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Beta2-adrenoceptor agonist

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https://www.readbyqxmd.com/read/27582089/vilanterol-and-fluticasone-furoate-for-asthma
#1
Kerry Dwan, Stephen J Milan, Lynne Bax, Nicola Walters, Colin Powell
BACKGROUND: Vilanterol (VI) is a long-acting beta2-agonist (LABA) that binds to the beta2-adrenoceptor on the airway smooth muscle, producing bronchodilation. LABA therapy, which is well established in adults as part of the British Thoracic Society (BTS) Guidelines for the Management of Asthma, leads to improvement in symptoms and lung function and reduction in exacerbations. At present, the commonly used LABAs licensed for use in asthma management (formoterol and salmeterol) require twice-daily administration, whereas VI is a once-daily therapy...
September 1, 2016: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/27442692/beta-adrenoceptors-in-obstetrics-and-gynecology
#2
REVIEW
Beata Modzelewska
One hundred and twenty years after the description of extracts from the adrenal medulla, the use of beta-blockers and beta-agonists evolved from antianginal drugs and tocolytics to ligand-directed signaling. Beta-blockers in the fields of obstetrics and gynecology have so far been limited to the consideration of continuing treatment of disorders of the cardiovascular system and other dysfunctions that started before pregnancy. Studies in recent years have shown that beta-adrenoceptor signaling might be crucial in carcinogenesis and metastasis, apoptosis and anoikis...
April 2016: Developmental Period Medicine
https://www.readbyqxmd.com/read/27301515/asthmatic-attack-complicated-with-takotsubo-cardiomyopathy-after-frequent-inhalation-of-inhaled-corticosteroids-long-acting-beta2-adrenoceptor-agonists
#3
Nayuta Saito, Manabu Suzuki, Satoru Ishii, Eriko Morino, Jin Takasaki, Go Naka, Motoyasu Iikura, Yuichiro Takeda, Masayuki Hojo, Haruhito Sugiyama
A 63-year-old man was transferred to our hospital because of an exacerbation of asthma. His symptoms deteriorated even after increasing the dose of inhaled corticosteroids/long-acting beta2-adrenoceptor agonists (ICS/LABA). He had no chest pain and an electrocardiogram revealed ST elevation. A coronary angiogram revealed a reduced left ventricular function with an apical ballooning pattern without coronary stenosis. He was diagnosed with Takotsubo cardiomyopathy. Catecholamine elevation due to acute asthma and an overdose of ICS/LABA may be triggers of this disease...
2016: Internal Medicine
https://www.readbyqxmd.com/read/27182262/clinical-efficacy-of-tiotropium-in-children-with-asthma
#4
Juan Huang, Ying Chen, Zhen Long, Xiaoqin Zhou, Junhua Shu
OBJECTIVE: To investigate the clinical efficacy of tiotropium in children with asthma. METHODS: Eighty children with newly diagnosed moderate persistent asthma were enrolled into this study. The children were randomly assigned to the fluticasone propionate aerosol group or the fluticasone propionate aerosol plus tiotropium group for 12 weeks. RESULTS: Lung function was significantly improved in both groups at 4, 8, and 12 weeks compared with baseline (P < 0...
March 2016: Pakistan Journal of Medical Sciences Quarterly
https://www.readbyqxmd.com/read/27164986/beta2-agonist-doping-control-and-optical-isomer-challenges
#5
Glenn A Jacobson, J Paul Fawcett
The World Anti-Doping Agency (WADA) currently allows therapeutic use of the beta2-agonists salbutamol, formoterol and salmeterol when delivered via inhalation despite some evidence suggesting these anti-asthma drugs may be performance enhancing. Beta2-agonists are usually administered as 50:50 racemic mixtures of two enantiomers (non-superimposable mirror images), one of which demonstrates significant beta2-adrenoceptor-mediated bronchodilation while the other appears to have little or no pharmacological activity...
May 10, 2016: Sports Medicine
https://www.readbyqxmd.com/read/25742648/4-methylnitrosamino-1-3-pyridyl-1-butanone-promotes-esophageal-squamous-cell-carcinoma-growth-via-beta-adrenoceptors-in-vitro-and-in-vivo
#6
Nana Zhang, Xiujing Sun, Mingjiong Sun, Shengtao Zhu, Li Wang, Dan Ma, Yongjun Wang, Shutian Zhang, Peng Li
Cigarette smoke is a risk factor for esophageal squamous cell carcinoma (ESCC). It contains several carcinogens known to initiate and promote tumorigenesis as well as metastasis. The nitrosamine 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) is one of the strongest carcinogens in tobacco and our previous studies have shown its proliferation-promoting role in the progression of ESCC. Recently, NNK was identified as an agonist for both beta1- and beta2-adrenoceptors. Thus, we hypothesized that the cancer-promoting effect of NNK was likely mediated through beta-adrenoceptors in ESCC...
2015: PloS One
https://www.readbyqxmd.com/read/25344552/%C3%AE-2-adrenergic-stimulation-enhances-ca2-release-and-contractile-properties-of-skeletal-muscles-and-counteracts-exercise-induced-reductions-in-na-k-atpase-vmax-in-trained-men
#7
M Hostrup, A Kalsen, N Ortenblad, C Juel, K Mørch, S Rzeppa, S Karlsson, V Backer, J Bangsbo
The aim of the present study was to examine the effect of β2-adrenergic stimulation on skeletal muscle contractile properties, sarcoplasmic reticulum (SR) rates of Ca(2+) release and uptake, and Na(+)-K(+)-ATPase activity before and after fatiguing exercise in trained men. The study consisted of two experiments (EXP1, n = 10 males, EXP2, n = 20 males), where β2-adrenoceptor agonist (terbutaline) or placebo was randomly administered in double-blinded crossover designs. In EXP1, maximal voluntary isometric contraction (MVC) of m...
December 15, 2014: Journal of Physiology
https://www.readbyqxmd.com/read/24968643/denervation-and-beta2-adrenoceptor-agonist-administration-on-craniofacial-bone-density
#8
COMPARATIVE STUDY
Brendan Fitzpatrick, Michael Woods, Gordon Lynch, David Manton
OBJECTIVE: Beta2-agonist medications are thought to have adverse effects on bone density. Surgical denervation and intramuscular beta2-agonist injections appear to have opposing effects on skeletal muscles. The present study has been designed to assess the effects of denervation of the masseter, intramuscular injection of a beta2-agonist and the combination of both procedures, on bone density in the craniofacial skeleton in rats. MATERIALS AND METHODS: Sprague-Dawley rats were prepared as four groups: 1...
May 2014: Australian Orthodontic Journal
https://www.readbyqxmd.com/read/24761394/comparing-clinical-efficacy-of-symbicort-versus-pulmicort-in-reducing-asthma-symptom-and-improving-its-control
#9
Mohammad Emami, Azadeh Tayebi, Mojgan Gharipour, Somayeh Farzamnia, Akbar Kargari Temyarti
BACKGROUND: Recently, higher efficacy of the combination of long-acting beta2-adrenoceptor agonist and inhaled corticosteroids on controlling asthma symptoms has been hypothesized. This study aimed to examine the clinical effects of the combination of Budesonide with formoterol (Symbicort) and Budesonide (Pulmicort) alone in persistent asthma. MATERIALS AND METHODS: In a randomized double-blinded clinical trial, 76 patients with definite diagnosis of moderate-to-severe asthma were randomized to receive Pulmicort 180 mcg/inhalation two puffs twice daily, or receive Symbicort 80/4...
2014: Advanced Biomedical Research
https://www.readbyqxmd.com/read/24361988/the-antiallodynic-action-of-nortriptyline-and-terbutaline-is-mediated-by-%C3%AE-2-adrenoceptors-and-%C3%AE-opioid-receptors-in-the-ob-ob-model-of-diabetic-polyneuropathy
#10
Nada Choucair-Jaafar, Eric Salvat, Marie-José Freund-Mercier, Michel Barrot
Peripheral polyneuropathy is a frequent complication of diabetes. One of its consequences is neuropathic pain which is often chronic and difficult to treat. This pain management classically involves anticonvulsant drugs or tricyclic antidepressant drugs (TCA). We have previously shown that β2 adrenoceptors and δ opioid receptors are critical for TCA action in a traumatic model of neuropathic pain. In the present work, we used the obese leptin deficient mice (ob/ob) which are a genetic model of type 2 diabetes in order to study the treatment of diabetic polyneuropathy...
February 10, 2014: Brain Research
https://www.readbyqxmd.com/read/23996715/the-effect-of-polymorphisms-of-beta2-adrenoceptors-on-response-to-long-acting-beta2-agonists-in-iranian-asthmatic-patients
#11
Fatemeh Soleimani, Fanak Fahimi, Parisa Adimi Naghan, Seyed Alireza Nadji, Saeid Morowati, Nima Naderi, Mohammad Reza Masjedi
The results of many studies suggested possible relationship between polymorphism at codons 16 and 27 and development of tolerance to beta-2 adrenoceptor agonist responses as well as disease severity in asthmatic patients. This study was designed to evaluate the effect of polymorphism of beta2 adrenoceptors on response to salmeterol and fluticasone (as inhaled Seretide).Sixty-four patients with either mild or moderate-severe asthma were evaluated in this study. A four-week therapy with Seretide was conducted in moderate-severe asthmatics...
December 2013: Iranian Journal of Allergy, Asthma, and Immunology
https://www.readbyqxmd.com/read/23409722/long-acting-beta-agonists-and-their-association-with-inhaled-corticosteroids-in-copd
#12
REVIEW
L Fuso, N Mores, S Valente, M Malerba, P Montuschi
Inhaled bronchodilators, including beta(2)-agonists and antimuscaric receptor antagonists, are the mainstay of pharmacotherapy in chronic obstructive pulmonary disease (COPD). The short-acting beta(2)-agonists, including salbutamol, and fenoterol, have a rapid onset of action, a bronchodilating effect for 3-6 h and are used on demand. The long-acting beta(2)-agonists (LABAs), including salmeterol and formoterol, have 12-hour duration of action and are used with a twice-daily dosing regimen for long-term COPD treatment...
2013: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/23232038/vilanterol-trifenatate-a-novel-inhaled-long-acting-beta2-adrenoceptor-agonist-is%C3%A2-well-tolerated-in-healthy-subjects-and-demonstrates-prolonged-bronchodilation-in-subjects-with-asthma-and-copd
#13
Rodger Kempsford, Virginia Norris, Sarah Siederer
Vilanterol (VI; GW642444M) is a novel inhaled long-acting β2-agonist with inherent 24 h activity in vitro in development as a combination with the inhaled corticosteroid fluticasone furoate for both COPD and asthma. These studies were conducted to determine the safety, tolerability, pharmacodynamics and pharmacokinetics of VI in healthy subjects and subjects with mild to moderate persistent asthma and moderate to severe COPD. Single doses of VI (25-100 μg) were given once daily to subjects with asthma and COPD and repeat doses once daily for 14 days to healthy subjects...
April 2013: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/22812411/clinical-implications-of-recent-insights-into-the-structural-biology-of-beta2-adrenoceptors
#14
REVIEW
Marcos Antonio Amezcua-Gutierrez, Fabiola Jimena Cipres-Flores, Jose Guadalupe Trujillo-Ferrara, Marvin Antonio Soriano-Ursua
Analysis of the crystal structure of beta-2 adrenoceptors (β2ARs) is providing new insights into the functioning of this receptor and perhaps of G-protein coupled receptors (GPCRs) as a whole. This class of receptors represents the target of at least a third of the drugs on the market and plays an essential role in the study of therapetic drug-response. Among GPCRs, the β2AR is the best understood in terms of function, expression and activation. Regarding the interaction of β2ARs with a specific ligand, polymorphisms, conformational changes and stereoselectivity are important factors...
September 1, 2012: Current Drug Targets
https://www.readbyqxmd.com/read/22592732/beta2-adrenoceptor-agonists-for-dysmenorrhoea
#15
REVIEW
Zbys Fedorowicz, Mona Nasser, Vanitha A Jagannath, Jessica H Beaman, Kiran Ejaz, Esther J van Zuuren
BACKGROUND: Dysmenorrhoea is a common gynaecological complaint that can affect as many as 50% of premenopausal women, 10% of whom suffer severely enough to be rendered incapacitated for one to three days during each menstrual cycle. Primary dysmenorrhoea is where women suffer from menstrual pain but lack any pathology in their pelvic anatomy. Beta2-adrenoceptor agonists have been used in the treatment of women with primary dysmenorrhoea but their effects are unclear. OBJECTIVES: To determine the effectiveness and safety of beta2-adrenoceptor agonists in the treatment of primary dysmenorrhoea...
2012: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/22390078/-mechanism-of-the-slow-inotropic-response-of-the-mouse-atrium-mediated-by-the-beta2-adrenoreceptor
#16
Iu G Odnoshivkina, A M Petrov, A L Zefirov
The abundant beta2-adrenoceptors (AR) expression was revealed in the mouse atrial cardiomyocytes, albeit its function is poorly understood. Recently we revealed the slow developing (for 20-40 min) positive inotropic effect in the mouse atrium which was induced by the specific agonist of the beta2-adrenoceptors (5 mkM fenoterol) and the task of this study involved investigation of the found effect. It was shown that stimulation of beta2-AR is enough for rapid triggering of up-regulation of two signalling pathways that have the opposite influence on the contraction force...
November 2011: Rossiĭskii Fiziologicheskiĭ Zhurnal Imeni I.M. Sechenova
https://www.readbyqxmd.com/read/21914848/structural-flexibility-of-the-g-alpha-s-alpha-helical-domain-in-the-beta2-adrenoceptor-gs-complex
#17
Gerwin H Westfield, Søren G F Rasmussen, Min Su, Somnath Dutta, Brian T DeVree, Ka Young Chung, Diane Calinski, Gisselle Velez-Ruiz, Austin N Oleskie, Els Pardon, Pil Seok Chae, Tong Liu, Sheng Li, Virgil L Woods, Jan Steyaert, Brian K Kobilka, Roger K Sunahara, Georgios Skiniotis
The active-state complex between an agonist-bound receptor and a guanine nucleotide-free G protein represents the fundamental signaling assembly for the majority of hormone and neurotransmitter signaling. We applied single-particle electron microscopy (EM) analysis to examine the architecture of agonist-occupied β(2)-adrenoceptor (β(2)AR) in complex with the heterotrimeric G protein Gs (Gαsβγ). EM 2D averages and 3D reconstructions of the detergent-solubilized complex reveal an overall architecture that is in very good agreement with the crystal structure of the active-state ternary complex...
September 20, 2011: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/21780541/the-effect-of-formoterol-on-airway-goblet-cell-hyperplasia-and-protein-muc5ac-expression-in-asthmatic-mice
#18
Y F Tan, W Zhang, L Yang, S P Jiang
OBJECTIVES: Aim for this study was to investigate the effect of long-acting beta2-adrenoceptor agonist formoterol on airway goblet cell hyperplasia and protein Muc5ac expression in asthmatic mice. MATERIALS AND METHODS: Forty female BABL/c mice were randomly divided into four groups with 10 mice in each. Mice in group A were treated with saline as control, and mice in group B, group C and group D were sensitized by intraperitoneal injection of 10 microg alum precipitated chicken egg ovalbumin (OVA) to establish asthmatic model, but group C were pretreated with formoterol and group D were pretreated with dexamethasone...
July 2011: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/21622733/inflammatory-stimuli-inhibit-glucocorticoid-dependent-transactivation-in-human-pulmonary-epithelial-cells-rescue-by-long-acting-beta2-adrenoceptor-agonists
#19
Christopher F Rider, Elizabeth M King, Neil S Holden, Mark A Giembycz, Robert Newton
By repressing inflammatory gene expression, glucocorticoids are the most effective treatment for chronic inflammatory diseases such as asthma. However, in some patients with severe disease, or who smoke or suffer from chronic obstructive pulmonary disease, glucocorticoids are poorly effective. Although many investigators focus on defects in the repression of inflammatory gene expression, glucocorticoids also induce (transactivate) the expression of numerous genes to elicit anti-inflammatory effects. Using human bronchial epithelial (BEAS-2B) and pulmonary (A549) cells, we show that cytokines [tumor necrosis factor α (TNFα) and interleukin 1β], mitogens [fetal calf serum (FCS) and phorbol ester], cigarette smoke, and a G(q)-linked G protein-coupled receptor agonist attenuate simple glucocorticoid response element (GRE)-dependent transcription...
September 2011: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/21139051/thrx-198321-is-a-bifunctional-muscarinic-receptor-antagonist-and-beta2-adrenoceptor-agonist-maba-that-binds-in-a-bimodal-and-multivalent-manner
#20
Tod Steinfeld, Adam D Hughes, Uwe Klein, Jacqueline A M Smith, Mathai Mammen
Biphenyl-2-yl-carbamic acid 1-{9-[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydro-quinolin-5-yl)-ethylamino]-nonyl}-piperidin-4-yl ester (THRX-198321) is a single molecule composed of a muscarinic acetylcholine receptor (mAChR) antagonist moiety, represented by the fragment MA, linked by a C9 polymethylene chain to a β(2)-adrenoceptor (β(2)AR) agonist moiety, represented by the fragment 8-hydroxy-5-((R)-1-hydroxy-2-methylamino-ethyl)-1H-quinolin-2-one (BA). THRX-198321 exhibited high affinity for mAChR (M(2) pK(I,App) = 10...
March 2011: Molecular Pharmacology
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