Genomes and Genes
Summary: Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only.
- Seifert R, Schneider E, Dove S, Brunskole I, Neumann D, Strasser A, et al. Paradoxical stimulatory effects of the "standard" histamine H4-receptor antagonist JNJ7777120: the H4 receptor joins the club of 7 transmembrane domain receptors exhibiting functional selectivity. Mol Pharmacol. 2011;79:631-8 pubmed publisher..We discuss future directions to get out of the current dilemma in which there is no "standard" H(4)R antagonist available to the scientific community. ..
- Mishra G, Tamboli V, Jwala J, Mitra A. Recent patents and emerging therapeutics in the treatment of allergic conjunctivitis. Recent Pat Inflamm Allergy Drug Discov. 2011;5:26-36 pubmed..In recent years newer drug molecules have been introduced in the treatment of allergic conjunctivitis. This article reviews recent patents and emerging therapeutics in the treatment of allergic conjunctivitis. ..
- Palikhe N, Kim S, Ye Y, Hur G, Cho B, Park H. Association of CRTH2 gene polymorphisms with the required dose of antihistamines in patients with chronic urticaria. Pharmacogenomics. 2009;10:375-83 pubmed publisher..001). The CRTH2 -466T>C gene polymorphism may not affect on the phenotype of CU, but contributes to the required dose of antihistamines in patients with CU. ..
- Huang J, Thurmond R. The new biology of histamine receptors. Curr Allergy Asthma Rep. 2008;8:21-7 pubmed..Thus, a new class of H4R-specific antihistamines may be distinctively effective in treating allergic diseases associated with chronic pruritus and asthma. ..
- Dunford P, Williams K, Desai P, Karlsson L, McQueen D, Thurmond R. Histamine H4 receptor antagonists are superior to traditional antihistamines in the attenuation of experimental pruritus. J Allergy Clin Immunol. 2007;119:176-83 pubmed..Histamine H(4) receptor antagonists may have therapeutic utility for treating chronic pruritic diseases in humans where histamine H(1) receptor antagonists are not effective. ..
- Gbahou F, Rouleau A, Morisset S, Parmentier R, Crochet S, Lin J, et al. Protean agonism at histamine H3 receptors in vitro and in vivo. Proc Natl Acad Sci U S A. 2003;100:11086-91 pubmed
- Thurmond R, Desai P, Dunford P, Fung Leung W, Hofstra C, Jiang W, et al. A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther. 2004;309:404-13 pubmed..These results indicate that the histamine H4 receptor plays a role in the inflammatory process. Selective H4 receptor antagonists like JNJ 7777120 may have the potential to be useful in treating inflammation in humans. ..
- Ling P, Ngo K, Nguyen S, Thurmond R, Edwards J, Karlsson L, et al. Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation. Br J Pharmacol. 2004;142:161-71 pubmed..The histamine-induced shape change and upregulation of adhesion molecules on eosinophils can serve as biomarkers for clinical studies of H(4) receptor antagonists. ..
- Łazewska D, Ligneau X, Schwartz J, Schunack W, Stark H, Kiec Kononowicz K. Ether derivatives of 3-piperidinopropan-1-ol as non-imidazole histamine H3 receptor antagonists. Bioorg Med Chem. 2006;14:3522-9 pubmed..The most potent antagonists in this series have been in vitro the 4-(1,1-dimethylpropyl)phenyl ether 19 (hH3R K(i) = 8.4 nM) and in vivo the simple ethyl ether 2 (ED50 = 1.0mg/kg). ..
- Gutzmer R, Diestel C, Mommert S, Köther B, Stark H, Wittmann M, et al. Histamine H4 receptor stimulation suppresses IL-12p70 production and mediates chemotaxis in human monocyte-derived dendritic cells. J Immunol. 2005;174:5224-32 pubmed..Histamine induces chemotaxis and IL-12p70 suppression via different receptors using different signaling pathways, which might be important for the pathogenesis of and therapeutic interventions in allergic diseases. ..
- Criado P, Criado R, Maruta C, Machado Filho C. Histamine, histamine receptors and antihistamines: new concepts. An Bras Dermatol. 2010;85:195-210 pubmed..Consequently, knowledge of their pharmacokinetic and pharmacodynamic characteristics is essential for a better medical care, especially that offered to pregnant women, children, the elderly, and patients with comorbidities. ..
- Bielory L, Lien K, Bigelsen S. Efficacy and tolerability of newer antihistamines in the treatment of allergic conjunctivitis. Drugs. 2005;65:215-28 pubmed..Lastly, topical corticosteroids may be considered for severe seasonal ocular allergy symptoms, although long-term use should be avoided because of risks of ocular adverse effects, including glaucoma and cataract formation. ..
- Matsuki M, Sato N, Matsuda K, Yamaki M, Nakagawa N, Sakamoto N, et al. Brugada syndrome whose ST-segment changes were enhanced by antihistamines and antiallergenic drugs. Intern Med. 2009;48:1009-13 pubmed..An ICD implantation was selected for the therapy since ventricular fibrillation was induced. Our report discusses the possible contribution of antihistamines and antiallergenic drugs to the Brugada type ST-segment changes. ..
- Gemkow M, Davenport A, Harich S, Ellenbroek B, Cesura A, Hallett D. The histamine H3 receptor as a therapeutic drug target for CNS disorders. Drug Discov Today. 2009;14:509-15 pubmed publisher..Whether a single compound profile for the treatment of different disorders can be defined remains to be seen. ..
- Morgan M, Khan D, Nathan R. Treatment for allergic rhinitis and chronic idiopathic urticaria: focus on oral antihistamines. Ann Pharmacother. 2005;39:2056-64 pubmed..Pharmacists can play an important role in the management of allergic rhinitis and CIU by considering the relative advantages of newer-generation agents when reviewing treatment options. ..
- Diav Citrin O, Shechtman S, Aharonovich A, Moerman L, Arnon J, Wajnberg R, et al. Pregnancy outcome after gestational exposure to loratadine or antihistamines: a prospective controlled cohort study. J Allergy Clin Immunol. 2003;111:1239-43 pubmed..This study on the use of loratadine in human pregnancy suggests that this agent does not represent a major teratogenic risk. The study was powered to find a 3-fold increase in the overall rate of major anomalies. ..
- Tashiro M, Mochizuki H, Sakurada Y, Ishii K, Oda K, Kimura Y, et al. 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 ketotifen. Br J Clin Pharmacol. 2006;61:16-26 pubmed
- Cowart M, Sun M, Zhao C, Witte D, Miller T, Krueger K, et al. A new family of histamine H3 receptor antagonists based on a natural product: discovery, SAR, and properties of the series. Inflamm Res. 2007;56 Suppl 1:S47-8 pubmed
- Holgate S, Canonica G, Simons F, Taglialatela M, Tharp M, Timmerman H, et al. Consensus Group on New-Generation Antihistamines (CONGA): present status and recommendations. Clin Exp Allergy. 2003;33:1305-24 pubmed
- Moreno Delgado D, Torrent A, Gomez Ramirez J, de Esch I, Blanco I, Ortiz J. Constitutive activity of H3 autoreceptors modulates histamine synthesis in rat brain through the cAMP/PKA pathway. Neuropharmacology. 2006;51:517-23 pubmed..These results indicate that constitutive activity of H3 receptors in rat brain cortex inhibits the adenylate cyclase/PKA pathway, and perhaps also the opening of N-type voltage sensitive calcium channels, but apparently not CaMKII. ..
- Yamauchi K, Shikanai T, Nakamura Y, Kobayashi H, Ogasawara M, Maeyama K. [Roles of histamine in the pathogenesis of bronchial asthma and reevaluation of the clinical usefulness of antihistamines]. Yakugaku Zasshi. 2011;131:185-91 pubmed..H1-blockers are recommended as first-line drugs to treat allergic rhinitis in the guidelines. Therefore H1-blockers are strongly recommended for patients with both asthma and allergic rhinitis...
- Mizuguchi H, Kitamura Y, Kondo Y, Kuroda W, Yoshida H, Miyamoto Y, et al. Preseasonal prophylactic treatment with antihistamines suppresses nasal symptoms and expression of histamine H? receptor mRNA in the nasal mucosa of patients with pollinosis. Methods Find Exp Clin Pharmacol. 2010;32:745-8 pubmed publisher
- Buckland K, Williams T, Conroy D. Histamine induces cytoskeletal changes in human eosinophils via the H(4) receptor. Br J Pharmacol. 2003;140:1117-27 pubmed..6. This study demonstrates that human eosinophils express functional H4 receptors and may provide a novel target for allergic disease therapy. ..
- Cowden J, Riley J, Ma J, Thurmond R, Dunford P. Histamine H4 receptor antagonism diminishes existing airway inflammation and dysfunction via modulation of Th2 cytokines. Respir Res. 2010;11:86 pubmed publisher..The ability of H4R antagonists to affect these key manifestations of asthma suggests their potential as novel human therapeutics. ..
- Leonardi S, Marchese G, Marseglia G, La Rosa M. Montelukast in allergic diseases beyond asthma. Allergy Asthma Proc. 2007;28:287-91 pubmed..although additional controlled testing will be required, these applications broaden the possible range of treatments for allergic disease in all its many aspects. ..
- McDonald K, Trick L, Boyle J. Sedation and antihistamines: an update. Review of inter-drug differences using proportional impairment ratios. Hum Psychopharmacol. 2008;23:555-70 pubmed publisher..There are also differences within the AH drug generations. The review highlights the necessity to consider the sedating potential of AHs, along with other factors such as efficacy, when prescribing AHs to ambulant patients. ..
- Stahl S. Selective histamine H1 antagonism: novel hypnotic and pharmacologic actions challenge classical notions of antihistamines. CNS Spectr. 2008;13:1027-38 pubmed..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. ..
- Price D, Kemp L, Sims E, von Ziegenweidt J, Navaratnam P, Lee A, et al. Observational study comparing intranasal mometasone furoate with oral antihistamines for rhinitis and asthma. Prim Care Respir J. 2010;19:266-73 pubmed publisher..97) for achieving rhinitis control. Patients with rhinitis and co-morbid asthma initiating rhinitis therapy achieved significantly better upper as well as lower airway outcomes with intranasal mometasone than with oral antihistamine. ..
- Cowden J, Zhang M, Dunford P, Thurmond R. The histamine H4 receptor mediates inflammation and pruritus in Th2-dependent dermal inflammation. J Invest Dermatol. 2010;130:1023-33 pubmed publisher..Therefore, the dual effects of H(4)R antagonists on pruritus and Th2-cell-mediated inflammation point to their therapeutic potential for the treatment of Th2-mediated skin disorders, including atopic dermatitis. ..
- Sadofsky L, Campi B, Trevisani M, Compton S, Morice A. Transient receptor potential vanilloid-1-mediated calcium responses are inhibited by the alkylamine antihistamines dexbrompheniramine and chlorpheniramine. Exp Lung Res. 2008;34:681-93 pubmed publisher..Thus, the inhibition of TRPV1 activation by dexbrompheniramine may provide one potential mechanism whereby this antihistamine exerts its therapeutic effect in chronic cough. ..
- Eschler D, Klein P. An evidence-based review of the efficacy of topical antihistamines in the relief of pruritus. J Drugs Dermatol. 2010;9:992-7 pubmed..To critically review the body of clinical trials refuting or supporting the efficacy of topical antihistamines in the relief of pruritus...
- Bongers G, Bakker R, Leurs R. Molecular aspects of the histamine H3 receptor. Biochem Pharmacol. 2007;73:1195-204 pubmed..In this paper, we review various molecular aspects of the hH(3)R including its signal transduction, dimerization and the occurrence of different H(3)R isoforms. ..
- Pavlinkova G, Yanagawa Y, Kikuchi K, Iwabuchi K, Onoe K. Effects of histamine on functional maturation of dendritic cells. Immunobiology. 2003;207:315-25 pubmed..Consequently, histamine may contribute to an immune response outcome. ..
- Kitbunnadaj R, Zuiderveld O, De Esch I, Vollinga R, Bakker R, Lutz M, et al. Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists. J Med Chem. 2003;46:5445-57 pubmed..Moreover, replacement of the piperidine ring of immepip by a pyrrolidine ring led to a pair of enantiomers that show a distinct stereoselectivity at the human H(3) and H(4) receptor. ..
- Parsons M, Ganellin C. Histamine and its receptors. Br J Pharmacol. 2006;147 Suppl 1:S127-35 pubmed..Finally, the most recently (1999) discovered H(4) receptor promises the potential to provide drugs acting on the immunological system with possible applications in asthma and inflammation. ..
- Kwiatkowski M, Gabranski E, Huber K, Chapline M, Christie A, Dickinson P. Coordination of distinct but interacting rhythmic motor programs by a modulatory projection neuron using different co-transmitters in different ganglia. J Exp Biol. 2013;216:1827-36 pubmed publisher..Overall, our data suggest that the PS neurons differentially utilize their co-transmitters in spatially distinct locations to coordinate the activity of three independent networks. ..
- Konieczna L, Bober L, Belka M, Ciesielski T, Baczeki T. Chemometric exploration of the dependencies between molecular modeling descriptors and analytical chemistry data of antihistaminic drugs. J AOAC Int. 2012;95:713-23 pubmed
- Bell J, Mezrani C, Blacker N, Leblanc T, Frank O, Alderman C, et al. Anticholinergic and sedative medicines - prescribing considerations for people with dementia. Aust Fam Physician. 2012;41:45-9 pubmed..Reducing the number and dose of anticholinergic and sedative medicines may improve cognitive function and reduce the likelihood of adverse events. ..
- Mizuguchi H, Ono S, Hattori M, Fukui H. Inverse agonistic activity of antihistamines and suppression of histamine H1 receptor gene expression. J Pharmacol Sci. 2012;118:117-21 pubmed
- Wiest E, Jones J. Towards evidence-based emergency medicine: best BETs from the Manchester Royal Infirmary. BET 1: Use of non-sedating antihistamines in the common cold. Emerg Med J. 2011;28:632-3 pubmed publisher..It is concluded that there is no good evidence for the use of non-sedating antihistamines in the common cold. ..
- Fejzo M, Magtira A, Schoenberg F, MacGibbon K, Mullin P, Romero R, et al. Antihistamines and other prognostic factors for adverse outcome in hyperemesis gravidarum. Eur J Obstet Gynecol Reprod Biol. 2013;170:71-6 pubmed publisher..Given these results, there is an urgent need to address the safety and effectiveness of medications containing antihistamines in women with severe nausea of pregnancy. ..
- Benze G, Geyer A, Alt Epping B, Nauck F. [Treatment of nausea and vomiting with 5HT3 receptor antagonists, steroids, antihistamines, anticholinergics, somatostatinantagonists, benzodiazepines and cannabinoids in palliative care patients : a systematic review]. Schmerz. 2012;26:481-99 pubmed publisher..The English full text version of this article will be available in SpringerLink as of November 2012 (under "Supplemental"). ..
- Bartho L, Benko R. Should antihistamines be re-considered as antiasthmatic drugs as adjuvants to anti-leukotrienes?. Eur J Pharmacol. 2013;701:181-4 pubmed publisherIn spite of histamine mimicking the symptoms of allergic bronchoconstriction and severe anaphylaxis, histamine antagonists most probably represent no effective treatment for these conditions...
- Kuitunen T, Leino T, Parkkola K. [Motion sickness at sea and in the air]. Duodecim. 2011;127:1378-80 pubmed..Children of 2 to 12 years are most susceptible. Women are more susceptible than men to motion sickness. Predisposing factors include menstruation and pregnancy. Scopolamine and antihistamines are used for prevention of motion sickness. ..
- Wang B, An N, Shaikh A, Wang H, Xiao L, Liu H, et al. Hyperosmolarity evokes histamine release from ileum mucosa by stimulating a cholinergic pathway. Biochem Biophys Res Commun. 2017;493:1037-1042 pubmed publisher..The changes of Na+ and HCO3- ion transport are involved in the glucose-evoked decrease of basal ISC. ..
- Fröhlich S, Geidel C, Lauener R, Ring J, Möhrenschlager M. Chronic relapsing urticaria confined to injection sites of upper arms. Pediatr Dermatol. 2012;29:663-5 pubmed publisher..New ongoing urticarial lesions confined to former injection sites of vaccination and allergy immunotherapy were observed in an 8-year-old boy. This finding can be best explained as an isotopic response phenomenon. ..
- Emhoff C, Barrett O Keefe Z, Padgett R, Hawn J, Halliwill J. Histamine-receptor blockade reduces blood flow but not muscle glucose uptake during postexercise recovery in humans. Exp Physiol. 2011;96:664-73 pubmed publisher..In conclusion, while oral ingestion of H(1)- and H(2)-receptor antagonists alters postexercise recovery by attenuating vasodilatation, leg glucose uptake is not universally affected in recreationally active individuals. ..
- Feng C, Miller M, Simon R. The united allergic airway: connections between allergic rhinitis, asthma, and chronic sinusitis. Am J Rhinol Allergy. 2012;26:187-90 pubmed publisher..The aggregation of research suggests that AR, asthma, and chronic rhinosinusitis are linked by the united allergic airway, a notion that encompasses commonalities in pathophysiology, epidemiology, and treatment. ..
- LÃ³pez M, Navajas Galimany L. What are the effects of omalizumab in refractory chronic spontaneous urticaria?. Medwave. 2015;15 Suppl 3:e6346 pubmed publisher..Concluimos que el uso de omalizumab disminuye los sÃntomas y mejora la calidad de vida en pacientes con urticaria crÃ³nica espontÃ¡nea. ..
- Säfholm J, Dahlen S, Adner M. Antagonising EP1 and EP2 receptors reveal that the TP receptor mediates a component of antigen-induced contraction of the guinea pig trachea. Eur J Pharmacol. 2013;718:277-82 pubmed publisher..PGE2 primarily regulate the basal tone via EP1 and EP2, whereas prostanoids, such as TXA2 and PGD2, contribute as mediator of the antigen-response by activation of the TP receptor. ..
- Huntington M. When bed bugs bite. J Fam Pract. 2012;61:384-8 pubmed..Treating bed bug bites is straightforward; helping patients control and even prevent future infestations is another matter. Here's how you can help. ..
- Lv Y, Sun Y, Fu J, Kong L, Han S. Screening anti-allergic components of Astragali Radix using LAD2 cell membrane chromatography coupled online with UHPLC-ESI-MS/MS method. Biomed Chromatogr. 2017;31: pubmed publisher..The LAD2 cell membrane chromatography online with UHPLC-ESI-MS/MS method is an effective technique for screening the anti-allergic components of Huangqi. ..
- Salomon J, Białynicki Birula R, Woźniak Z, Baran E. Pachydermatous eosinophilic dermatitis. Acta Dermatovenerol Croat. 2011;19:31-5 pubmed..After one month of treatment, the skin changes markedly improved. ..
- Papadopoulou V, Ioannou S, Levidou G, Variami E, Kouzis P, Siakantaris M. Systemic mastocytosis accompanied by a non-secretory plasma cell dyscrasia and nephrotic syndrome-level proteinuria in a 76-year-old patient. Acta Haematol. 2014;131:78-83 pubmed publisher..This is a unique report of systemic mastocytosis with a non-secretory plasma cell dyscrasia and nephrotic syndrome. The pathophysiological relevance between these entities along with the probability of occult amyloidosis is discussed. ..
- Perrot Minnot M, Dion E, Cézilly F. Modulatory effects of the serotonergic and histaminergic systems on reaction to light in the crustacean Gammarus pulex. Neuropharmacology. 2013;75:31-7 pubmed publisher..pulex was also decreased by exogenous administration of the histamine receptor antagonist cimetidine, suggesting that photic behaviour may be controlled by more complex interactions between serotonergic and histaminergic systems. ..
- Dunford P, Holgate S. The role of histamine in asthma. Adv Exp Med Biol. 2010;709:53-66 pubmed..Novel immunomodulatory roles for histamine and the discovery of a novel histamine receptor, the histamine H4 receptor, have resulted in a reassessment of its importance in asthma. ..
- van der Mark S, Segers D, Bakker R, van Wijngaarden P. [DRESS syndrome as a result of sulfasalazine use]. Ned Tijdschr Geneeskd. 2010;154:A2161 pubmed..However, 20% of patients are severely affected and the DRESS syndrome is potentially life-threatening. The patient was successfully treated with a glucocorticoid and an antihistamine. ..
- Crayne C, Gerhold K, Cron R. Anaphylaxis to etanercept in two children with juvenile idiopathic arthritis. J Clin Rheumatol. 2013;19:129-31 pubmed publisher..Herein, we report 2 cases of anaphylaxis in children with JIA after etanercept injections. Although rare, pediatricians need to be aware of this potentially dangerous occurrence...
- Vasili E, Savo I, Doci X, Shkodrani E, Ntemoy A. Cutaneous mastocytosis: a case of bullous urticaria pigmentosa. Cutis. 2013;91:70-2 pubmed..We present a case of a 4-month-old infant with bullous UP. ..
- Figueroa K, Shankley N. One hundred years of histamine research. Adv Exp Med Biol. 2010;709:1-9 pubmed..The complexity is potentially overwhelming, but the promise of value to patients beyond that already provided by the first approved generations of histamine receptor blockers is a compelling driver. ..
- Di Gioacchino M, Cavallucci E, Ballone E, Cervone M, Di Rocco P, Piunti E, et al. Dose-dependent clinical and immunological efficacy of sublingual immunotherapy with mite monomeric allergoid. Int J Immunopathol Pharmacol. 2012;25:671-9 pubmed..Notably, the group treated with the higher dose showed significantly better clinical and immunological results. The efficacy of LAIS is correlated to the immune modulation in a clear dose-dependent effect. ..
- Benetti F, Da Silveira C, da Silva W, Cammarota M, Izquierdo I. Histamine reverses a memory deficit induced in rats by early postnatal maternal deprivation. Neurobiol Learn Mem. 2012;97:54-8 pubmed publisher..The present results suggest that the memory deficit induced by early postnatal maternal deprivation in rats may in part be due to an impairment of histamine mediated mechanisms in the CA1 region of the rat hippocampus. ..
- Li X, Xu X, Albano D, You T. Optimization using central composite design for antihistamines separation by nonaqueous capillary electrophoresis with electrochemical and electrochemiluminescence detections. Analyst. 2011;136:5294-301 pubmed publisher..This work is instructive for investigators in simplifying the NACE-EC/ECL development procedures for multi-component analysis. ..
- Zhou Z, Nie K, Huang Q, Li K, Sun Y, Zhou R, et al. Changes of cecal microflora in chickens following Eimeria tenella challenge and regulating effect of coated sodium butyrate. Exp Parasitol. 2017;177:73-81 pubmed publisher..In conclusion, our results show that coated sodium butyrate can balance the disorders of cecal microflora caused by E. tenella; thus, it can be a useful supplement for the control of avian coccidiosis. ..
- Sher L, Chang J, Patel I, Balkrishnan R, Fleischer A. Relieving the pruritus of atopic dermatitis: a meta-analysis. Acta Derm Venereol. 2012;92:455-61 pubmed publisher..Overall, the topical treatments were more successful at reducing atopic pruritus compared to the systemic treatments. Calcineurin inhibitors were the most effective antipruritic agent. ..