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Leukotriene antagonists

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https://www.readbyqxmd.com/read/27909742/the-anti-inflammatory-effect-of-montelukast-a-cysteinyl-leukotriene-receptor-1-antagonist-against-estradiol-induced-nonbacterial-inflammation-in-the-rat-prostate
#1
Mahmoud M Said, Maarten C Bosland
There is no standard treatment of chronic nonbacterial prostatitis in humans. The current study was aimed to investigate the effect of montelukast, an antagonist of cysteinyl leukotriene receptor-1, against estrogen-induced, nonbacterial lateral lobe-specific prostate inflammation in rats. Male Wistar rats were randomized into five groups of six rats, including sham controls (group 1) and castrated rats (group 2), whereas nonbacterial prostatitis (NBP) was induced in groups 3-5 by castration followed by a daily subcutaneous injection of estradiol (0...
December 1, 2016: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/27908761/discovery-of-dual-positive-allosteric-modulators-pams-of-the-metabotropic-glutamate-2-receptor-and-cyslt1-antagonists-for-treating-migraine-headache
#2
Maria-Jesus Blanco, Dana R Benesh, James A Knobelsdorf, Albert Khilevich, Guillermo S Cortez, Fese Mokube, Thomas D Aicher, Todd M Groendyke, Fredrik P Marmsater, Tony P Tang, Kirk W Johnson, Amy Clemens-Smith, Mark A Muhlhauser, Steven Swanson, John Catlow, Renee Emkey, Michael P Johnson, Jeffrey M Schkeryantz
Pyridylmethylsulfonamide series were the first reported example of positive allosteric modulators (PAM) of the mGlu2 receptor. The hydroxyacetophenone scaffold is a second series of mGlu2 PAMs we have identified. This series of molecules are potent mGlu2 potentiators and possess significant CysLT1 (cysteinyl leukotriene receptor 1) antagonist activity, showing in vivo efficacy in a dural plasma protein extravasation (PPE) model of migraine. In this paper, we describe the dual SAR, pharmacokinetics and preclinical in vivo efficacy data for a tetrazole containing hydroxyacetophenone scaffold...
November 18, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27888045/effects-of-tiotropium-on-lung-function-in-current-smokers-and-never-smokers-with-bronchial-asthma
#3
Makoto Yoshida, Yasuko Kaneko, Akiko Ishimatsu, Masashi Komori, Tomoaki Iwanaga, Hiromasa Inoue
The effects of tiotropium, an inhaled long-acting muscarinic antagonist, on lung function were investigated in current smokers and nonsmokers with asthma treated with inhaled corticosteroids (ICSs) and other asthma controllers: inhaled long-acting β2 agonists, leukotriene receptor antagonists, and/or theophylline. We conducted a double-blind, placebo-controlled study of an inhaled single dose of tiotropium in 9 asthmatics currently smoking and 9 asthmatics who have never smoked in a crossover manner. Lung function was measured before and 1, 3, and 24 h after inhalation of 18 μg of tiotropium or a placebo...
November 22, 2016: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/27885204/genetic-interactions-between-adrb2-and-ptger4-on-responses-to-salmeterol-or-montelukast-in-japanese-patients-with-mild-persistent-asthma
#4
Hideyasu Yamada, Hironori Masuko, Toshihide Inui, Jun Kanazawa, Yohei Yatagai, Tohru Sakamoto, Hiroaki Iijima, Satoshi Konno, Kaoruko Shimizu, Hironi Makita, Masaharu Nishimura, Fumio Kokubu, Takefumi Saito, Takeo Endo, Hiroki Ninomiya, Norihiro Kaneko, Nobuyuki Hizawa
BACKGROUND: Long-acting β2-agonists (LABA) and leukotriene receptor antagonists (LTRA) are two principal agents that can be added to inhaled corticosteroids (ICS) for patients with asthma that is not adequately controlled by ICS alone. In our previous study, the Gly16Arg genotype of the β2-adrenergic receptor (ADRB2) gene did not influence the differential bronchodilator effect of salmeterol versus montelukast as an add-on therapy to ICS within 16 weeks of follow-up (the J-Blossom study)...
2016: Arerugī, [Allergy]
https://www.readbyqxmd.com/read/27863551/in-vitro-cow-uterine-response-to-escherichia-coli-leukotrienes-and-cytokines
#5
A J Korzekwa, M Łupicka, B M- Socha, A A Szczepańska, E Piotrowicz, W Barański
The aim was to determine the dynamic profile of interactions between Escherichia coli (E. coli) and the actions of leukotrienes (LTs) and TNF and INFγ (cytokines) in the uterus in vitro. Uterine explants (N=6) were incubated for 2, 12 and 24h either as E. coli-treated (10(6)CFU) or non-treated and/or with: LTB4 and C4 (10(-6)M, for both LTs), LTs receptors antagonists (aLTR; 10(-6)M) and/or cytokines (each 10ng/ml). Toll Like Receptor 4 (TLR4) mRNA expression increased in explants incubated with E. coli, cytokines and LTs after 2 and 12h and aLTR inhibited the effect of LTs in explants incubated with E...
December 2016: Veterinary Immunology and Immunopathology
https://www.readbyqxmd.com/read/27854355/effects-of-asian-dust-particles-on-the-early-stage-antigen-induced-immune-response-of-asthma-in-nc-nga-mice
#6
Jun Kurai, Masanari Watanabe, Hiroyuki Sano, Degejirihu Hantan, Yuji Tohda, Eiji Shimizu
Asian dust (AD) can aggravate airway inflammation in asthma, but the association between AD and the development of asthma remains unclear. This study aimed to investigate the effects of AD on the early stage of antigen sensitization using a mouse model of asthma, as well as the role of leukotrienes (LTs) in antigen-induced airway inflammation potentiated by AD particles. NC/Nga mice were co-sensitized by intranasal instillation of AD particles and/or Dermatophagoides farinae (Df) for five consecutive days. Df-sensitized mice were stimulated with an intranasal Df challenge at seven days...
November 16, 2016: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/27826962/asthma-severity-and-the-controller-prescription-in-children-at-12-tertiary-hospitals
#7
Dong In Suh, Hyeon Jong Yang, Bong Seong Kim, Youn Ho Shin, So Yeon Lee, Geunhwa Park, Woo Kyung Kim, Hyo Bin Kim, Heysung Baek, Ja Kyoung Kim, Jin Tack Kim, Dae Hyun Lim
PURPOSE: Guidelines need to be tailored to where they are applied. We aimed to describe the distinctive asthma severity profile and the pattern of controller prescription in Korean children. METHODS: Twelve pediatric allergists from tertiary medical centers reviewed medical records of all asthmatic children who visited their clinics between September 1 and November 30 of 2013. Controller prescriptions were re-classified into 4 categories, then the prevalence of each asthma severity category and the controller prescription patterns according to asthma severity assessed by a Western (Global Initiative for Asthma, GINA) and an Asia-Pacific (Japanese Pediatric GuideLine, JPGL) guideline were evaluated...
January 2017: Allergy, Asthma & Immunology Research
https://www.readbyqxmd.com/read/27826703/leukotriene-receptor-antagonists-and-antiallergy-drugs
#8
Tsutomu Tamada, Masakazu Ichinose
As one of the candidates of the therapeutic strategy for asthma in addition to inhaled corticosteroids (ICS), leukotriene receptor antagonists (LTRAs) are known to be useful for long-term management of asthma patients complicated by allergic rhinitis (AR) or exercise-induced asthma (EIA). Currently available LTRAs are pranlukast hydrate, zafirlukast, and montelukast. These LTRAs have a bronchodilator action and inhibit airway inflammation, resulting in a significant improvement of asthma symptoms, respiratory function, inhalation frequency of as-needed inhaled β2-agonist, airway inflammation, airway hyperresponsiveness, dosage of ICSs, asthma exacerbations, and patients' QOL...
November 9, 2016: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/27817787/-effect-of-montelukast-sodium-intervention-on-airway-remodeling-and-percentage-of-th17-cells-cd4-cd25-regulatory-t-cells-in-asthmatic-mice
#9
Li Li, Chun-Yan Lou, Min Li, Jian-Bo Zhang, Jie Chen
OBJECTIVE: To study the dynamic changes in the percentage of Th17 cells/CD4(+)CD25(+) regulatory T cells after intervention with montelukast sodium, a leukotriene receptor antagonist, in asthmatic mice and the association between them. METHODS: Balb/c mice were randomly divided into blank group, asthma group, and montelukast sodium group. The asthmatic mouse model of airway remodeling was established by sensitization with intraperitoneal injection of chicken ovalbumin (OVA) and aluminum hydroxide suspension and aerosol inhalation of OVA...
November 2016: Zhongguo Dang Dai Er Ke za Zhi, Chinese Journal of Contemporary Pediatrics
https://www.readbyqxmd.com/read/27777180/individualized-therapy-for-persistent-asthma-in-young-children
#10
Anne M Fitzpatrick, Daniel J Jackson, David T Mauger, Susan J Boehmer, Wanda Phipatanakul, William J Sheehan, James N Moy, Ian M Paul, Leonard B Bacharier, Michael D Cabana, Ronina Covar, Fernando Holguin, Robert F Lemanske, Fernando D Martinez, Jacqueline A Pongracic, Avraham Beigelman, Sachin N Baxi, Mindy Benson, Kathryn Blake, James F Chmiel, Cori L Daines, Michael O Daines, Jonathan M Gaffin, Deborah Ann Gentile, W Adam Gower, Elliot Israel, Harsha Vardhan Kumar, Jason E Lang, Stephen C Lazarus, John J Lima, Ngoc Ly, Jyothi Marbin, Wayne Morgan, Ross E Myers, J Tod Olin, Stephen P Peters, Hengameh H Raissy, Rachel G Robison, Kristie Ross, Christine A Sorkness, Shannon M Thyne, Stanley J Szefler
BACKGROUND: Phenotypic presentations in young children with asthma are varied and may contribute to differential responses to asthma controller medications. METHODS: The Individualized Therapy for Asthma in Toddlers (INFANT) study was a multicenter, randomized, double-blind, double-dummy, clinical trial in children age 12-59 months (n=300) with asthma necessitating treatment with daily controller (Step 2) therapy. Participants completed a 2-8 week run-in period followed by three crossover periods with daily inhaled corticosteroid (ICS), daily leukotriene receptor antagonist (LTRA), and as-needed ICS treatment co-administered with albuterol...
October 21, 2016: Journal of Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/27742625/state-of-the-art-of-chronic-spontaneous-urticaria-in-italy-a-multicentre-survey-to-evaluate-physicians-and-patients-perspectives
#11
Marco Rimoldi, Oliviero Rossi, Nadia Rota
OBJECTIVE: To assess the clinical status of chronic spontaneous urticaria (CSU) and understand treatment approaches in Italy through specialists who treat CSU (dermatologists and allergy specialists) and CSU patients' experience. DESIGN: Multicentre survey. SETTING: Online structured questionnaires (one for physicians and one for patients). PARTICIPANTS: Physicians and patients with CSU in Italy. INTERVENTIONS: None...
October 14, 2016: BMJ Open
https://www.readbyqxmd.com/read/27725151/expression-and-cell-distribution-of-leukotriene-b4-receptor-1-in-the-rat-brain-cortex-after-experimental-subarachnoid-hemorrhage
#12
Zhen-Nan Ye, Zong Zhuang, Ling-Yun Wu, Jing-Peng Liu, Qiang Chen, Xiang-Sheng Zhang, Meng-Liang Zhou, Zi-Huan Zhang, Wei Li, Xiao-Liang Wang, Chun-Hua Hang
Convincing evidence supports that nuclear factor kappa B (NF-κB)-meditated inflammation contributes to the adverse prognosis of aneurysmal subarachnoid hemorrhage (SAH), and pathologic neutrophil accumulation after SAH in the brain parenchyma enhances the inflammatory process. Leukotriene B4 (LTB4) is a highly potent lipid chemoattractant of neutrophils, and its biological effects are mediated primarily through the high-affinity LTB4 receptor 1 (BLT1). It is verified that NF-κB-dependent BLT1 mediates LTB4 signaling and LTB4 stimulates NF-κB-dependent inflammation via BLT1...
October 7, 2016: Brain Research
https://www.readbyqxmd.com/read/27720931/cyslt1r-downregulation-reverses-intracerebroventricular-streptozotocin-induced-memory-impairment-via-modulation-of-neuroinflammation-in-mice
#13
Arijit Ghosh, Fang Chen, Feng Wu, Su-Su Tang, Mei Hu, Yan Long, Hong-Bin Sun, Ling-Yi Kong, Hao Hong
Our previous studies showed that cysteinyl leukotrienes receptor 1 (CysLT1R) is upregulated in amyloid-β (Aβ)-induced neurotoxicity and that administration of CysLT1R antagonists such as pranlukast or montelukast can ameliorate memory impairment in mice. In the current study, we sought to explore the role of CysLT1R in intracerebroventricular streptozotocin (STZ-ICV)-induced mouse model of memory impairment and neuroinflammation through shRNA-mediated knockdown of CysLT1R and also its pharmacological blockade by pranlukast...
February 6, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/27709465/leukotriene-receptor-antagonists-for-the-treatment-of-asthma-in-elderly-patients
#14
Hoang Kim Tu Trinh, Ga-Young Ban, Ji-Ho Lee, Hae-Sim Park
Elderly asthma (EA) is regarded as a distinct phenotype of asthma and is associated with age-related changes in airway structure and alterations in lung function and immune responses. EA is difficult to diagnose because of aging and co-morbidities, and overlaps with fixed airway obstructive disease. Novel modalities to differentiate between EA and chronic obstructive pulmonary disease (COPD) are necessary. A multifaceted approach, including clinical history, smoking habits, atopy, and measurement of lung function, is mandatory to differentiate asthma from COPD...
October 2016: Drugs & Aging
https://www.readbyqxmd.com/read/27703200/leukotriene-b4-receptor-type-2-protects-against-pneumolysin-dependent-acute-lung-injury
#15
Misako Shigematsu, Tomoaki Koga, Ayako Ishimori, Kazuko Saeki, Yumiko Ishii, Yoshitaka Taketomi, Mai Ohba, Airi Jo-Watanabe, Toshiaki Okuno, Norihiro Harada, Takeshi Harayama, Hideo Shindou, Jian-Dong Li, Makoto Murakami, Sumio Hoka, Takehiko Yokomizo
Although pneumococcal infection is a serious problem worldwide and has a high mortality rate, the molecular mechanisms underlying the lethality caused by pneumococcus remain elusive. Here, we show that BLT2, a G protein-coupled receptor for leukotriene B4 and 12(S)-hydroxyheptadecatrienoic acid (12-HHT), protects mice from lung injury caused by a pneumococcal toxin, pneumolysin (PLY). Intratracheal injection of PLY caused lethal acute lung injury (ALI) in BLT2-deficient mice, with evident vascular leakage and bronchoconstriction...
October 5, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27702591/montelukast-ameliorates-streptozotocin-induced-cognitive-impairment-and-neurotoxicity-in-mice
#16
Chun Teng Zhang, Jing Ran Lin, Feng Wu, Arijit Ghosh, Su Su Tang, Mei Hu, Yan Long, Hong Bin Sun, Hao Hong
Extensive studies have demonstrated that neuroinflammation is associated with Alzheimer's disease (AD) and cysteinyl leukotriene receptor 1 (CysLT1R) was involved in neuroinflammation. Montelukast, a highly selective CysLT1R antagonist, has been reported to attenuate learning and memory impairments in the amyloid-β-induced mouse model of AD. However, whether montelukast also exerts beneficial effects on streptozotocin (STZ)-induced memory deficits in mice is not well known. In the present study, we aimed to investigate the effects of montelukast on STZ-induced cognitive impairment, neuroinflammation and apoptosis in mice...
October 1, 2016: Neurotoxicology
https://www.readbyqxmd.com/read/27697457/aryl-hydrocarbon-receptor-ligand-axis-mediates-pulmonary-fibroblast-migration-and-differentiation-through-increased-arachidonic-acid-metabolism
#17
Hsiang-Han Su, Hsin-Ting Lin, Jau-Ling Suen, Chau Chyun Sheu, Kazunari K Yokoyama, Shau-Ku Huang, Chih Mei Cheng
Pulmonary fibroblast migration and differentiation are critical events in fibrogenesis; meanwhile, fibrosis characterizes the pathology of many respiratory diseases. The role of aryl hydrocarbon receptor (AhR), a unique cellular chemical sensor, has been suggested in tissue fibrosis, but the mechanisms through which the AhR-ligand axis influences the fibrotic process remain undefined. In this study, the potential impact of the AhR-ligand axis on pulmonary fibroblast migration and differentiation was analyzed using human primary lung fibroblasts HFL-1 and CCL-202 cells...
September 30, 2016: Toxicology
https://www.readbyqxmd.com/read/27677381/prevalence-and-risk-factors-for-asthma-among-children-aged-0-14-years-in-hangzhou-a-cross-sectional-survey
#18
Dan Xu, Yingshuo Wang, Zhimin Chen, Shuxian Li, Yungai Cheng, Li Zhang, Lingzhi Zhao
BACKGROUND: Asthma is a global problem. Prevalence varies among different countries and cities. We aimed to obtain the prevalence, describe the characteristics, and discover factors that may relate to asthma in Hangzhou. METHODS: This cross-sectional study was conducted in Hangzhou. The subjects were children aged 14 years and younger. A control group of non-asthma children that matched in age and sex with each asthmatic patient was also randomly selected and interviewed...
September 27, 2016: Respiratory Research
https://www.readbyqxmd.com/read/27671822/boswellic-acids-and-their-role-in-chronic-inflammatory-diseases
#19
H P T Ammon
: Boswellic acids, which are pentacyclic triterpenes belong to the active pharmacological compounds of the oleogum resin of different Boswellia species. In the resin, more than 12 different boswellic acids have been identified but only KBA and AKBA received significant pharmacological interest. Biological Activity: In an extract of the resin of Boswellia species multiple factors are responsible for the final outcome of a therapeutic effect, be it synergistic or antagonistic. Moreover, the anti-inflammatory actions of BAs are caused by different mechanisms of action...
2016: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/27650241/allergy-medications-during-pregnancy
#20
REVIEW
Alexei Gonzalez-Estrada, Stephen A Geraci
Allergic diseases are common in women of childbearing age. Both asthma and atopic conditions may worsen, improve or remain the same during pregnancy. Primary care physicians commonly encounter women receiving multiple medications for pre-existing atopic conditions, who then become pregnant and require medication changes to avoid potential fetal injury or congenital malformations. Each medication should be evaluated; intranasal and inhaled steroids are relatively safe to continue during pregnancy (budesonide is the drug of choice), second-generation antihistamines of choice are cetirizine and loratadine, leukotriene receptor antagonists are safe, sparing use of oral decongestants during the first trimester and omalizumab may be used for both uncontrolled asthma and for antihistamine-resistant urticaria...
September 2016: American Journal of the Medical Sciences
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