramine and tripelennamine accelerated the recovery. Histamine H3 receptor agonist Nalpha-methylhistamine and antagonist thioperamide had no effect...
  3. ncbi Molecular cloning and pharmacology of functionally distinct isoforms of the human histamine H(3) receptor
    P Wellendorph
    ACADIA Pharmaceuticals Inc, San Diego, CA 92121, USA
    Neuropharmacology 42:929-40. 2002
    ....
  4. ncbi Influence of a selective histamine H3 receptor antagonist on hypothalamic neural activity, food intake and body weight
    K Malmlof
    Department of Pharmacology Research, Novo Nordisk A S, Måløv, Denmark
    Int J Obes (Lond) 29:1402-12. 2005
    This study was conducted to elucidate whether antagonistic targeting of the histamine H3 receptor increases hypothalamic histamine levels, in parallel with decreases in food intake and body weight.
  5. ncbi Cloning and functional expression of the human histamine H3 receptor
    T W Lovenberg
    R W Johnson Pharmaceutical Research Institute, San Diego, California, USA
    Mol Pharmacol 55:1101-7. 1999
    ..The existence of the histamine H3 receptor was demonstrated pharmacologically 15 years ago, yet despite intensive efforts, its molecular identity has ..
  6. doi A pharmacogenetic study of risperidone on histamine H3 receptor gene (HRH3) in Chinese Han schizophrenia patients
    Zhiyun Wei
    Bio X Institutes, Key Laboratory for the Genetics of Developmental and Neuropsychiatric Disorders, Ministry of Education, Shanghai Jiao Tong University, Shanghai, China
    J Psychopharmacol 26:813-8. 2012
    Evidence suggests that the human histamine H3 receptor (HRH3) may be involved in the pharmacodynamics of risperidone and influence clinical efficacy...
  7. pmc The gastric H3 receptor: a review
    M J Lewin
    INSERM, , Paris, France
    Yale J Biol Med 65:607-11; discussion 621-3. 1992
    ..vivo and in vitro studies from our laboratory have revealed a line of pharmacological evidence supporting histamine H3 receptor(s) involvement in the control of gastric acid secretion...
  8. ncbi Role of capsaicin-sensitive nerves and histamine H1, H2, and H3 receptors in the gastroprotective effect of histamine against stress ulcers in rats
    Artur Dembinski
    Department of Physiology, Jagiellonian University Medical School, 16 Grzegorzecka Street, Krakow 31 531, Poland
    Eur J Pharmacol 508:211-21. 2005
    ..antagonist pyrilamine (100 micromol/kg), histamine H2 receptor antagonist ranitidine (100 micromol/kg), histamine H3 receptor antagonist thioperamide (100 micromol/kg), or a combination of histamine with these histamine receptor ..
  9. pmc Characterization of the binding of the first selective radiolabelled histamine H3-receptor antagonist, [125I]-iodophenpropit, to rat brain
    F P Jansen
    Leiden Amsterdam Center for Drug Research, Department of Pharmacochemistry, Faculty of Chemistry, Vrije Universiteit, The Netherlands
    Br J Pharmacol 113:355-62. 1994
    ..Histamine H3-receptor binding; radiolabelled H3-receptor antagonist; [125I]-iodophenpropit; rat cerebral cortex membranes; high affinity; guanine nucleotide shift; G-protein; autoradiography; distribution, histamine H3-receptor subtypes..
  10. pmc Plasticity of histamine H3 receptor expression and binding in the vestibular nuclei after labyrinthectomy in rat
    Adrian F Lozada
    Department of Biology, Abo Akademi University, BioCity, Artillerigatan 6A, FIN 20520 Turku, Finland
    BMC Neurosci 5:32. 2004
    ..Evidence suggesting that the histamine H3 receptor plays a key role in vestibular compensation comes from studies indicating that betahistine, a histamine-..
  11. doi Acute central administration of immepip, a histamine H3 receptor agonist, suppresses hypothalamic histamine release and elicits feeding behavior in rats
    Seiichi Chiba
    Department of Internal Medicine I, School of Medicine, Oita University, 1 1 Idaigaoka, Hasama, Oita 879 5593, Japan
    Brain Res Bull 79:37-40. 2009
    ..These results suggest that i3v administration of immepip, an H3 receptor agonist, suppresses hypothalamic histamine release and elicits feeding behavior in rats...
  12. pmc Effects of L-histidine depletion and L-tyrosine/L-phenylalanine depletion on sensory and motor processes in healthy volunteers
    P van Ruitenbeek
    Department of Neuropsychology and Psychopharmacology, Faculty of Psychology and Neuroscience, Maastricht University, Maastricht, The Netherlands
    Br J Pharmacol 157:92-103. 2009
    ..Here we evaluated whether depletion of L-histidine, the precursor of histamine, was effective in altering measures associated with histamine in humans and the behavioural and electrophysiological (event-related-potentials) effects...
  13. ncbi Activation of histamine H3 receptors in human nasal mucosa inhibits sympathetic vasoconstriction
    LoriAnn M Varty
    Allergy, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033 1300, USA
    Eur J Pharmacol 484:83-9. 2004
    The peripheral histamine H3 receptor is a presynaptic heterologous receptor located on postganglionic sympathetic nerve fibers innervating sympathetic effector systems such as blood vessels and the heart...
  14. ncbi G protein-dependent pharmacology of histamine H3 receptor ligands: evidence for heterogeneous active state receptor conformations
    Kathleen M Krueger
    Neurosciences Research, Abbott Laboratories, Global Pharmaceutical Research and Development, Abbott Park, IL 60064 6125, USA
    J Pharmacol Exp Ther 314:271-81. 2005
    Previously reported pharmacological studies using the imidazole-containing histamine H3 receptor ligands GT-2331 (Cipralisant) and proxyfan resulted in a range of classifications (antagonist, agonist, and protean) for these compounds...
  15. ncbi Role of the histamine system in nefopam-induced antinociception in mice
    Philippe Girard
    Laboratoires Biocodex, Service de Pharmacologie, Zac de Mercières 60200 Compiègne, France
    Eur J Pharmacol 503:63-9. 2004
    ..The histamine H3 receptor agonist R(-)alpha-methylhistamine (RAMH, 10 mg/kg) did not significantly modify the nefopam analgesic ..
  16. ncbi Investigation into the role of histamine receptors in rodent antinociception
    C Lamberti
    Department of Preclinical and Clinical Pharmacology, University of Florence, Firenze, Italy
    Pharmacol Biochem Behav 53:567-74. 1996
    ..It is suggested that the histaminergic system modulates nociception via activation of the H2-receptor...
  17. ncbi In vivo modulation of rat hypothalamic histamine release by the histamine H3 receptor ligands, immepip and clobenpropit. Effects of intrahypothalamic and peripheral application
    F P Jansen
    Leiden Amsterdam Center for Drug Research, Department of Pharmacochemistry, Faculty of Chemistry, Vrije Universiteit, Amsterdam, Netherlands
    Eur J Pharmacol 362:149-55. 1998
    We investigated the effect of the new potent and selective histamine H3 receptor agonist, immepip, and the histamine H3 receptor antagonist, clobenpropit, on in vivo neuronal histamine release from the anterior hypothalamic area of ..
  18. ncbi Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist
    Timothy A Esbenshade
    Abbott Laboratories, Global Pharmaceutical Research Division, Department of Neuroscience Research, Abbott Park, IL 60064, USA
    Biochem Pharmacol 68:933-45. 2004
    ..Thus, A-349821 is a novel, selective non-imidazole H3 antagonist/inverse agonist with balanced high potency across species and favorable cognition enhancing effects in rats...
  19. ncbi Temporal changes in gene expression in the arcuate nucleus precede seasonal responses in adiposity and reproduction
    Alexander W Ross
    Rowett Research Institute, Greenburn Road, Bucksburn, Aberdeen AB21 9SB, Scotland, United Kingdom
    Endocrinology 146:1940-7. 2005
    ..Genes encoding nuclear receptors (RXR/RAR), retinoid binding proteins (CRBP1 and CRABP2), and histamine H3 receptor were photoperiodically regulated with significantly lower expression in SD, whereas VGF mRNA expression ..
  20. ncbi Opposite functions of histamine H1 and H2 receptors and H3 receptor in substantia nigra pars reticulata
    Fu Wen Zhou
    Department of Pharmacology, University of Tennessee College of Medicine, Memphis, TN 38163, USA
    J Neurophysiol 96:1581-91. 2006
    ..In Parkinson's disease, histamine innervation and histamine H3 receptor expression in SNr may be increased...
  21. pmc Production by R-alpha-methylhistamine of a histamine H3 receptor-mediated decrease in basal vascular resistance in guinea-pigs
    R L McLeod
    Department of Pharmacology and Toxicology, New Jersey Medical School UMDNJ, Newark
    Br J Pharmacol 110:553-8. 1993
    1. The effect of the selective histamine H3 receptor agonist, R-alpha-methylhistamine given intravenously (10-100 micrograms kg-1) was examined on baseline total peripheral resistance (TPR), and cardiovascular haemodynamics in ..
  22. pmc Histamine H3-receptor agonists and imidazole-based H3-receptor antagonists can be thermodynamically discriminated
    E A Harper
    James Black Foundation, Dulwich, London, UK
    Br J Pharmacol 151:504-17. 2007
    ..Studies suggest that measurement of thermodynamic parameters can allow discrimination of agonists and antagonists. Here we investigate whether agonists and antagonists can be thermodynamically discriminated at histamine H(3) receptors...
  23. doi 4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists
    Maikel Wijtmans
    Leiden Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Faculty of Exact Sciences, VU University Amsterdam, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands
    J Med Chem 51:2944-53. 2008
    Research on the therapeutic applications of the histamine H3 receptor (H3R) has traditionally focused on antagonists/inverse agonists...
  24. pmc Histamine H3-receptor-mediated [35S]GTP gamma[S] binding: evidence for constitutive activity of the recombinant and native rat and human H3 receptors
    A Rouleau
    Unité de Neurobiologie et Pharmacologie Moléculaire U 109 de l INSERM, Centre Paul Broca, 2ter rue d Alesia, 75014 Paris, France
    Br J Pharmacol 135:383-92. 2002
    ....
  25. ncbi The histaminergic, but not the serotoninergic, system mediates amylin's anorectic effect
    T A Lutz
    Institute of Veterinary Physiology, University of Zuerich, Switzerland
    Peptides 17:1317-22. 1996
    ..Pretreatment of rats with the histamine H3 receptor agonists R-alpha-methylhistamine (MH: 3 mg/kg, IP) and Imerit (3 mg/kg, IP), which block transmission in ..
  26. ncbi Lack of cataleptogenic potentiation with non-imidazole H3 receptor antagonists reveals potential drug-drug interactions between imidazole-based H3 receptor antagonists and antipsychotic drugs
    Min Zhang
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, AP9A, R4N5, 100 Abbott Park, Abbott Park, IL 60064 6115, USA
    Brain Res 1045:142-9. 2005
    Since H3 receptor (H3R) antagonists/inverse agonists can improve cognitive function in animal models, they may have the potential to be used as add-on therapy in the treatment of schizophrenia, a disease with significant cognitive ..
  27. ncbi Histamine H3 receptor agonist- and antagonist-evoked vacuous chewing movements in 6-OHDA-lesioned rats occurs in an absence of change in microdialysate dopamine levels
    Przemysław Nowak
    Department of Pharmacology, Medical University of Silesia, H Jordana 38, 41 808 Zabrze, Poland
    Eur J Pharmacol 552:46-54. 2006
    ..On the basis of the present study, we believe that histaminergic systems may augment dyskinesias induced by dopamine receptor agonists, independent of direct actions on dopaminergic neurons...
  28. pmc Histamine H3-receptor signaling in cardiac sympathetic nerves: Identification of a novel MAPK-PLA2-COX-PGE2-EP3R pathway
    Roberto Levi
    Department of Pharmacology, Weill Medical College of Cornell University, New York, NY 10021, USA
    Biochem Pharmacol 73:1146-56. 2007
    ..Accordingly, this novel H(3)R signaling pathway may ultimately bear therapeutic significance in hyper-adrenergic states...
  29. doi Anxiolytic-like profiles of histamine H3 receptor agonists in animal models of anxiety: a comparative study with antidepressants and benzodiazepine anxiolytic
    Fumikazu Yokoyama
    Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd, 760 Morooka cho, Kohoku Ku, Yokohama 222 8567, Japan
    Psychopharmacology (Berl) 205:177-87. 2009
    b>Histamine H3 receptor functions as a presynaptic auto- and hetero-receptor on histaminergic and non-histaminergic neurons in the brain regulating the synaptic release of numerous neurotransmitters...
  30. ncbi Inhibition of electrically evoked contractions of guinea-pig ileum preparations mediated by the histamine H3 receptor
    G J Menkveld
    Department of Pharmacochemistry, Faculty of Chemistry, Vrije Universiteit, Amsterdam, The Netherlands
    Eur J Pharmacol 186:343-7. 1990
    ..2; thioperamide, 8.5). Our results indicate that H3-receptors are present on both cholinergic and NANC nerves in the myenteric plexus and that the preparation can be used as a rapid and simple test system for histamine H3-receptors...
  31. ncbi Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties
    Timothy A Esbenshade
    Neuroscience Research, Abbott Laboratories, R4MN, AP9A, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    J Pharmacol Exp Ther 313:165-75. 2005
    b>Histamine H3 receptor antagonists are being developed to treat a variety of neurological and cognitive disorders that may be ameliorated by enhancement of central neurotransmitter release...
  32. ncbi Pharmacological control of the human gastric histamine H2 receptor by famotidine: comparison with H1, H2 and H3 receptor agonists and antagonists
    C Gespach
    INSERM U 55, Hopital Saint Antoine, Paris, France
    Eur J Clin Invest 19:1-10. 1989
    ..and extend the previous observations that (R) alpha-MeHA and thioperamide are two selective ligands at histamine H3 receptor sites...
  33. ncbi [New therapeutic alternatives in migraine prophylaxis using histamine H3 receptor agonists]
    Rebeca O Millan-Guerrero
    Unidad de Investigacion en Epidemiologia Clinica, Hospital General de Zona 1, Instituto Mexicano del Seguro Social, Colima, Col
    Gac Med Mex 144:291-5. 2008
    ..Subcutaneous histamine at low concentrations interacts with H3-receptors and may constitute a new therapeutic drug in migraine prophylaxis. It acts by limiting the excessive inflammatory response involved in migraine pathophysiology...
  34. ncbi Molecular cloning and characterization of a novel type of histamine receptor preferentially expressed in leukocytes
    T Oda
    Helix Research Institute, Inc, 1532 3 Yana, Kisarazu shi, Chiba, 292 0812, Japan
    J Biol Chem 275:36781-6. 2000
    Recently cDNA encoding the histamine H3 receptor was isolated after 15 years of considerable research. However, several studies have proposed heterogeneity of the H3 receptor...
  35. ncbi Waking selective neurons in the posterior hypothalamus and their response to histamine H3-receptor ligands: an electrophysiological study in freely moving cats
    G Vanni-Mercier
    INSERM U480, Departement de Medecine Experimentale, Universite Claude Bernard, 8, avenue Rockefeller, 69373 Lyon Cedex 08, France
    Behav Brain Res 144:227-41. 2003
    ....
  36. ncbi Homologous down-regulation of histamine H3 receptors in rat striatal slices
    Belén Garduño-Torres
    Departamento de Fisiologia, Biofisica y Neurociencias, Centro de Investigacion y de Estudios Avanzados, Apdo Postal 14 740, 07000 Mexico, D F, Mexico
    Synapse 60:165-71. 2006
    ..76% +/- 4% of control values). Taken together our results indicate that agonist binding promotes the down-regulation of striatal H3 receptors resulting in a significant loss of function...
  37. ncbi Histamine H3 receptor ligands break ground in a remarkable plethora of therapeutic areas
    Maikel Wijtmans
    Vrije Universiteit Amsterdam, Leiden Amsterdam Center of Drug Research, Division of Medicinal Chemistry, Faculty of Sciences, De Boelelaan 1083, Amsterdam, The Netherlands
    Expert Opin Investig Drugs 16:967-85. 2007
    ..Considering the tremendous efforts by industry, it can be expected that the first H(3)R drugs will reach the market soon...
  38. ncbi Histamine H(3) receptor ligands modulate L-dopa-evoked behavioral responses and L-dopa derived extracellular dopamine in dopamine-denervated rat striatum
    Przemyslaw Nowak
    Department of Pharmacology, Medical University of Silesia, 41 808 Zabrze, Poland
    Neurotox Res 13:231-40. 2008
    ..Furthermore, evidence from behavioral studies indicate that histamine H3 receptor blockade markedly improved motor coordination...
  39. pmc Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cells
    Jillian G Baker
    Institute of Cell Signalling, Medical School, University of Nottingham, Queen s Medical Centre, Nottingham, NG7 2UH, UK
    BMC Pharmacol 8:9. 2008
    ....
  40. doi Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics
    Y von Coburg
    Johann Wolfgang Goethe Universitat, Institut fur Pharmazeutische Chemie, Biozentrum, ZAFES CMP, Max von Laue Strasse 9, 60438 Frankfurt, Germany
    Bioorg Med Chem Lett 19:538-42. 2009
    b>Histamine H3 receptor (H3R) antagonists have some antipsychotic properties although the clear molecular mechanism is still unknown...
  41. ncbi Histamine receptor-mediated signaling during development and brain function in adulthood
    J Raber
    Departments of Behavioral Neuroscience and Neurology, Division of Neuroscience, ONPRC, Oregon Health and Science University, 3181 S W Sam Jackson Park Road, Portland, OR 97239, USA
    Cell Mol Life Sci 64:735-41. 2007
    ..Our data support this hypothesis. In the developing mouse brain, histamine H3 receptor blockade, which increases histamine release, has detrimental sex-dependent effects on object recognition, ..
  42. ncbi Molecular and pharmacological characterization of the mouse histamine H3 receptor
    Jingcai Chen
    Johnson and Johnson Pharmaceutical Research and Development, 3210 Merryfield Row, San Diego, CA 92121, USA
    Eur J Pharmacol 467:57-65. 2003
    ..Taken together, these findings allow a further appreciation of the histamine H(3) receptor at the molecular level and provide an additional species to assist in the pharmacological assessment of histamine H(3) receptor function...
  43. ncbi A qualitative model for the histamine H3 receptor explaining agonistic and antagonistic activity simultaneously
    I J De Esch
    Department of Pharmacochemistry, Faculty of Chemistry, Vrije Universiteit, Amsterdam, The Netherlands
    Arch Pharm (Weinheim) 333:254-60. 2000
    ....
  44. doi Substance P is involved in the effect of histamine H3 receptor agonist, Sch 50971 on nasal allergic symptoms in mice
    Emiko Yokota
    Department of Medicinal Pharmacology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Tsushima naka 1 1 1, Okayama 700 8530, Japan
    Int Immunopharmacol 8:1083-8. 2008
    The aim of this study was to clarify the mechanisms of the inhibitory effect of a histamine H3 receptor agonist, Sch 50971, on nasal signs in an allergic rhinitis model in mice...
  45. ncbi Heterogeneity of histamine H3 receptor genomic expression in the cerebral cortex of spontaneously hypertensive rat
    J B Shaw
    Department of Biological Sciences, Tennessee State University, Nashville, TN 37209, USA
    Cell Mol Biol (Noisy-le-grand) 53:45-50. 2007
    ....
  46. doi Cloning and characterization of the monkey histamine H3 receptor isoforms
    Marina I Strakhova
    Neuroscience Research, Global Pharmaceutical Research Division, Abbott Laboratories, R 4MN, AP9A, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA
    Eur J Pharmacol 601:8-15. 2008
    ....
  47. pmc Characterization of histamine-H3 receptors controlling non-adrenergic non-cholinergic contractions of the guinea-pig isolated ileum
    S J Taylor
    Department of Neuropharmacology, Glaxo Group Research, Ware, Herts
    Br J Pharmacol 105:667-74. 1992
    ..of the second contraction, with no effect on the initial contraction, were observed after inclusion of the histamine H3 receptor agonists (R)-alpha-methylhistamine (pD2 = 7.6), N alpha-methylhistamine (pD2 = 7...
  48. pmc Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed
    R Leurs
    Department of Pharmacochemistry, Faculty of Chemistry, Vrije Universiteit, Amsterdam, The Netherlands
    Br J Pharmacol 116:2315-21. 1995
    1. In the present study we evaluated the receptor selectivity of the potent histamine H3 receptor antagonist, iodophenpropit (IPP) in comparison with the prototype antagonist, thioperamide. 2...
  49. ncbi Development of trans-2-[1H-imidazol-4-yl] cyclopropane derivatives as new high-affinity histamine H3 receptor ligands
    C E Tedford
    Gliatech Inc, Cleveland, Ohio, USA
    J Pharmacol Exp Ther 289:1160-8. 1999
    ..Several compounds were tested in vitro which suggested HA H3 receptor heterogeneity and are discussed in terms of structure-activity relationships for the HA H3 receptor...
  50. ncbi Cloning and cerebral expression of the guinea pig histamine H3 receptor: evidence for two isoforms
    J Tardivel-Lacombe
    Unité de Neurobiologie et Pharmacologie Moléculaire U 109 INSERM, Centre Paul Broca, Paris, France
    Neuroreport 11:755-9. 2000
    ..g. pyramidal cells in the cerebral cortex or cerebellar Purkinje cells, in some instances already known to express other histamine receptor subtypes...
  51. ncbi The rat H3 receptor: gene organization and multiple isoforms
    S Morisset
    Unité de Neurobiologie et Pharmacologie Moléculaire U109 de L INSERM, Centre Paul Broca, 2 ter rue d Alesia, Paris, 75014, France
    Biochem Biophys Res Commun 280:75-80. 2001
    Genomic DNA analysis revealed that the coding region of the rat histamine H3 receptor comprises three exons interrupted by two introns of approximately 1 kb each...
  52. ncbi Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects
    Timothy A Esbenshade
    Neuroscience Research, Global Pharmaceutical Research Division, Abbott Laboratories, R4MN, AP9A, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    J Pharmacol Exp Ther 305:887-96. 2003
    b>Histamine H3 receptor (H3R) antagonists enhance neurotransmitter release and are being developed for the treatment of a variety of neurological and cognitive disorders...
  53. ncbi Replacement of imidazole by a piperidine moiety differentially affects the potency of histamine H3-receptor antagonists
    Susanna Liedtke
    Institut fur Pharmakologie und Toxikologie, Universitat Bonn, Reuterstrasse 2b, 53113 Bonn, Germany
    Naunyn Schmiedebergs Arch Pharmacol 367:43-50. 2003
    ..The discrepancy between the p K(i) and p A2 values may be accounted for by partial agonism in the case of proxyfan but can, at present, not be satisfactorily explained with respect to FUB 138 and FUB 153...
  54. ncbi Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists
    Ramin Faghih
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park 60064 6123, USA
    Bioorg Med Chem Lett 13:1325-8. 2003
    ..Most compounds were highly potent and selective for human and rat H(3) receptors and selected examples such as A-349821 showed functional antagonism of H(3) receptors in vitro and in a mouse dipsogenia model...
  55. ncbi Genetic and pharmacological aspects of histamine H3 receptor heterogeneity
    Arthur A Hancock
    Neuroscience Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064 6125, USA
    Life Sci 73:3043-72. 2003
    ..The promise of newly available tools to further explore H3 receptor function may provide the insight to bring the promised clinical potential of H3 receptor ligands to realization...
  56. ncbi Comparative cytotoxicity of N-substituted N'-(4-imidazole-ethyl)thiourea in precision-cut rat liver slices
    Rob C A Onderwater
    Leiden Amsterdam Center for Drug Research LACDR, Division of Molecular Toxicology, Vrije Universiteit, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands
    Toxicology 197:81-91. 2004
    ..to more rationally design thiourea-containing drugs and drug candidates, specifically thiourea-containing histamine H3 receptor antagonists, it is necessary to develop structure-toxicity relationships (STRs)...
  57. ncbi Search for histamine H3 receptor antagonists with combined inhibitory potency at Ntau-methyltransferase: ether derivatives
    J Apelt
    Institut fur Pharmazie, Freie Universitat Berlin, Germany
    Pharmazie 60:97-106. 2005
    With the recent development of new hybrid compounds having histamine H3 receptor antagonist with combined histamine Ntau-methyltransferase (HMT) inhibitory potency an innovative approach was described in the research of novel lead ..
  58. ncbi Discovery of histamine H3 receptor antagonistic property of simple imidazole-free derivatives: Preliminary pharmacological investigation
    Elisabetta Barocelli
    Dipartimento di Scienze Farmacologiche, Biologiche e Chimiche Applicate, Universita di Parma, Parco Area delle Scienze 27 A, 43100 Parma, Italy
    Pharmacol Res 53:226-32. 2006
    The histamine H3 receptor subtype negatively modulates the release of various neurotransmitters such as histamine, glutamate, norepinephrine, acetylcholine and many others mainly in the CNS and H3 antagonists have been developed to treat ..
  59. ncbi Histamine receptors influence blood-spinal cord barrier permeability, edema formation, and spinal cord blood flow following trauma to the rat spinal cord
    H S Sharma
    Department of Surgical Sciences, Anesthesiology and Intensive Care, University Hospital, Uppsala University, Uppsala, Sweden
    Acta Neurochir Suppl 96:316-21. 2006
    ..The effects of ranitidine were far superior to cimetidine in identical doses. Pretreatment with a histamine H3 receptor agonist alpha-methylhistamine (1 mg and 2 mg/kg/i.p...
  60. ncbi Synthesis and SAR of novel histamine H3 receptor antagonists
    Cynthia D Jesudason
    Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
    Bioorg Med Chem Lett 16:3415-8. 2006
    ..The substitution around these rings as well as the nature of the substituent on nitrogen is explored. Several compounds with high affinity and selectivity for the human and rat H(3) receptors are reported...
  61. ncbi 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
    Haibin Dai
    Department of Pharmacology, School of Medicine, Zhejiang University, Hangzhou 310058, and Department of Pharmacy, Second Affiliated Hospital, China
    Eur J Pharmacol 563:117-23. 2007
    Using the histamine H3 receptor antagonist clobenpropit, the roles of histamine H3 receptors in NMDA-induced necrosis were investigated in rat cultured cortical neurons...
  62. ncbi Novel heterocyclic-substituted benzofuran histamine H3 receptor antagonists: in vitro properties, drug-likeness, and behavioral activity
    Marlon Cowart
    GPRD_AP9a 216, Department of Neuroscience Research, Abbott Laboratories, Abbott Park, IL 60064 6123, USA
    Biochem Pharmacol 73:1243-55. 2007
    ..v. administration (t(1/2) in rat of 2.9h, 1.7h in dog, 1.8h in monkey), suggesting poor human pharmacokinetics, the data overall indicated that A-688057 has an excellent profile for use as a pharmacological tool compound...
  63. doi Diamine derivatives containing imidazolidinylidene propanedinitrile as a new class of histamine H3 receptor antagonists. Part I
    Setsuya Sasho
    Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co Ltd, 1188, Shimotogari, Nagaizumi cho, Sunto gun, Shizuoka ken, 411 8731, Japan
    Bioorg Med Chem Lett 18:2288-91. 2008
    ..High-affinity ligands 3d, 3k, and 3n showed potent H(3) receptor antagonism and excellent selectivity over human H(1), H(2) and H(4) receptors...
  64. doi Refined docking as a valuable tool for lead optimization: application to histamine H3 receptor antagonists
    Nicolas Levoin
    Bioprojet Biotech, Saint Grégoire, France
    Arch Pharm (Weinheim) 341:610-23. 2008
    ..Third, the database is issued from concrete SAR (Bioprojet H(3) BF2.649 library) and is not simply constituted by few active ligands buried in a chemical catalogue...
  65. doi No evidence for functional selectivity of proxyfan at the human histamine H3 receptor coupled to defined Gi/Go protein heterotrimers
    David Schnell
    Institute for Pharmacology, Medical School of Hannover, Carl Neuberg Str 1, D 30625 Hannover, Germany
    J Pharmacol Exp Ther 332:996-1005. 2010
    ....
  66. doi Benzimidazole- and indole-substituted 1,3'-bipyrrolidine benzamides as histamine H3 receptor antagonists
    Derek C Cole
    Chemical Sciences, Wyeth Research, 401 N Middletown Rd Pearl River, NY 10965, United States
    Bioorg Med Chem Lett 20:1237-40. 2010
    ..Optimization of the physical properties of the series led to (S)-6n, with improved brain to plasma exposure and efficacy in both water intake and novel object recognition models...
  67. doi Modulation of histamine H(3) receptor function by monovalent ions
    David Schnell
    Department of Pharmacology and Toxicology, University of Regensburg, D 93040 Regensburg, Germany
    Neurosci Lett 472:114-8. 2010
    ..NaCl had a stronger effect on basal hH3R-signalling when Galpha(i3) was co-expressed. Asp80(2...
  68. pmc Histamine H3 receptor activation decreases kainate-induced hippocampal gamma oscillations in vitro by action potential desynchronization in pyramidal neurons
    Richard Andersson
    Neuronal Oscillations Laboratory, Department of Neuroscience, Karolinska Institute, SE 17177 Stockholm, Sweden
    J Physiol 588:1241-9. 2010
    ..Our data provide a possible mechanism of action for histamine in regulating gamma oscillations in the hippocampal network...
  69. doi Antinociceptive effects of histamine H3 receptor antagonist in the preclinical models of pain in rats and the involvement of central noradrenergic systems
    Gin C Hsieh
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    Brain Res 1354:74-84. 2010
    ..Our data also provide support that selective H(3) antagonists may represent a class of agents for the treatment of pain disorders...
  70. doi Effects of histamine H3 receptor ligands on the rewarding, stimulant and motor-impairing effects of ethanol in DBA/2J mice
    Saara Nuutinen
    Neuroscience Center, Biomedicum Helsinki, University of Helsinki, P O Box 63, Haartmaninkatu 8, FIN 00014 Helsinki, Finland
    Neuropharmacology 60:1193-9. 2011
    b>Histamine H3 receptor (H3R) antagonists are currently being investigated for the possible therapeutic use in various cognitive deficits such as those in schizophrenia, attention deficit hyperactivity disorder and Alzheimer's disease...
  71. doi The hydrophobic amino acids in putative helix 8 in carboxy-terminus of histamine H(3) receptor are involved in receptor-G-protein coupling
    Atsuo Kuramasu
    Department of Pharmacology, Tohoku University Graduate School of Medicine, Sendai, Miyagi 980 8575, Japan
    Cell Signal 23:1843-9. 2011
    ..Our results suggest that hydrophobic interface of putative helix 8 is important for the regulation of H(3) receptor activity, presumably by stabilizing the helix to the plasma membrane...
  72. ncbi Protective effects of histamine H3-receptor ligands in schizophrenic behaviors in experimental models
    Danish Mahmood
    Department of Pharmacology, Faculty of Pharmacy, Hamdard University, New Delhi 110062, India
    Pharmacol Rep 64:191-204. 2012
    ..Learning and memory deficits, as evaluated on elevated plus maze, followed by estimation of brain AChE activity demonstrated positive results with these protypical imidazole H(3)R-antagonists/inverse agonists...
  73. doi Voltage sensitivities and deactivation kinetics of histamine H₃ and H₄ receptors
    Kristoffer Sahlholm
    Department of Neuroscience, Karolinska Institutet, Stockholm, Sweden
    Biochim Biophys Acta 1818:3081-9. 2012
    ..The differences in voltage sensitivities and deactivation kinetics between the hH(3)(445), hH(3)(365), and H₄ receptors might be relevant to their respective physiological roles...
  74. ncbi Histamine H3 receptor function and ligands: recent developments
    Mahaveer Singh
    Department of Pharmacy, Birla Institute of Technology and Sciences Pilani, Pilani Campus, Vidya Vihar, Pilani, Rajasthan, India
    Mini Rev Med Chem 13:47-57. 2013
    ..Also, it is aimed at collating the information on efforts of various medicinal chemists to synthesize the H3 receptor agonists and antagonists in single article...
  75. pmc Histamine H3 receptor antagonists/inverse agonists on cognitive and motor processes: relevance to Alzheimer's disease, ADHD, schizophrenia, and drug abuse
    Divya Vohora
    Faculty of Pharmacy, Department of Pharmacology, Jamia Hamdard Hamdard University New Delhi, India
    Front Syst Neurosci 6:72. 2012
    b>Histamine H3 receptor (H3R) antagonists/inverse agonists possess potential to treat diverse disease states of the central nervous system (CNS)...
  76. doi Discovery of aryl ureas and aryl amides as potent and selective histamine H3 receptor antagonists for the treatment of obesity (part II)
    Zhongli Gao
    LGCR SMRPD Chemical Research, Sanofi US, 153 1 122, 153 2nd Ave, Waltham, MA 02451, USA
    Bioorg Med Chem Lett 23:3421-6. 2013
    A novel series of histamine H3 receptor (H3R) antagonists was derived from an arylurea lead series (1) via bioisosteric replacement of the urea functionality by an amide linkage...
  77. ncbi [Identification of a HEK-293 cell line containing stably-transfected H3R gene and screening for novel non-imidazole histamine H3 receptor antagonists]
    Ping He
    Department of Pharmacy, The Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou 310009, China
    Zhejiang Da Xue Xue Bao Yi Xue Ban 42:276-82. 2013
    To identify a HEK293 cell line containing stably-transfected H3R gene, and to screen the novel non-imidazole compounds with H3R antagonist activity.
  78. doi Histamine H3 receptor activation prevents dopamine D1 receptor-mediated inhibition of dopamine release in the rat striatum: a microdialysis study
    Alfonso Alfaro-Rodriguez
    Departamento de Neurorrehabilitación, Instituto Nacional de Rehabilitacion, SSA, Mexico
    Neurosci Lett 552:5-9. 2013
    ..5 and 1 μM) significantly reduced DA release (26-58%), and this effect was prevented by co-administration of the H3R agonist immepip (10 μM). In turn, the effect of immepip was blocked by the H3R antagonist thioperamide (10 μM)...
  79. doi Synthesis and SAR studies of benzimidazolone derivatives as histamine H3-receptor antagonists
    Qingbei Zeng
    Merck Research Laboratories, 126 E Lincoln Avenue, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 23:6001-3. 2013
    ..These benzimidazolone analogs demonstrate potent H3-receptor binding affinities, no P450 enzyme inhibition, and strong H3 functional activity. Compound 1o exhibits the best overall profile with H3Ki=0.95nM and rat AUC=12.9μMh. ..
  80. pmc The effect of the sympathetic nervous system on splenic natural killer cell activity in mice administered the Lactobacillus pentosus strain S-PT84
    Takayuki Izumo
    aInstitute for Health Care Science, Suntory Wellness Limited bANBAS Corporation, Osaka, Japan
    Neuroreport 24:988-91. 2013
    ..This phenomenon was inhibited by pretreatment with thioperamide (histamine H3 receptor antagonist), suggesting that S-PT84 directly affected splenic SNA...
  81. pmc Associations of polymorphisms in histidine decarboxylase, histamine N-methyltransferase and histamine receptor H3 genes with breast cancer
    Gong Hao He
    Department of Pharmacy, Kunming General Hospital of Chengdu Military Region, Kunming, Yunnan, China
    PLoS ONE 9:e97728. 2014
    ..histamine-related genes, such as histidine decarboxylase (HDC), histamine N-methyltransferase (HNMT) and histamine H3 receptor (HRH3), remain unexplored...
  82. doi Sodium binding to hH3R and hH 4R--a molecular modeling study
    Hans Joachim Wittmann
    Faculty of Chemistry and Pharmacy, University of Regensburg, Universitätsstraße 31, 93040, Regensburg, Germany
    J Mol Model 20:2394. 2014
    Several aminergic GPCRs, e.g., the human histamine H3-receptor (hH3R) are sensitive to sodium ions...
  83. doi Predicting targets of compounds against neurological diseases using cheminformatic methodology
    Katarina Nikolic
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Institute of Pharmaceutical Chemistry, University of Belgrade, Vojvode Stepe 450, 11000, Belgrade, Serbia
    J Comput Aided Mol Des 29:183-98. 2015
    ..B; acetylcholinesterase and butyrylcholinesterase; or with histamine N-methyltransferase and histamine H3-receptor (H3R)...
  84. doi Safety, tolerability and pharmacokinetics of 2-pyridylacetic acid, a major metabolite of betahistine, in a phase 1 dose escalation study in subjects with ADHD
    Ganesh Moorthy
    University of Cincinnati, Cincinnati, Ohio, USA
    Biopharm Drug Dispos 36:429-39. 2015
    Betahistine, a potent histamine H3 receptor antagonist, is being developed for the treatment of attention deficit hyperactivity disorder (ADHD) that manifests with symptoms such as hyperactivity, impulsivity and inattention...
  85. doi Chlorophenoxy aminoalkyl derivatives as histamine H(3)R ligands and antiseizure agents
    Kamil Kuder
    Jagiellonian University Medical College, Faculty of Pharmacy, Department of Technology and Biotechnology of Drugs, Medyczna 9, 30 688 Krakow, Poland
    Bioorg Med Chem 24:53-72. 2016
    ..derivatives (9-28) was synthesized and evaluated on their binding properties at the human histamine H3 receptor (hH3R). The spacer alkyl chain contained five to seven carbon atoms...
  86. pmc Development of TASP0410457 (TASP457), a novel dihydroquinolinone derivative as a PET radioligand for central histamine H3 receptors
    Kazumi Koga
    Molecular Imaging Center, National Institute of Radiological Sciences, 4 9 1 Anagawa, Inage Ku, Chiba, Chiba, 263 8555, Japan
    EJNMMI Res 6:11. 2016
    b>Histamine H3 receptor (H3R) is a potential therapeutic target of sleep- and cognition-related disorders...
  87. ncbi [Isoforms of the human histamine H3 receptor: Generation, expression in the central nervous system and functional implications]
    Ana Maricela García-Gálvez
    Departamento de Fisiologia, Biofisica y Neurociencias, Centro de Investigación y de Estudios Avanzados Cinvestav, Mexico, D F, Mexico
    Gac Med Mex 152:94-102. 2016
    ..The H3 receptor (H3R) is found exclusively in neuronal cells, where it functions as auto- and hetero-receptor...
  88. pmc Multiple Targeting Approaches on Histamine H3 Receptor Antagonists
    Mohammad A Khanfar
    Stark Lab, Institut fuer Pharmazeutische and Medizinische Chemie, Heinrich Heine Universitaet DuesseldorfDuesseldorf, Germany Faculty of Pharmacy, The University of JordanAmman, Jordan
    Front Neurosci 10:201. 2016
    ..market approval of pitolisant (Wakix®), the interest in clinical applications of novel multifunctional histamine H3 receptor antagonists has clearly increased...
  89. doi Cholinesterase inhibitory activity of chlorophenoxy derivatives-Histamine H3 receptor ligands
    Dorota Łazewska
    Department of Technology and Biotechnology of Drugs, Jagiellonian University Medical College, Medyczna 9, 30 688 Krakow, Poland
    Bioorg Med Chem Lett 26:4140-5. 2016
    ..Combination of both: a histamine H3 receptor antagonist/inverse agonist and a cholinesterases inhibitor in one molecule could provide a new therapeutic ..
  90. doi Cimetidine disrupts the renewal of testicular cells and the steroidogenesis in a hermaphrodite fish
    María García-García
    Sección de Microscopía, Servicio de Apoyo a la Investigación, University of Murcia, Murcia 30100, Spain
    Comp Biochem Physiol C Toxicol Pharmacol 189:44-53. 2016
    ..We report here for the first time that histamine and the mRNA of Hrh1, Hrh2 and Hrh3 are all present in the gonad of the hermaphrodite teleost fish gilthead seabream...
  91. ncbi Ovariectomy Alters Gene Expression of the Hippocampal Formation in Middle-Aged Rats
    Miklós Sárvári
    Laboratory of Endocrine Neurobiology, Institute of Experimental Medicine, Hungarian Academy of Sciences, Budapest, Hungary
    Endocrinology . 2016
    ..Cck, Cckbr, Crhr1 and 2, Oprd1, Nts, Penk, Sstr1, Vip), neurotransmitter signaling (Htr2c, Chrna3, Chrm4, Grm8, Hrh3, Slc17a6) and potassium channels (Kcnk9, Kcnj9, Kcnma1, Kcnc2)...
  92. doi Isoform-Specific Biased Agonism of Histamine H3 Receptor Agonists
    Darren M Riddy
    Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia D M R, A E C, N A D, S B, R B, R J S, W N C, P M S, A C, C J L and Institut de Recherches Internationales Servier, Suresnes, France C M C, E M
    Mol Pharmacol 91:87-99. 2017
    ....
  93. doi Histamine H3R receptor activation in the dorsal striatum triggers stereotypies in a mouse model of tic disorders
    M Rapanelli
    Department of Psychiatry, Yale University, New Haven, CT, USA
    Transl Psychiatry 7:e1013. 2017
    ..We found elevated expression of the histamine H3 receptor in the striatum of Hdc knockout mice...
  94. ncbi A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines
    Richard Apodaca
    Johnson and Johnson Pharmaceutical Research and Development, L L C, 3210 Merryfield Row, San Diego, California 92121, USA
    J Med Chem 46:3938-44. 2003
    ..One member of this series, 1-[4-(3-piperidin-1-ylpropoxy)benzyl]piperidine (7b), was found to be a selective and potent human H(3) receptor antagonist...
  95. ncbi Age-related changes in histamine receptor mRNA levels in the mouse brain
    Akira Terao
    Molecular Neurobiology Laboratory, SRI International, 333 Ravenswood Avenue, Menlo Park, CA 94025, USA
    Neurosci Lett 355:81-4. 2004
    ..mice, significant differences were found in histamine H1 receptor (H1R), histamine H2 receptor (H2R), and histamine H3 receptor (H3R) mRNA levels in several brain regions...
  96. ncbi Histamine h3 receptor antagonists potentiate methamphetamine self-administration and methamphetamine-induced accumbal dopamine release
    Patrik Munzar
    Preclinical Pharmacology Section, Behavioral Neuroscience Research Branch, Intramural Research Program, NIDA, NIH, Department of Health and Human Services, Baltimore, MD 21224, USA
    Neuropsychopharmacology 29:705-17. 2004
    ..The aim of the present study was to evaluate the effects of two histamine H3 receptor antagonists, clobenpropit and thioperamide, on rewarding and neurochemical effects of methamphetamine ..
  97. ncbi Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency
    Minghua Sun
    Neuroscience Research, Global Pharmaceutical Research Division, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064 6123, USA
    J Med Chem 48:6482-90. 2005
    ..The synthesis, SAR of the H3 binding affinities, in vitro assay for phospholipidosis, and pharmacokinetic properties of the new compounds are described...
  98. ncbi [Participation of cyclic nucleotides and phospholipidis in signal transduction of histamin receptor H3 of the gastric mucosa parietal cells in rats with experimental ulcer]
    V O Chaĭka
    Ukr Biokhim Zh 77:118-22. 2005
    ..the work was to evaluate plasma membrane phospholipid composition in rat gastric parietal cells under the histamine H3 receptor activation. The content of cyclic nucleotides was also studied...
  99. ncbi Recent advances in molecular pharmacology of the histamine systems: physiology and pharmacology of histamine H3 receptor: roles in feeding regulation and therapeutic potential for metabolic disorders
    Shigeru Tokita
    Tsukuba Research Institute, Banyu Pharmaceutical Co, Ltd, Ibaraki, Japan
    J Pharmacol Sci 101:12-8. 2006
    ..To further understand the physiological roles of H3Rs in vivo, we produced H3R knockout (H3R-/-) mice and found that H3R-/- mice displayed hyperphagia and late-onset obesity associated with ..
  100. pmc Role of histamine and its receptors in cerebral ischemia
    Wei Wei Hu
    Department of Pharmacology, Key Laboratory of Medical Neurobiology of the Ministry of Health of China, Zhejiang Province Key Laboratory of Neurobiology, School of Basic Medical Sciences, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang 310058, P R China
    ACS Chem Neurosci 3:238-47. 2012
    ..However, important questions about the molecular aspects and pathophysiology of histamine and related agents in cerebral ischemia remain to be answered to form a solid scientific basis for therapeutic application...
  101. doi Virtual fragment screening: discovery of histamine H3 receptor ligands using ligand-based and protein-based molecular fingerprints
    Francesco Sirci
    Laboratory for Chemometrics and Chemoinformatics, Chemistry Department, University of Perugia, Via Elce di Sotto, 10, I 06123 Perugia, Italy
    J Chem Inf Model 52:3308-24. 2012
    ..The first construction and application of customized FLAP models for the discovery of fragment-like biologically active molecules demonstrates that VFS is an efficient way to explore protein-fragment interaction space in silico...

Research Grants11

  1. Histamine Receptor Norepinephrine in Cardiac Dysfunction
    Roberto Levi; Fiscal Year: 2013
    ..selective H3-receptor agonists) mimicking the beneficial effects of preconditioning and enabling a safe and effective treatment of congestive heart failure with natriuretic peptides. and ATP sensory/sympathetic nerves will be assessed ..
  2. DANIEL DEXTER SAVAGE; Fiscal Year: 2015
    ..We have observed that the histamine H3 receptor antagonist ABT-239 ameliorates fetal ethanol-induced deficits in dentate gyrus long-term potentiation (LTP)..
  3. Development of Cyclopropyl Metal Carbene Based Methods for Organic Synthesis
    Weiping Tang; Fiscal Year: 2013
    ..including antibiotics, antiviral agents, antimicrobial agents, analgesics, selective CYP inhibitors, and histamine H3 receptor antagonists...
  4. Susceptibilty and Resistance Loci in Mouse EAE
    Cory Teuscher; Fiscal Year: 2008
    ....
  5. IMMUNOREGULATORY LOCI IN ORGAN SPECIFIC AUTOIMMUNITY
    Cory Teuscher; Fiscal Year: 2001
    ..D2Orch3CT3 recombinant congenic mice to narrow down the support interval encoding the locus to a size amenable to positional cloning (less than 1 cM), and 2) construct a yeast artificial chromosome (YAC) contig encompassing Orch3. ..
  6. Voltammetric analysis of striatal dopamine dynamics
    Fu Ming Zhou; Fiscal Year: 2006
    ..The results will provide important new information about the dynamic nature of the striatal [DA]ext and its regulation by therapeutic agents of neuropsychiatric disorders. ..
  7. Androgens and apoE4 induced cognitive impairments
    Jacob Raber; Fiscal Year: 2005
    ....
  8. Genetics of Suscptibility to Anthrax Toxin in vivo
    Cory Teuscher; Fiscal Year: 2008
    ..abstract_text> ..
  9. AUTOIMMUNE DISEASE AND NEONATAL TOLERANCE
    Cory Teuscher; Fiscal Year: 2009
    ..abstract_text> ..
  10. Ang II and Norepinephrine in Cardiac Sympathetic Nerves
    Roberto Levi; Fiscal Year: 2009
    ..abstract_text> ..
  11. Sex Chromosomes in Fetal Programming and Susceptibility to EAE
    Cory Teuscher; Fiscal Year: 2010
    ....