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Beta2-adrenoceptor agonist

Søren Jessen, Johan Onslev, Anders Lemminger, Vibeke Backer, Jens Bangsbo, Morten Hostrup
INTRODUCTION: Due to a high prevalence of asthma and exercise-induced bronchoconstriction in elite athletes, there is a high use of beta2 -adrenoceptor agonists (beta2 -agonists) in the athletic population. While anabolic in rodents, no study has been able to detect hypertrophy in humans after chronic beta2 -agonist inhalation. METHODS: We investigated if inhaled beta2 -agonist, terbutaline, alters body composition and metabolic rate with and without concurrent exercise training in healthy young men...
May 19, 2018: Scandinavian Journal of Medicine & Science in Sports
Morten Hostrup, Johan Onslev, Glenn A Jacobson, Richard Wilson, Jens Bangsbo
KEY POINTS: While several studies have investigated the effects of exercise training in human skeletal muscle and the chronic effect of β2 -agonist treatment in rodent muscle, their effects on muscle proteome signature with related functional measures in humans are still incompletely understood. Herein we show that daily β2 -agonist treatment attenuates training-induced enhancements in exercise performance and maximal oxygen consumption, and alters muscle proteome signature and phenotype in trained young men...
January 15, 2018: Journal of Physiology
Johan Onslev, Glenn Jacobson, Christian Narkowicz, Vibeke Backer, Anders Kalsen, Michael Kreiberg, Søren Jessen, Jens Bangsbo, Morten Hostrup
PURPOSE: β2 -Agonists have been proposed as weight-loss treatment, because they elevate energy expenditure. However, it is unknown what effect β2 -agonists have on energy expenditure in overweight individuals. Furthermore, the influence of β2 -agonist R- and S-enantiomer ratio for the increased energy expenditure is insufficiently explored. METHODS: Nineteen males were included in the study of which 14 completed. Subjects were 31.6 (±3.5) years [mean (±95% CI)] and had a fat percentage of 22...
September 2017: European Journal of Applied Physiology
Glenn A Jacobson, Morten Hostrup, Christian K Narkowicz, David S Nichols, E Haydn Walters
Salmeterol (USAN, INN, BAN) is a long-acting beta2-adrenoceptor agonist (LABA) widely used in the treatment of airways disease. Although salmeterol is permitted via inhalation by athletes and supratherapeutic dosing may enhance performance, no urine threshold has been established by the World Anti-Doping Agency (WADA). Salmeterol is a chiral compound consisting of (R)- and (S)-enantiomers, normally administered as racemic (rac-) mixture via inhalation. Levels of rac-salmeterol in urine are often below detectable levels and there is surprisingly little information regarding the enantioselectivity of salmeterol pharmacokinetics...
August 2017: Drug Testing and Analysis
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
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
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
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
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...
December 2016: Sports Medicine
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
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
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
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
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
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
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
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
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
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
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
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