Genomes and Genes
histamine h1 antagonists
Summary: Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.
Publications178 found, 100 shown here
- A double-blind, randomized, single-dose, crossover comparison of levocetirizine with ebastine, fexofenadine, loratadine, mizolastine, and placebo: suppression of histamine-induced wheal-and-flare response during 24 hours in healthy male subjectsJ Andrew Grant
University of Texas Medical Branch, Galveston77555 1083, USA
Ann Allergy Asthma Immunol 88:190-7. 2002..Levocetirizine is the active enantiomer of cetirizine, a potent drug with little metabolism widely used for allergic rhinitis and urticaria...
- Histamine H1 receptor occupancy and pharmacodynamics of second generation H1-antihistaminesM Gillard
UCB S.A, In Vitro Pharmacology Department, Chemin du Foriest, UCB S.A, 1420, Braine l'Alleud, Belgium
Inflamm Res 54:367-9. 2005....
- Risk of first-generation H(1)-antihistamines: a GA(2)LEN position paperM K Church
Department of Dermatology and Allergy, Charite Universitatsmedizin Berlin, Germany
Allergy 65:459-66. 2010....
- Antihistamines and driving ability: evidence from on-the-road driving studies during normal trafficJoris C Verster
Utrecht Institute for Pharmaceutical Sciences, Department of Psychopharmacology, University of Utrecht, Utrecht, The Netherlands
Ann Allergy Asthma Immunol 92:294-303; quiz 303-5, 355. 2004..All antihistamines are capable of crossing the blood-brain barrier and thus may cause sedation. Most antihistamine users are ambulatory patients and therefore presumably drive a car...
- S100A13 is involved in the regulation of fibroblast growth factor-1 and p40 synaptotagmin-1 release in vitroC Mouta Carreira
Center for Molecular Medicine, Maine Medical Center Research Institute, South Portland, Maine 04106, USA
J Biol Chem 273:22224-31. 1998....
- Antihistamine effects on actual driving performance in a standard test: a summary of Dutch experience, 1989-94J F O'Hanlon
Institute for Human Psychopharmacology, University of Limburg, Maastricht, The Netherlands
Allergy 50:234-42. 1995..One or possibly two of the newer drugs possessed both performance-enhancing and -impairing properties, depending on dose, suggesting two mechanisms of action...
- Allergic rhinitis: evidence for impact on asthmaMike Thomas
Department of General Practice and Primary Care, University of Aberdeen, Foresterhill Health Centre, Westburn Road, Aberdeen AB25 2AY, UK
BMC Pulm Med 6:S4. 2006..This paper reviews the current evidence indicating that comorbid allergic rhinitis may have clinically relevant effects on asthma...
- Clinical pharmacology of H1-antihistamines in the skinF Estelle R Simons
Department of Pediatrics and Child Health, Faculty of Medicine, University of Manitoba, Canada
J Allergy Clin Immunol 110:777-83. 2002..CONCLUSIONS: In skin disorders for which H(1)-antihistamines are recommended, these results support the use of fexofenadine or loratadine, and they indicate the need for reexamination of the use of chlorpheniramine...
- Selective histamine H1 antagonism: novel hypnotic and pharmacologic actions challenge classical notions of antihistaminesStephen M Stahl
Department of Psychiatry, University of California San Diego, La Jolla, CA, USA
CNS Spectr 13:1027-38. 2008..Selective H1 antagonism is emerging as a novel approach to the treatment of insomnia, without tolerance, weight gain, or the need for the restrictive prescription scheduling required of other hypnotics...
- Methapyrilene toxicity: anchorage of pathologic observations to gene expression alterationsHisham K Hamadeh
National Institute of Environmental Health Sciences, Research Triangle Park, North Carolina 27709, USA
Toxicol Pathol 30:470-82. 2002....
- Population pharmacokinetics of epinastine, a histamine H1 receptor antagonist, in adults and childrenA Sarashina
Department of Drug Metabolism and Pharmacokinetics, Kawanishi Pharma Research Institute, Nippon Boehringer Ingelheim Co. Ltd, Kawanishi 666-0193, Japan
Br J Clin Pharmacol 59:43-53. 2005..The model shows that, if dosage is adjusted based on the body weight, the epinastine exposure in paediatric patients is similar to that in adults...
- Antihistamines as analgesicsR B Raffa
Temple University School of Pharmacy, Philadelphia, PA 19140, USA
J Clin Pharm Ther 26:81-5. 2001..However, it is possible that other mechanisms account for the analgesic effect...
- Advances in H1-antihistaminesF Estelle R Simons
Section of Allergy and Clinical Immunology, Department of Pediatrics and Child Health, and the Canadian Institutes of Health Research National Allergy, Faculty of Medicine, University of Manitoba, Winnipeg, Canada
N Engl J Med 351:2203-17. 2004
- Methapyrilene hepatotoxicity is associated with oxidative stress, mitochondrial disfunction and is prevented by the Ca2+ channel blocker verapamilG S Ratra
Department of Toxicology, St Bartholomew s and the Royal London School of Medicine and Dentistry, UK
Toxicology 130:79-93. 1998..Taken together, these data indicate that methapyrilene intoxication leads to mitochondrial disfunction and suggest a critical role for a loss of mitochondrial Ca2+ homeostasis in this model of hepatocyte death...
- Effects of induction and inhibition of cytochromes P450 on the hepatotoxicity of methapyrileneG S Ratra
Department of Toxicology, St Bartholomew s and the Royal London School of Medicine and Dentistry, United Kingdom
Toxicol Sci 46:185-96. 1998..Together this suggested that CYP2C11 was responsible for the suicide substrate bioactivation of methapyrilene and the toxicologic outcome largely relied upon an abundance of detoxifying enzymes present in the liver...
- Effects of mast cell membrane stabilizing agents in a rat lung ischemia-reperfusion modelK M Vural
Department of Cardiothoracic Surgery, College of Physicians and Surgeons, Columbia University, New York, New York, USA
Ann Thorac Surg 69:228-32. 2000....
- Effects of fexofenadine and other antihistamines on components of the allergic response: adhesion moleculesGiorgio Ciprandi
Allergy and Respiratory Diseases, Department of Internal Medicine, University of Genoa, Genoa, Italy
J Allergy Clin Immunol 112:S78-82. 2003....
- Cetirizine, an H1-receptor antagonist, suppresses the expression of macrophage migration inhibitory factor: its potential anti-inflammatory actionT Shimizu
Departments of Dermatology Molecular Biochemistry, Hokkaido University Graduate School of Medicine, Sapporo, Japan
Clin Exp Allergy 34:103-9. 2004....
- Ketotifen abrogates local and systemic consequences of rat intestinal ischemia-reperfusion injuryNeena Kalia
Academic Unit of Surgical Oncology, Division of Clinical Sciences (South, Royal Hallamshire Hospital, Sheffield, UK
J Gastroenterol Hepatol 20:1032-8. 2005..However, its effects are manifested in the absence of any influence on intestinal I/R-induced vascular leakage...
- Potentiation of antimalarial drug action by chlorpheniramine against multidrug-resistant Plasmodium falciparum in vitroSunan Nakornchai
Department of Biochemistry, Faculty of Science, Mahidol University, Rama VI Road, Bangkok 10400, Thailand
Parasitol Int 55:195-9. 2006..falciparum K1 and T9/94. The results in this study indicate that antihistaminic drugs may be promising candidates for potentiating antimalarial drug action against drug resistant malarial parasites...
- Suppressive activity of fexofenadine hydrochloride on metalloproteinase production from nasal fibroblasts in vitroK Asano
Department of Physiology, School of Medicine, Showa University, Tokyo 142 8555, Japan
Clin Exp Allergy 34:1890-8. 2004..Matrix metalloproteinases (MMPs), MMP-2 and MMP-9, are the major proteolytic enzymes that induce airway remodelling. These enzymes are also important in the migration of inflammatory cells through basement membrane components...
- Intranasal steroids and the risk of emergency department visits for asthmaRobert J Adams
Department of Medicine, University of Adelaide, The Queen Elizabeth Hospital Campus, Woodville, Australia
J Allergy Clin Immunol 109:636-42. 2002..These results support the use of intranasal steroids by individuals with asthma and upper airways conditions...
- Suppressive activity of fexofenadine hydrochloride on thymus- and activation-regulated chemokine production from human peripheral blood leukocytes in response to antigenic stimulation in vitroKazuhito Asano
Department of Physiology, School of Medicine, Showa University, Tokyo, Japan
Int Arch Allergy Immunol 133:267-75. 2004..The aim of this study is to examine the influence of fexofenadine hydrochloride (FEX), an H1-receptor antagonist, on TARC production from human peripheral blood leukocytes (PBL) using an in vitro cell culture technique...
- Allergy, histamine 1 receptor blockers, and the risk of multiple sclerosisAlvaro Alonso
Department of Epidemiology, Harvard School of Public Health, Boston, MA 02115, USA
Neurology 66:572-5. 2006....
- Epinastine hydrochloride antagonism against interleukin-4-mediated T cell cytokine imbalance in vitroKen-Ichi Kanai
Department of Otolaryngology, School of Medicine, Showa University, Tokyo, Japan
Int Arch Allergy Immunol 140:43-52. 2006....
- Biochemical characterization of desloratadine, a potent antagonist of the human histamine H(1) receptorJohn C Anthes
Schering Plough Research Institute, K15 1 1600, 2015 Galloping Hill Rd, Kenilworth, NJ 07033, USA
Eur J Pharmacol 449:229-37. 2002..The mechanism of desloratadine antagonism of the human histamine H(1) receptor may help to explain the high potency and 24-h duration of action observed in clinical studies...
- Tolerance to daytime sedative effects of H1 antihistaminesGary S Richardson
Sleep Disorders Clinic and Research Center, Henry Ford Hospital, Detroit, Michigan 48202, USA
J Clin Psychopharmacol 22:511-5. 2002..While other antihistamines and dosing regimens may differ, these results suggest that tolerance to the sedation produced by these drugs develops with remarkable rapidity...
- Dissociable effects of histamine H1 antagonists on reaction-time performance in ratsA Blokland
Maastricht Brain and Behaviour Institute, Faculty of Psychology, Section Neurocognition, Maastricht University, PO Box 616, 6200 MD Maastricht, The Netherlands
Pharmacol Biochem Behav 70:427-36. 2001..These findings suggest that the reaction-time task may be a sensitive tool for assessing effects of drugs on psychomotor function...
- Antihistamine antinociception is mediated by Gi-protein activationN Galeotti
Department of Preclinical and Clinical Pharmacology, Viale G. Pieraccini 6, I-50139 Florence, Italy
Neuroscience 109:811-8. 2002..These results suggest an important role played by the Gi-protein pathway in the transduction mechanism involved in the enhancement of the pain threshold produced by H(1)-antihistamines...
- Effect of cetirizine on bronchial hyperresponsiveness in patients with seasonal allergic rhinitis and asthmaM Aubier
, H pital Bichat, Paris, France
Allergy 56:35-42. 2001..011 ). These data demonstrate a protective nasal effect of C against BHR measured 6 h after nasal allergen challenge in patients with AR. They suggest that C may be useful in patients with asthma associated with AR...
- Desloratadine: A new, nonsedating, oral antihistamineR S Geha
Boston Children's Hospital and Harvard Medical School, Enders Building, Room 809, 300 Longwood Ave, Boston, MA 02115, USA
J Allergy Clin Immunol 107:751-62. 2001....
- Histamine H1 receptor antagonism by cetirizine in isolated guinea pig tissues: influence of receptor reserve and dissociation kineticsBernard Christophe
UCB Pharma, Allergo Respiratory Pharmacology Department, Chemin du Foriest, Bâtiment R1, B 1420 Braine l Alleud, Belgium
Eur J Pharmacol 470:87-94. 2003..Their mixed antagonism profile observed in the trachea can be explained by the small receptor reserve present in this tissue compared to the ileum and their very slow dissociation rate from the histamine H(1) receptor...
- Desloratadine demonstrates dose proportionality in healthy adults after single dosesSamir Gupta
Schering-Plough Research Institute, Kenilworth, New Jersey 07033-0539, USA
Clin Pharmacokinet 41:1-6. 2002..CONCLUSION: In this study, single doses of desloratadine as high as 4 times the recommended clinical dose of 5mg were well tolerated. The C(max) and AUC(S) for doses of 5 to 20mg increased in a dose-proportional manner...
- Adenosine monophosphate bronchial provocation and the actions of asthma therapyD K C Lee
Asthma and Allergy Research Group, Ninewells Hospital and Medical School, University of Dundee, Dundee DD1 9SY, Scotland, UK
Clin Exp Allergy 33:287-94. 2003
- Update on ocular allergy treatmentLeonard Bielory
UMDNJ Asthma and Allergy Research Center, Department of Medicine, Pediatrics and Ophthalmology, New Jersey Medical School, Newark, New Jersey 07103, USA
Expert Opin Pharmacother 3:541-53. 2002..The increased interest in advancing ocular treatment will lead to the development of additional therapies, novel pharmacokinetic delivery systems and, thus, improved healthcare outcomes for patients with allergic conjunctivitis...
- The pharmacologic profile of desloratadine: a reviewB M Henz
Department of Dermatology and Allergy, , Berlin, Germany
Allergy 56:7-13. 2001..Novel antiallergic and anti-inflammatory effects have also been noted with desloratadine, a fact which may be relevant to its clinical efficacy...
- [Effect of histamine on intracortical blood vessels of rats]Jian Jun Zhao
Research Center for Neuroscience, Department of Anatomy, Histology and Embryology, School of Medicine of Xi an Jiaotong University, Xi an 710061, China
Nan Fang Yi Ke Da Xue Xue Bao 26:1284-7. 2006..To investigate histamine-induced changes of the intracortical vessels in the cortical slice of rat brain...
- [Oral second generation antihistamines in allergic rhinitis]H Riechelmann
Laryngorhinootologie 84:30-41. 2005..CONCLUSION: Due to their minimal adverse effects and efficient symptom reduction oral second generation antihistamines are particularly useful for the treatment of less severe intermittent forms of nasal allergy...
- Comparative antiallergic effects of second-generation H1-antihistamines ebastine, cetirizine and loratadine in preclinical modelsJosep Llupià
Department of Pharmacological Development, Almirall Prodesfarma, Research Centre, Cardener 68 74, 08024 Barcelona, Spain
Arzneimittelforschung 53:93-7. 2003..In accordance with the clinical data, ebastine proved to be the substance with the widest range of application in animal experiments, too...
- Effect of histamine on phasic and tonic contractions of isolated uterine tissue from pregnant womenEgle Bytautiene
Division of Reproductive Sciences, Department of Obstetrics and Gynecology, University of Texas Medical Branch, Galveston, Tex 77555, USA
Am J Obstet Gynecol 188:774-8. 2003..CONCLUSION: Histamine increases spontaneous, but inhibits tonic, contractions of uterine strips from term pregnant nonlaboring women. Both effects are mediated through activation of H(1) receptors...
- Role of capsaicin-sensitive nerves and histamine H1, H2, and H3 receptors in the gastroprotective effect of histamine against stress ulcers in ratsArtur Dembinski
Department of Physiology, Jagiellonian University Medical School, 16 Grzegorzecka Street, Krakow 31 531, Poland
Eur J Pharmacol 508:211-21. 2005....
- Histamine signaling through the H(2) receptor in the Peyer's patch is important for controlling Yersinia enterocolitica infectionScott A Handley
Department of Molecular Microbiology, Washington University School of Medicine, 660 South Euclid Avenue, St Louis, MO 63110, USA
Proc Natl Acad Sci U S A 103:9268-73. 2006..In this study, we provide evidence that histamine signaling through the histamine H(2) but not the H(1) receptor is important for controlling Y. enterocolitica infection within the Peyer's patches and mesenteric lymph nodes of mice...
- Comparative efficacy of cetirizine and fexofenadine for seasonal allergic rhinitis, 5-12 hours postdose, in the environmental exposure unitJames H Day
Department of Medicine, Queen's University, Kingston, Ontario, Canada
Allergy Asthma Proc 26:275-82. 2005..6 and 0%, respectively; placebo, 35.0 and 0%, respectively. In conclusion, cetirizine produced greater relief of seasonal allergic rhinitis symptoms than fexofenadine at 12 hours postdose and over the 5- to 12-hour postdose period...
- Airway closure after antigen challenge in cynomolgus monkeys: effect of the histamine H1 receptor antagonist, chlorpheniramine maleateSusan Skeans
Schering-Plough Research Institute, Kenilworth, NJ 07033-0539, USA
Int Arch Allergy Immunol 137:37-44. 2005..Conclusions: These results demonstrate that airway closure occurs immediately after the antigen challenge in allergic cynomolgus monkeys and that histamine H1 receptors contribute very minimally to this response...
- Intravenous administration of diphenhydramine reduces histamine-induced vasodilator effects in the retina and choroidGünther Weigert
Department of Clinical Pharmacology, Medical University of Vienna, Austria
Invest Ophthalmol Vis Sci 47:1096-100. 2006..The receptor mediating this response has not yet been identified. The present study was undertaken to clarify whether H1 receptor blockade with diphenhydramine affects the hemodynamic response of histamine in the choroid and the retina...
- Histamine H1 receptors in rat dorsal raphe nucleus: pharmacological characterisation and linking to increased neuronal activityAlfonso Barbara
Departamento de Fisiologia, Biofisica y Neurociencias, Centro de Investigacion y de Estudios Avanzados, Apdo Postal 14 740, 07000 Mexico, DF, Mexico
Brain Res 954:247-55. 2002..Taken together, our results indicate that histamine modulates the firing of DRN presumed serotonergic neurones through the activation of H(1) receptors coupled to phosphonositide hydrolysis...
- Histaminergic neurons protect the developing hippocampus from kainic acid-induced neuronal damage in an organotypic coculture systemTiina Kaisa Kukko-Lukjanov
Department of Pharmacology and Clinical Pharmacology, University of Turku, FIN 20520 Turku, Finland
J Neurosci 26:1088-97. 2006..Our results suggest that histaminergic neurons protect the developing hippocampus from KA-induced neuronal damage, with regulation of neuronal survival being at least partly mediated through H1 and H3 receptors...
- Inhibition of tryptase release from human colon mast cells by histamine receptor antagonistsShao Heng He
Allergy and Inflammation Research Institute, Shantou University Medical College, Shantou 515031, China
Asian Pac J Allergy Immunol 23:35-9. 2005....
- The various effects of four H1-antagonists on serum substance P levels in patients with atopic dermatitisKunio Izu
Department of Dermatology, University of Occupational and Environmental Health, 1-1 Iseigaoka, Yahatanishi-ku, Kitakyushu 807-8555, Japan
J Dermatol 32:776-81. 2005....
- Yawning/cortical activation induced by microinjection of histamine into the paraventricular nucleus of the ratYoshinari Seki
Department of Physiology, Toho University School of Medicine, 5-21-16 Omori-nishi, Ohta-ku, Tokyo 143-8540, Japan
Behav Brain Res 134:75-82. 2002..These data demonstrate that a histamine receptive site for triggering yawning/arousal responses exists in the PVN, and suggest that these responses are mediated by activation of H1 receptor within the PVN...
- [Effect of fexofenadine--selective antagonist of histamine receptor (H1) on histamine-induced bronchoconstriction]Iwona Grzelewska-Rzymowska
Klinika Gruzlicy i Chorób Płuc Instytutu Medycyny Wewnetrznej Uniwersytetu Medycznego w Łodzi
Pol Merkur Lekarski 14:43-6. 2003..After another three days without fexofenadine, bronchial responsiveness returned to the initial value. The study points out that fexofenadine blocks H1 receptors in the bronchial tree...
- Similar rapid onset of action and magnitude of effect of fexofenadine and cetirizine as assessed by inhibition of histamine-induced wheal-and-flare reactionAshok Purohit
INSERM U425/EA3771, Faculte de Pharmacie, Illkirch, and Service de Pneumologie, , Strasbourg, France
Ann Allergy Asthma Immunol 93:562-7. 2004..12 by exact permutation test). CONCLUSIONS: Fexofenadine and cetirizine have comparable onset of action times and similar frequencies of inhibition, as evaluated by the occurrence of 95% inhibition of histamine-induced wheal and flare...
- Effect of histamine on the permeability of the nasal mucosa in vivoTian-Qun Yang
Department of Otorhinolaryngology, Mie University School of Medicine, Tsu, Mie, Japan
Acta Otolaryngol 123:401-5. 2003..CONCLUSION: These results indicate that histamine plays an important role in the change in mucosal permeability observed in allergic rhinitis in vivo via the histamine H1 receptor...
- Signaling via histamine receptors in cat duodenal smooth muscle cellsJi Hoon Jeong
Department of Pharmacology, College of Pharmacy, Chung Ang University, Seoul 156-756, Korea
Mol Cells 16:180-6. 2003..We conclude that histamine-induced contraction in cat duodenal smooth muscle cells is mediated by H1 receptors coupled to a PTX-insensitive Gq protein and results in activation of phosphatidylinositol-specific phospholipase C (PI-PLC)...
- Epileptogenic activity induced by histamine H(1) antagonists in amygdala-kindled ratsYoko Fujii
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Okayama University, Tsushima-naka 1-1-1, Okayama 700-8530, Japan
Brain Res 991:258-61. 2003..In conclusion, first-generation H(1) antagonists likely elicit epileptogenic activity in amygdala-kindled rats more potent than that in sham rats...
- Randomized double-blind comparison of cetirizine and fexofenadine after pollen challenge in the Environmental Exposure Unit: duration of effect in subjects with seasonal allergic rhinitisJames H Day
Division of Allergy and Immunology, Department of Medicine, Queen's University and Kingston General Hospital, Kingston, Ontario, Canada
Allergy Asthma Proc 25:59-68. 2004..Onset of action was comparable and both treatments were safe and well tolerated...
- Comparative effects of desloratadine, fexofenadine, and levocetirizine on nasal adenosine monophosphate challenge in patients with perennial allergic rhinitisD K C Lee
Asthma and Allergy Research Group, Ninewells Hospital and Medical School, University of Dundee, Dundee, Scotland, UK
Clin Exp Allergy 34:650-3. 2004..However, further long-term studies will be required to study their comparative effects on nasal symptoms, quality of life, as well as on nasal inflammatory cells...
- Comparison of the effects of desloratadine and levocetirizine on histamine-induced wheal, flare and itch in human skinK J Denham
Division of Infection, Inflammation and Repair, School of Medicine, University of Southampton, Southampton, UK
Inflamm Res 52:424-7. 2003..The difference is suggested to reflect the basic pharmacokinetics of the two drugs...
- Allergy medication in Japanese volunteers: treatment effect of single doses on nocturnal sleep architecture and next day residual effectsJulia Boyle
HPRU Medical Research Centre, University of Surrey, Guildford, UK
Curr Med Res Opin 22:1343-51. 2006..To evaluate the acute effects of two histamine H(1)-receptor antagonists on nocturnal sleep architecture and on next day cognitive function and psychomotor performance...
- Role of the histamine system in nefopam-induced antinociception in micePhilippe Girard
Laboratoires Biocodex, Service de Pharmacologie, Zac de Mercières 60200 Compiègne, France
Eur J Pharmacol 503:63-9. 2004..In conclusion, nefopam analgesic activity is not mediated by histamine H1 or H2 receptors, but can be slightly modulated by histamine H3 receptors in mouse pain tests...
- H1-receptor blocker antihistamine, terfenadine durably influences the glucocorticoid receptor, and lymphocyte histamine content of weanling ratsG Csaba
Department of Genetics, Cell and Immunobiology, Semmelweis University, P O Box 370, H 1445 Budapest, Hungary
Pharmacol Res 48:241-4. 2003..This means that not only the acute effects, but the prolonged side-effects must be considered...
- Influence of histamine and H1-receptor antagonists on ejaculated human spermatozoa: role of intrasperm Ca2+A Gupta
Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala 147 002, India
Indian J Exp Biol 42:481-5. 2004..However, pretreatment with famotidine, a H2-receptor antagonist did not produce such a protective action. The results strongly suggest that histamine elicits its spermicidal action via H1-receptors present on sperm cells...
- [H1 histamine antagonists]J Duchateau
Service d'Immunologie-C.H.U. Brugmann, U.L.B
Rev Med Brux 24:95-100. 2003..The authors are discussing the respective benefits of two recent molecules presented as 3rd generation molecules: fexofenadine and levocetirizine, while repositioning their use among available treatment strategy...
- Effects of bepotastine, cetirizine, fexofenadine, and olopatadine on histamine-induced wheal-and flare-response, sedation, and psychomotor performanceH Takahashi
Department of Dermatology, Asahikawa Medical College, Midorigaokahigashi, Asahikawa, Japan
Clin Exp Dermatol 29:526-32. 2004..Although olopatadine and cetirizine showed the strongest and most persistent suppression of histamine-induced wheal-and-flare response, olopatadine showed a considerable sedative effect with impaired psychomotor performance...
- Desloratadine inhibits constitutive and histamine-stimulated nuclear factor-kappaB activity consistent with inverse agonism at the histamine H1 ReceptorRen-Long Wu
Schering-Plough Research Institute, Schering-Plough Corporation, Kenilworth, NJ 07033, USA
Int Arch Allergy Immunol 135:313-8. 2004..Inhibition of basal and histamine-stimulated NF-kappaB activity may help to explain previously reported inhibitory effects of desloratadine on allergic inflammatory mediators...
- H1-antihistaminic activity of cetirizine and fexofenadine in allergic childrenF Estelle R Simons
John Buhler Research Center Allergy Laboratory, Faculty of Medicine, Faculty of Pharmacy, University of Manitoba, Winnipeg, Manitoba, Canada
Pediatr Allergy Immunol 14:207-11. 2003..In children age 6-11 years, cetirizine 10 mg has a rapid onset of H1-antihistaminic activity, a 24-h duration of action, and greater H1-activity than fexofenadine 30 mg. Higher doses of fexofenadine should be tested in children...
- Inhibition of the histamine wheal by ebastine compared with cetirizine, fexofenadine and loratadine at steady stateW Carey
Hammersmith Medicines Research, Central Middlesex Hospital, London NW10 7NS, United Kingdom
Drugs Exp Clin Res 28:243-7. 2002....
- Involvement of the betagamma subunits of G proteins in the cAMP response induced by stimulation of the histamine H1 receptorTakeshi Maruko
Department of Molecular Pharmacology, Kitasato University School of Pharmaceutical Sciences, 5-9-1 Shirokane, Minato-ku, Tokyo, 108-8641, Japan
Naunyn Schmiedebergs Arch Pharmacol 372:153-9. 2005..These results suggest that stimulation of histamine H1 receptors activates adenylyl cyclase through the release of G betagamma subunits from G proteins, thereby elevating intracellular cAMP levels...
- Ginkgo biloba extract improves spatial memory in rats mainly but not exclusively via a histaminergic mechanismYasuko Yamamoto
Department of Medicinal Pharmacology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama 700 8530, Japan
Brain Res 1129:161-5. 2007..From these findings, we concluded that the effects of GBE are mainly contributable to cholinergic activity and perhaps partly due to a histaminergic mechanism...
- 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 signalingR A Bakker
Leiden/Amsterdam Center for Drug Research, Department of Pharmacochemistry, Vrije Universiteit Amsterdam, Amsterdam, The Netherlands
Mol Pharmacol 60:1133-42. 2001....
- [Comparative activity of antihistamines on area under dose-response curve from histamine-induced wheal and flare responses in human skin]Rui qi Wang
Department of Allergy, PUMC Hospital, CAMS and PUMC, Beijing 100730, China
Zhongguo Yi Xue Ke Xue Yuan Xue Bao 26:634-8. 2004..To compare the activity of antihistamines by the index of area under dose-response curve (AUDRC) obtained from histamine-induced wheal and flare reactions...
- A comparative study of histamine activities on differentiation of osteoblasts and osteoclastsYoshiko Ikawa
J Toxicol Sci 32:555-64. 2007..This observation is consistent with the traditionally recognized histamine action of bone resorption at the osteoclast site...
- Inhibition of the histamine-induced weal and flare response: a valid surrogate measure for antihistamine clinical efficacy?P Devillier
Hopital Foch, Suresnes, France
Clin Exp Allergy 37:400-14. 2007....
- Twenty-four hours of activity of cetirizine and fexofenadine in the skinA Purohit
, H pitaux Universitaires, Strasbourg, France
Ann Allergy Asthma Immunol 86:387-92. 2001..CONCLUSIONS: Our study clearly shows better duration of action and consistency of the antihistaminic activity of cetirizine compared with fexofenadine (120 and 180 mg) in the histamine-induced skin reaction during a 24-hour period...
- Dopaminergic effects of histamine administration in the nucleus accumbens and the impact of H1-receptor blockadeR Galosi
Institute of Physiology and Neurophysiology Research Group of Hungarian Academy of Sciences, Pecs University Medical School, Pecs, Hungary
Neuropharmacology 40:624-33. 2001..These data are discussed with respect to the possible interactions between dopaminergic and histaminergic mechanisms in the mesolimbic system and their relation to mechanisms of reinforcement...
- Pharmacological profile of histaprodifens at four recombinant histamine H1 receptor species isoformsAndrea Strasser
Department of Pharmacology and Toxicology, University of Regensburg, Universitatsstrasse 31, D 93053 Regensburg, Germany
J Pharmacol Exp Ther 324:60-71. 2008....
- A randomized, double-blind, crossover comparison among cetirizine, levocetirizine, and ucb 28557 on histamine-induced cutaneous responses in healthy adult volunteersJ L Devalia
Academic Respiratory Medicine, St Bartholomew's and the Royal London School of Medicine and Dentistry, St Bartholomew's Hospital, London, UK
Allergy 56:50-7. 2001....
- Involvement of histamine released from mast cells in acute radiation dermatitis in miceSaiko Moriyasu
Department of Medical Physics and Engineering, Division of Health Sciences, Graduate School of Medicine, Osaka University, Japan
J Pharmacol Sci 104:187-90. 2007..These results suggest that gamma irradiation-induced erythema and edema were caused by histamine released from mast cells via histamine H1 receptor, and epilation was induced by other inflammatory mediators...
- ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammationUffe B Olsen
Department of General Pharmacology, Novo Nordisk A/S, 2760 Maaloev, Denmark
Eur J Pharmacol 435:43-57. 2002..ReN 1869 represents a new class of antihistamines with pain-relieving properties that probably is mediated centrally through histamine H(1) receptors but alternative mechanisms of action cannot be excluded...
- [Efficacy and safety of fexofenadine and cetirizine in the treatment of allergic rhinitis]A Lopez Garcia
Servicio de alergología e inmunología clínica, Hospital Universitario de Puebla
Rev Alerg Mex 48:168-72. 2001..Allergic rhinitis affects 20 million of people in United States and a higher figure all around the world...
- The histamine H1 receptor is not involved in local control of mammary blood flow in dairy cowsT G Madsen
Department of Basic Animal and Veterinary Sciences, The Faculty of Life Sciences, Copenhagen University, DK 1870 Frederiksberg C, Denmark
J Dairy Sci 91:2461-8. 2008..The mechanism by which an amino acid deficiency influences mammary blood flow does not involve histamine signaling through the H(1) receptor and remains unidentified...
- Analysis of disease-dependent sedative profiles of H(1)-antihistamines by large-scale surveillance using the visual analog scaleN Izumi
Department of Molecular Pharmacology, Institute of Health Biosciences, University of Tokushima Graduate School, Tokushima, Japan
Methods Find Exp Clin Pharmacol 30:225-30. 2008..Therefore, appropriate H(1)-antihistamines may need to be selected, depending on allergic diseases, to improve patients' QOL...
- Elevated nasal mucosal G protein levels and histamine receptor affinity in a guinea pig model of nasal hyperresponsivenessYoshihiko Chiba
Department of Pharmacology, School of Pharmacy, Hoshi University, 2 4 41 Ebara, Shinagawa ku, Tokyo 142 8501, Japan
Int Arch Allergy Immunol 127:285-93. 2002....
- [Comparative antihistamine and anti-allergic effects of various antihistamine preparations]D G Fridliand
Ter Arkh 74:67-72. 2002..The illustrated method may be helpful for individual selection of H1-antagonists for treatment of patients with allergic diseases...
- Stimulation of histamine H1 receptor up-regulates histamine H1 receptor itself through activation of receptor gene transcriptionAsish K Das
Department of Molecular Pharmacology, Graduate School of Health Biosciences, The University of Tokushima, Japan
J Pharmacol Sci 103:374-82. 2007..This finding provides new insights into the therapeutic target of H1R antagonist in allergic diseases...
- Histamine-induced modulation of vascular tone in the isolated chicken basilar artery: a possible involvement of endotheliumTadatsune Okuno
Department of Veterinary Pharmacology, Faculty of Agriculture, Kagoshima University, 1 21 24 Korimoto, Kagoshima 890 0065, Japan
Comp Biochem Physiol C Toxicol Pharmacol 147:339-44. 2008..The main relaxing factor released from endothelial cells is probably nitric oxide. The resting vascular tone was modulated by spontaneously released nitric oxide, but not by prostaglandins or thromboxane A(2)...
- Effects of histidine, a precursor of histamine, on pentylenetetrazole-induced seizures in ratsZhong Chen
Department of Pharmacology Department of Psychology, School of Medicine, Zhejiang University, Hangzhou 310031, China
Acta Pharmacol Sin 23:361-6. 2002..The effect of histidine on pentylenetetrazole-induced seizures was investigated in rats...
- Endogenous mast cell degranulation modulates cervical contractility in the guinea pigEgle Bytautiene
Department of Obstetrics and Gynecology, Division of Reproductive Sciences, The University of Texas Medical Branch, Galveston 77555-1062, USA
Am J Obstet Gynecol 186:438-45. 2002..Cervical infiltration and modulation of contractility by mast cells may play an important physiologic and/or pathologic role in the control of cervical function during pregnancy...
- Histamine H1 receptor activation stimulates mitogenesis in human astrocytoma U373 MG cellsA Hernández-Angeles
Departamento de Fisiologia, Biofísica y Neurociencias y, Centro de Investigacion y de Estudios Avanzados, Mexico City, Mexico
J Neurooncol 55:81-9. 2001..These results show that histamine H1 receptor activation stimulates the proliferation of human astrocytoma U373 MG cells. The action of histamine appears to be partially mediated by PKC stimulation and MAPK activation...
- Effects of histamine H1 receptor antagonists on action potentials in guinea-pig isolated papillary musclesI Ki
Department of Toxicology and Pharmacology, Dainippon Pharmaceutical Co, Ltd, Suita Osaka, Japan
Arch Int Pharmacodyn Ther 331:59-73. 1996....
- Clinical pharmacology of new histamine H1 receptor antagonistsF E Simons
Faculty of Medicine, University of Manitoba, Winnipeg, Canada
Clin Pharmacokinet 36:329-52. 1999..The studies cited in this review provide the scientific foundation for using the new H1 antagonists with optimal effectiveness and safety...
- Participation of histamine H1 and H2 receptors in passive cutaneous anaphylaxis-induced scratching behavior in ICR miceN Inagaki
Department of Pharmacology, Gifu Pharmaceutical University, Japan
Eur J Pharmacol 367:361-71. 1999..Histamine might also play an important role in compound 48/80-induced scratching behavior...
- Characterization of nasal obstruction in the allergic guinea pig using the forced oscillation methodRobbie L McLeod
Department of Allergy, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033 0539, USA
J Pharmacol Toxicol Methods 48:153-9. 2002..This is the first report to evaluate changes in nasal resistance in a preclinical animal model using the forced oscillation method...
- Comparative tolerability of second generation antihistaminesF Horak
ENT Clinic, University of Vienna, Austria
Drug Saf 20:385-401. 1999..Taking into account their negligible CNS activity, the low incidence of cardiovascular adverse effects, their lack of anticholinergic effects and other benefits, this class of antiallergic drugs represents a definite advance in therapy...
- Histamine H1 and H2 receptor antagonists accelerate skin barrier repair and prevent epidermal hyperplasia induced by barrier disruption in a dry environmentY 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..In conclusion, both the histamine H1 and H2 receptors in the epidermis are involved in skin barrier function and the cutaneous condition of epidermal hyperplasia...
- Targeting adenosine receptors: novel therapeutic targets in asthma and chronic obstructive pulmonary diseaseSteuart Rorke
Division of Respiratory Cell and Molecular Biology, University of Southampton School of Medicine, Southampton General Hospital, Southampton, UK
Am J Respir Med 1:99-105. 2002....
- [Molecular imaging of histamine receptors in the human brain]Manabu Tashiro
Division of Cyclotron Nuclear Medicine, Tohoku University Cyclotron and Radioisotope Centre, 6 3 Aoba, Aramaki, Aoba ku, Sendai 980 8575, Japan
Brain Nerve 59:221-31. 2007..A series of clinical studies on histamine H1 antagonists, or antihistamines, have demonstrated that antihistamines can be classified into sedative, mildly-..
- Roles of histamine in regulation of arousal and cognition: functional neuroimaging of histamine H1 receptors in human brainManabu Tashiro
Department of Pharmacology, Tohoku University Graduate School of Medicine, 2 1 Seiryo machi, Aoba ku, Miyagi, 980 8575, Sendai shi, Japan
Life Sci 72:409-14. 2002..b>Histamine H1 antagonists, or antihistamines, often prescribed for treatment of allergic disorders, sometimes induce sleepiness and ..
- Desloratadine for chronic idiopathic urticaria: a review of clinical efficacyLawrence Dubuske
Immunology Research Institute of New England, Gardner, Massachusetts 01440, USA
Am J Clin Dermatol 8:271-83. 2007..Other important prescribing considerations are that, unlike all first-generation and some second-generation antihistamines, desloratadine is nonsedating at its clinically approved dosage and does not impair psychomotor function...
- Effects of L-histidine depletion and L-tyrosine/L-phenylalanine depletion on sensory and motor processes in healthy volunteersP 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...
- Comparative anticholinergic activities of 10 histamine H1 receptor antagonists in two functional modelsRaymond F Orzechowski
Department of Pharmaceutical Sciences, Pharmacology and Toxicology Division, University of the Sciences in Philadelphia, Philadelphia, PA 19104, USA
Eur J Pharmacol 506:257-64. 2005..The remaining antihistamines had no significant effect at i.v. infusion doses up to 50 imol/kg. Cetirizine and fexofenadine did not antagonize cholinergic responses in either model...
Research Grants112 found, 100 shown here
- MEKK2 Regulation of Mast Cell/T Cell Cytokine ProductionErwin Gelfand; Fiscal Year: 2003..The studies will also define MEKK2 and ERK5 as targets for drug discovery for the control of allergic inflammation. ..
- Inflammation, Airways Reactivity and AsthmaErwin Gelfand; Fiscal Year: 2007..abstract_text> ..
- Optotrack Motion Analysis SystemTimothy Hain; Fiscal Year: 2005..Motion analysis equipment is critical to all of our research faculty, and we have also recently added investigators to the department who need motion analysis capabilities. ..
- HEAD CONTROL MECHANISMS DURING VOLUNTARY TRUNK MOVEMENTSTimothy Hain; Fiscal Year: 2002..The comparison of intact and BVL populations will elucidate why some persons with BVL recover relatively high functional levels, and others do not. ..
- Advances in Allergy, Asthma and ImmunologyLeonard Bielory; Fiscal Year: 2002..Summary: This application will provide the catalyst for establishing an ongoing forum for the review and promotion of scientifically based research assessing the impact of CAM in allergy, asthma and immunology. ..
- RELATIONSHIP BETWEEN ALLERGIC RHINITIS AND SINUSITISFuad Baroody; Fiscal Year: 2003..This will hopefully help to improve our therapeutic modalities for this enigmatic illness that affects millions of Americans every year. ..
- Restraint stress-induced neurogenic bladder inflammationTheoharis Theoharides; Fiscal Year: 2006..Our findings may be relevant to the pathophysiology of IC and may suggest new therapeutic approaches. ..
- Metabolic Polymorphisms and Survival from Brain TumorsMelissa Bondy; Fiscal Year: 2004..Thus, patients who can tolerate higher doses of chemotherapy can be treated more efficiently, suffering from less side effects and potentially may have a better outcome. ..
- PHARMACOGENOMICS OF ARRHYTHMIA THERAPYDan Roden; Fiscal Year: 2007..Participation in the Network will enable the long-term vision of exploiting human genomic information for more rationale drug development and ..
- Genetic Epidemiology of Glioma International ConsortiumMelissa Bondy; Fiscal Year: 2007..This information has translational significance for brain tumor patients and their families, and will enable us to develop appropriate genetic screening and counseling approaches to reduce the incidence and mortality of this disease. ..
- OCULOMOTOR SYSTEM AND BODY POSTURAL MECHANISMSBernard Cohen; Fiscal Year: 2006..abstract_text> ..
- Keratinocyte-derived immuno-suppressive cytokinesStephen Ullrich; Fiscal Year: 2005..A better understanding of the mechanisms involved may help with the design of rational approaches to block the induction of immune suppression, thereby reducing one of the major risk factors for skin cancer induction. ..
- CORTICOTROPIN RELEASING HORMONE INDUCED DURA MAST CELL ATheoharis Theoharides; Fiscal Year: 2001..They may also help explain some key events in the pathophysiology of migraines, the clinical symptoms of which are often precipitated by stress. ..
- Tools for Economic Analysis of Patient Management Interventions in Heart FailureShelby Reed; Fiscal Year: 2009..The TEAM-HF projects will provide clinicians and researchers with user-friendly tools to facilitate the conduct of high-quality economic evaluations of patient-focused interventions. ..
- Telecommunications Enhanced Asthma Management (TEAM)Bruce G Bender; Fiscal Year: 2010..designed using the RE-AIM framework so that it should have high reach and be consistently implemented at modest cost, and if effective, it can be maintained within KPCO as well as readily exported to other clinical healthcare settings ..
- HEPATIC DRUG TRANSPORTERS IN DRUG DISPOSITIONDan Roden; Fiscal Year: 2006..Moreover, variability in the extent of rifampin-mediated induction of the drug metabolizing enzyme, CYP3A, among subjects with variant OATP-C alleles, will also be tested. ..
- Do NKT cells mediate UV induced Immune Suppression?Stephen Ullrich; Fiscal Year: 2005..A better understanding of the mechanisms involved in UV-induced immune suppression may help with the design of rational approaches to block immune suppression, thereby reducing one of the major risk factors for skin cancer induction. ..
- Brain mast cells and Chronic Fatigue SyndromeTheoharis C Theoharides; Fiscal Year: 2010..The proposed research is expected to advance our understanding of how activation of brain mast cells can contribute to inflammation and CFS, as well as to the development of novel and effective treatments. ..
- Sublingual Immunotherapy for Peanut AllergyARVIL WESLEY BURKS; Fiscal Year: 2010..The development of a treatment and understanding the mechanism of how it works is important for the future treatment of patients with food allergy. ..
- Telecommunications Enhanced Asthma Management (TEAM)Bruce Bender; Fiscal Year: 2007..designed using the RE-AIM framework so that it should have high reach and be consistently implemented at modest cost, and if effective, it can be maintained within KPCO as well as readily exported to other clinical healthcare settings ..
- P GLYCOPROTEIN INDUCTION--KINETIC/DYNAMIC IMPLICATIONSGARY POLLACK; Fiscal Year: 2004....
- IMMUNOTHERAPY FOR PATIENTS WITH PEANUT ANAPHYLAXISARVIL BURKS; Fiscal Year: 2003..abstract_text> ..
- Understanding the Mechanism of Mucosal ImmunotherapyARVIL WESLEY BURKS; Fiscal Year: 2010..The long-term goal of the study is to utilize egg and peanut OIT for the induction of clinical and immunologic tolerance to the allergen that will be sustained once the protocol is completed. ..
- Understanding the Mechanism of Mucosal ImmunotherapyARVIL BURKS; Fiscal Year: 2007..The long-term goal of the study is to utilize egg and peanut OIT for the induction of clinical and immunologic tolerance to the allergen that will be sustained once the protocol is completed. ..
- Immunotherapy for Peanut AllergyARVIL BURKS; Fiscal Year: 2007..The significance of this proposal is that if peanut SLIT in peanut allergic patients is effective, the treatment would provide an immediate therapeutic option for patients. ..
- Dry Eye in PostmenopauseKelly K Nichols; Fiscal Year: 2010..This project is a unique blend of interdisciplinary clinical and basic research, which may lead to the translation of findings to clinical care in dry eye disease. ..
- Sublingual Immunotherapy for Peanut AllergyARVIL BURKS; Fiscal Year: 2009..The development of a treatment and understanding the mechanism of how it works is important for the future treatment of patients with food allergy. ..
- Meningioma: Risk Factors and Quality of LifeMelissa L Bondy; Fiscal Year: 2010..This study represents the first concentrated effort to examine environmental and genetic risk factors for meningiomas. ..
- Does UV-induced Unconventional Mast Cell Migration Activate Immune Suppression?Stephen E Ullrich; Fiscal Year: 2010....
- International Case Control Study of Malignant GliomaMelissa L Bondy; Fiscal Year: 2010..It will identify common genetic variants contributing to the risk of glioma from a genome wide association study. ..
- Soy Immunotherapy for Patients with Peanut AnaphylaxisARVIL BURKS; Fiscal Year: 2004..If soybean IT in peanut allergic patients is effective, the treatment would provide an immediate therapeutic option. ..
- EXTRAMURAL RES FACILITIES CONSTR PROJARVIL BURKS; Fiscal Year: 2002....
- GENETIC AND MOLECULAR EPIDEMIOLOGY OF GLIOMASMelissa Bondy; Fiscal Year: 1999..In addition, they are collecting blood from each new patient and their specimen repository will be available to study future candidate genes to integrate with the family data. ..
- The Effectiveness of Treatment for Adult PeriodontitisPhilippe Hujoel; Fiscal Year: 2006..This information can help determine in what area of periodontal research definitive clinical trials may offer the greatest contribution. ..
- Determinants of Breast Cancer SurvivalMelissa Bondy; Fiscal Year: 2006..abstract_text> ..
- ARKANSAS CHILDREN HOSP RES INST CONSTR: PAIN OSTEOGENESIS ARVIL BURKS; Fiscal Year: 2002..The planned facility expansion does not replace existing ACHRI facilities and will correct deficiencies and limitations in the present facilities. ..
- Dry Eye in PostmenopauseKelly Nichols; Fiscal Year: 2007..This project is a unique blend of interdisciplinary clinical and basic research, which may lead to the translation of findings to clinical care in dry eye disease. ..
- Inflammatory mediators and UV-induced carcinogenesisStephen Ullrich; Fiscal Year: 2007..The focus of the studies presented here is to provide evidence to support the hypothesis that these drugs can act as novel agents to prevent skin cancer formation. ..
- Meningioma: Risk Factors and Quality of LifeMelissa Bondy; Fiscal Year: 2007..This study represents the first concentrated effort to examine environmental and genetic risk factors for meningiomas. ..
- MOLECULAR EPIDEMIOLOGY OF GLIOMASMelissa Bondy; Fiscal Year: 2004..no abstract available ..