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.
Publications198 found, 100 shown here
- 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....
- Seizure-modifying potential of histamine H1 antagonists: a clinical observationIppei Miyata
Department of Pediatrics, Enshu General Hospital, Hamamatsu City, Shizuoka, Japan
Pediatr Int 53:706-8. 2011..The widely used histamine H(1) antagonists have a potential to induce seizures, although clinical evaluation is scarce except for a few case reports...
- H1 histamine receptor antagonists induce genotoxic and caspase-2-dependent apoptosis in human melanoma cellsShawkat Muhialdin Jangi
Department of Cell Biology and Histology, Faculty of Medicine and Dentistry, University of the Basque Country, Leioa E 48940, and Department of Dermatology, Cruces Hospital, Vizcaya, Spain
Carcinogenesis 27:1787-96. 2006..The present results may contribute to the elaboration of novel therapeutic strategies for the treatment of malignant human melanoma...
- Clinical pharmacokinetics of fexofenadine enantiomersMasatomo Miura
Akita University Hospital, Department of Pharmacy, Akita 010 8543, Japan
Expert Opin Drug Metab Toxicol 6:69-74. 2010....
- Brain histamine H receptor occupancy of orally administered antihistamines measured by positron emission tomography with (11)C-doxepin in a placebo-controlled crossover study design in healthy subjects: a comparison of olopatadine and ketotifenManabu Tashiro
Department of Pharmacology, Tohoku University Graduate School of Medicine, Sendai, Miyagi, Japan
Br J Clin Pharmacol 61:16-26. 2006..The purpose of the present study is to measure histamine H(1) receptor (H(1)R) occupancy due to olopatadine, a new second-generation antihistamine and to compare it with that of ketotifen...
- 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...
- P-glycoprotein limits the brain penetration of nonsedating but not sedating H1-antagonistsCuiping Chen
Pfizer Global Research and Development, Pfizer Inc, Groton, Connecticut 06340, USA
Drug Metab Dispos 31:312-8. 2003..In contrast, nonsedating H1-antagonists cetirizine, loratadine, and desloratadine are P-gp substrates. Affinity for P-gp at BBB may explain the lack of central nervous system side effects of modern H1-antagonists...
- 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...
- Antihistamines in dermatologyMalcolm W Greaves
National Skin Centre, Singapore, Singapore
Skin Pharmacol Physiol 18:220-9. 2005..Two early low-sedation second-generation antihistamines caused arrhythmias in a small number of patients but these compounds have now been withdrawn. Generally, the second-generation H1 antihistamines are well tolerated...
- 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 ..
- Histamine H1 receptor antagonist blocks histamine-induced proinflammatory cytokine production through inhibition of Ca2+-dependent protein kinase C, Raf/MEK/ERK and IKK/I kappa B/NF-kappa B signal cascadesMasahiro Matsubara
Department of Pharmacology and Molecular Biology, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co Ltd, Shizuoka 411 8731, Japan
Biochem Pharmacol 69:433-49. 2005..Thus, the anti-inflammatory benefit of H1 antagonists may be in part due to prevention of cytokine production...
- An effective and more convenient drug regimen for prophylaxis against paclitaxel-associated hypersensitivity reactionsM Markman
Department of Hematology Medical Oncology, The Cleveland Clinic Foundation, Ohio 44195, USA
J Cancer Res Clin Oncol 125:427-9. 1999....
- Lack of preventing effect of systemically and topically administered histamine H(1) or H(4) receptor antagonists in a dog model of acute atopic dermatitisWolfgang Baumer
Department of Pharmacology, Toxicology and Pharmacy, University of Veterinary Medicine, Hannover, Germany
Exp Dermatol 20:577-81. 2011..In conclusion, the preventive administration of H1R or H4R antagonists has no impact on the development of acute skin lesions in this experimental canine atopic dermatitis model...
- 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...
- 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....
- The noncompetitive antagonism of histamine H1 receptors expressed in Chinese hamster ovary cells by olopatadine hydrochloride: its potency and molecular mechanismYuichi Matsumoto
Pharmaceutical Research Center, Kyowa Hakko Kogyo Co, Ltd, Japan
Pharmacology 81:266-74. 2008..The second extracellular loop in aminergic G-protein-coupled receptors contributes to ligand binding and therefore the noncompetitive property of olopatadine may be explained by the interaction with Glu 181...
- P-glycoprotein limits the brain penetration of olopatadine hydrochloride, H1-receptor antagonistNobuhito Mimura
Pharmacokinetic Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co, Ltd, Sunto gun, Shizuoka, Japan
Drug Metab Pharmacokinet 23:106-14. 2008..These results suggest that olopatadine is a substrate of P-gp, and that P-gp limits the brain penetration but dose not affect the plasma concentration of olopatadine...
- 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....
- 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...
- Addition of fexofenadine to a topical corticosteroid reduces the pruritus associated with atopic dermatitis in a 1-week randomized, multicentre, double-blind, placebo-controlled, parallel-group studyM Kawashima
Department of Dermatology, Tokyo Women s Medical University, 8 1, Kawada cho, Shinjuku ku, Tokyo, 162 8666, Japan
Br J Dermatol 148:1212-21. 2003..The pruritus associated with atopic dermatitis is considered to be induced, in part, by histamine. Therefore, we thought that fexofenadine may be useful in the relief of pruritus associated with atopic dermatitis...
- 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...
- A comparison of two prophylactic regimens for hypersensitivity reactions to paclitaxelJanice S Kwon
Division of Gynecologic Oncology, University of Toronto, Toronto, Ontario, M5S 1A1, Canada
Gynecol Oncol 84:420-5. 2002....
- 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..The extent of the distribution of H(1)- antihistamines into the skin and H(1)-antihistamine activity in the skin are clinically relevant in the treatment of allergic skin disorders...
- 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...
- Neuroimaging of histamine H1-receptor occupancy in human brain by positron emission tomography (PET): a comparative study of ebastine, a second-generation antihistamine, and (+)-chlorpheniramine, a classical antihistamineM Tagawa
Department of Pharmacology, Tohoku University School of Medicine, Sendai, Japan
Br J Clin Pharmacol 52:501-9. 2001....
- An evaluation of the effects of high-dose fexofenadine on the central nervous system: a double-blind, placebo-controlled study in healthy volunteersI Hindmarch
HPRU Medical Research Centre, University of Surrey, Guildford, UK
Clin Exp Allergy 32:133-9. 2002....
- 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....
- Central effects of fexofenadine and cetirizine: measurement of psychomotor performance, subjective sleepiness, and brain histamine H1-receptor occupancy using 11C-doxepin positron emission tomographyManabu Tashiro
Department of Pharmacology, Tohoku University School of Medicine, 2 1 Seiryo cho, Aoba ku, Sendai, Miyagi 980 8575, Japan
J Clin Pharmacol 44:890-900. 2004..H1RO was negligible with fexofenadine (-0.1%) but moderately high with cetirizine (26.0%). In conclusion, fexofenadine 120 mg is distinguishable from cetirizine 20 mg, as assessed by H1RO and psychomotor testing...
- 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...
- Evaluation of efficacy and sedative profiles of H(1) antihistamines by large-scale surveillance using the visual analogue scale (VAS)Norimasa Izumi
Department of Molecular Pharmacology, Institute of Health Biosciences, The University of Tokushima Graduate School, Japan
Allergol Int 57:257-63. 2008..However, it is not easy to obtain these parameters. Here, we sought to evaluate the sedative properties of H(1) antihistamines by means of a large-scale surveillance at health insurance pharmacies...
- 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...
- 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...
- 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...
- Consensus Group on New-Generation Antihistamines (CONGA): present status and recommendationsS T Holgate
Respiratory Cell and Molecular Biology, Infection, Inflammation, and Repair Division, School of Medicine, University of Southampton, UK
Clin Exp Allergy 33:1305-24. 2003
- 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..The present study was undertaken to examine whether H1 receptor antagonists could modulate IL-4-mediated immune responses in vitro...
- 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...
- 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...
- 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..The purpose of the present study was to evaluate the effects of the mast cell stabilizer, ketotifen, on leukocyte adhesion within, and tissue leakage from the mucosal villous microcirculation after intestinal I/R...
- 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....
- 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...
- 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..Cetirizine, a putative H1-receptor antagonist, has recently been shown to have anti-inflammatory properties through the inhibition of leucocyte recruitment and activation, and by the reduction of ICAM-1 expression on keratinocytes...
- 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
- 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....
- 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..Our objective was to develop a population pharmacokinetic (PPK) model for epinastine, a histamine H(1) receptor antagonist, in adults and children and to obtain pharmacokinetic information to support dosing recommendations in children...
- 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...
- 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...
- 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..In patients with asthma, treatment for associated conditions, such as rhinitis, is recommended. It is unknown whether this treatment can reduce the risk for emergency department (ED) visits for asthma...
- 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....
- 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....
- An evidence-based review of the efficacy of antihistamines in relieving pruritus in atopic dermatitisP A Klein
Department of Dermatology, State University of New York at Stony Brook, 11794 8165, USA
Arch Dermatol 135:1522-5. 1999..To critically review the body of clinical trials that refute or support the efficacy of antihistamines in relieving pruritus in patients with atopic dermatitis...
- The effects of acute doses of fexofenadine, promethazine, and placebo on cognitive and psychomotor function in healthy Japanese volunteersFran Ridout
HPRU Medical Research Centre, University of Surrey, Egerton Road, Guildford, Surrey, United Kingdom
Ann Allergy Asthma Immunol 90:404-10. 2003..Genetic variations in cross-cultural metabolic capability may attenuate the lack of central nervous system effects of fexofenadine...
- 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
- 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..To evaluate the dose proportionality and linearity and pharmacokinetic profile of desloratadine after single oral doses over the range of 5 to 20mg...
- 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...
- 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...
- 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...
- 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...
- 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...
- 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, Hopitaux Universitaires, Strasbourg, France
Ann Allergy Asthma Immunol 93:562-7. 2004..Histamine-induced wheal-and-flare studies are useful, objective tests for determining differences in the peripheral H1-receptor blockade activities of antihistamines...
- 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..Certain H1 antihistamines have recently been shown to inhibit basal NF-kappaB activity by stabilizing the H1 receptor in an inactive state, a phenomenon called 'inverse agonism'...
- 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...
- 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)...
- 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...
- 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...
- 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...
- 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...
- 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 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...
- 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..This double blind, crossover study examined the effects of desloratadine in 12 healthy volunteers. Levocetirizine was used as a comparator...
- 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...
- 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...
- 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...
- [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...
- [Oral second generation antihistamines in allergic rhinitis]H Riechelmann
Univ HNO Klinik Ulm
Laryngorhinootologie 84:30-41. 2005..Histamine is a key mediator of the allergic immediate reaction. Antihistamines belong to the most frequently used treatment modalities in allergic rhinitis...
- [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...
- 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....
- 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....
- 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...
- [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...
- 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...
- 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...
- 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...
- 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...
- 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...
- 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....
- Involvement of the βγ 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...
- 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 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....
- 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..In this study, an allergic cynomolgus monkey model was used to characterize the condition of airway closure and assess the contribution of histamine H1 receptors to this response...
- 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)...
- 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....
- 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....
- [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...
- 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....
- 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....
- 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...
- 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...
- 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..To enhance our understanding of the uterotonic effect of histamine, we compared the effects of histamine on spontaneous phasic and tonic contractile activity of uterine strips from term pregnant nonlaboring women...
- [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...
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 ..