Database : MEDLINE
Search on : D02.033.100.291.905 [DeCS Category]
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PMID:28719816
Author:Zhou L; Sleiman M; Ferronato C; Chovelon JM; de Sainte-Claire P; Richard C
Address:Univ Lyon, Université Claude Bernard Lyon 1, CNRS, IRCELYON, F-69626, 2 Avenue Albert Einstein, Villeurbanne, France; Université Clermont Auvergne, CNRS, Sigma-Clermont, Institut de Chimie de Clermont-Ferrand, F-63178, Aubière, France.
Title:Sulfate radical induced degradation of ß2-adrenoceptor agonists salbutamol and terbutaline: Phenoxyl radical dependent mechanisms.
Source:Water Res; 123:715-723, 2017 Oct 15.
ISSN:1879-2448
Country of publication:England
Language:eng
Abstract:The present study investigated the reactivity and oxidation mechanisms of salbutamol (SAL) and terbutaline (TBL), two typical ß2-adrenoceptor agonists, towards sulfate radical (SO ) by using photo-activated persulfate (PS). The reaction pathways and mechanisms were proposed based on products identification using high resolution HPLC-ESI-MS, laser flash photolysis (LFP) and molecular orbital calculations. The results indicated that SO was the dominant reactive species in the UV/PS process. The second-order rate constants of sulfate radical reaction with SAL and TBL were measured as (3.7 ± 0.3) × 10 and (4.2 ± 0.3) × 10 M s by LFP, respectively. For both SAL and TBL, phenoxyl radicals were found to play key roles in the orientation of the primary pathways. For SAL, a benzophenone derivative was generated by oxidation of the phenoxyl radical. However, in the case of TBL, the transformation of the phenoxyl radical into benzoquinone was impossible. Instead, the addition of OSO H on the aromatic ring was the major pathway. The same reactivity pattern was observed in the case of TBL structural analogs resorcinol and 3,5-dihydroxybenzyl alcohol. Our results revealed that basic conditions inhibited the decomposition of SAL and TBL, while, increasing PS dose enhanced the degradation. The present work could help for a better understanding of the difference in oxidation reactivity of substituted phenols widely present in natural waters.
Publication type:JOURNAL ARTICLE
Name of substance:0 (Adrenergic Agonists); 0 (Phenols); 0 (Sulfates); 0 (sulfate radical); 3229-70-7 (phenoxy radical); N8ONU3L3PG (Terbutaline); QF8SVZ843E (Albuterol)


  2 / 3030 MEDLINE  
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PMID:28710773
Author:Carvajal Gonczi CM; Tabatabaei Shafiei M; East A; Martire E; Maurice-Ventouris MHI; Darlington PJ
Address:The Center for Structural and Functional Genomics, Concordia University, Montreal, QC, Canada.
Title:Reciprocal modulation of helper Th1 and Th17 cells by the ß2-adrenergic receptor agonist drug terbutaline.
Source:FEBS J; 284(18):3018-3028, 2017 Sep.
ISSN:1742-4658
Country of publication:England
Language:eng
Abstract:Catecholamine hormones are powerful regulators of the immune system produced by the sympathetic nervous system (SNS). They regulate the adaptive immune system by altering T-cell differentiation into T helper (Th) 1 and Th2 cell subsets, but the effect on Th17 cells is not known. Th17 cells, defined, in part, by chemokine receptor CCR6 and cytokine interleukin (IL)-17A, are crucial for mediating certain pathogen-specific responses and are linked with several autoimmune diseases. We demonstrated that a proportion of human Th17 cells express beta 2-adrenergic receptor (ß2AR), a G protein-coupled receptor that responds to catecholamines. Activation of peripheral blood mononuclear cells, which were obtained from venous blood drawn from healthy volunteers, with anti-cluster of differentiation 3 (CD3) and anti-CD28 and with a ß2-agonist drug, terbutaline (TERB), augmented IL-17A levels (P < 0.01) in the majority of samples. TERB reduced interferon gamma (IFNγ) indicating that IL-17A and IFNγ are reciprocally regulated. Similar reciprocal regulation was observed with dbcAMP. Proliferation of Th cells was monitored by carboxyfluorescein diacetate N-succinimidyl ester labeling and flow cytometry with antibody staining for CD3 and CD4. TERB increased proliferation by a small but significant margin (P < 0.001). Next, Th17 cells (CD4 CXCR3 CCR6 ) were purified using an immunomagnetic positive selection kit, which removes all other mononuclear cells. TERB increased IL-17A from purified Th17 cells, which argues that TERB acts directly on Th17 cells. Thus, hormone signals from the SNS maintain a balance of Th cells subtypes through the ß2AR.
Publication type:JOURNAL ARTICLE
Name of substance:0 (Adrenergic beta-2 Receptor Agonists); 0 (Antibodies, Monoclonal); 0 (CD28 Antigens); 0 (CD3 Complex); 0 (IL17A protein, human); 0 (Interleukin-17); 0 (Receptors, Adrenergic, beta-2); 63X7MBT2LQ (Bucladesine); 82115-62-6 (Interferon-gamma); N8ONU3L3PG (Terbutaline)


  3 / 3030 MEDLINE  
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PMID:28602874
Author:Pineton de Chambrun M; Gousseff M; Mauhin W; Lega JC; Lambert M; Rivière S; Dossier A; Ruivard M; Lhote F; Blaison G; Alric L; Agard C; Saadoun D; Graveleau J; Soubrier M; Lucchini-Lecomte MJ; Christides C; Bosseray A; Levesque H; Viallard JF; Tieulie N; Lovey PY; Le Moal S; Bibes B; Malizia G; Abgueguen P; Lifermann F; Ninet J; Hatron PY; Amoura Z; EurêClark Study Group
Address:Service de médecine interne 2, CHU La Pitié-Salpêtrière, APHP, Université Paris 6, France; Service de réanimation médicale, CHU La Pitié-Salpêtrière, APHP, Université Paris 6, France.
Title:Intravenous Immunoglobulins Improve Survival in Monoclonal Gammopathy-Associated Systemic Capillary-Leak Syndrome.
Source:Am J Med; 130(10):1219.e19-1219.e27, 2017 Oct.
ISSN:1555-7162
Country of publication:United States
Language:eng
Abstract:BACKGROUND: Monoclonal gammopathy-associated systemic capillary-leak syndrome, also known as Clarkson disease, is a rare condition characterized by recurrent life-threatening episodes of capillary hyperpermeability in the context of a monoclonal gammopathy. This study was conducted to better describe the clinical characteristics, natural history, and long-term outcome of monoclonal gammopathy-associated systemic capillary-leak syndrome. METHODS: We conducted a cohort analysis of all patients included in the European Clarkson disease (EurêClark) registry between January 1997 and March 2016. From diagnosis to last follow-up, studied outcomes (eg, the frequency and severity of attacks, death, and evolution toward multiple myeloma) and the type of preventive treatments administered were monitored every 6 months. RESULTS: Sixty-nine patients (M/F sex ratio 1:1; mean ± SD age at disease onset 52 ± 12 years) were included in the study. All patients had monoclonal gammopathy of immunoglobulin G type, with kappa light chains in 47 (68%). Median (interquartile range) follow-up duration was 5.1 (2.5-9.7) years. Twenty-four patients (35%) died after 3.3 (0.9-8) years. Fifty-seven (86%) patients received at least one preventive treatment, including intravenous immunoglobulins (IVIg) n = 48 (73.8%), theophylline n = 22 (33.8%), terbutaline n = 22 (33.8%), and thalidomide n = 5 (7.7%). In the 65 patients with follow-up, 5- and 10-year survival rates were 78% (n = 35) and 69% (n = 17), respectively. Multivariate analysis found preventive treatment with IVIg (hazard ratio 0.27; 95% confidence interval, 0.10-0.70; P = .007) and terbutaline (hazard ratio 0.35; 95% confidence interval, 0.13-0.96; P = .041) to be independent predictors of mortality. CONCLUSIONS: We describe the largest cohort to date of patients with well-defined monoclonal gammopathy-associated systemic capillary-leak syndrome. Preventive treatment with IVIg was the strongest factor associated with survival, suggesting the use of IVIg as the first line in prevention therapy.
Publication type:JOURNAL ARTICLE
Name of substance:0 (Immunoglobulins, Intravenous); C137DTR5RG (Theophylline); N8ONU3L3PG (Terbutaline)


  4 / 3030 MEDLINE  
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PMID:28427362
Author:Jenkins CR; Eriksson G; Bateman ED; Reddel HK; Sears MR; Lindberg M; O'Byrne PM
Address:Department of Thoracic Medicine, Concord Hospital and The George Institute for Global Health, PO Box M201, Missenden Rd, Sydney, NSW, 2050, Australia. christine.jenkins@sydney.edu.au.
Title:Efficacy of budesonide/formoterol maintenance and reliever therapy compared with higher-dose budesonide as step-up from low-dose inhaled corticosteroid treatment.
Source:BMC Pulm Med; 17(1):65, 2017 Apr 20.
ISSN:1471-2466
Country of publication:England
Language:eng
Abstract:BACKGROUND: Asthma management may involve a step up in treatment when symptoms are not well controlled. We examined whether budesonide/formoterol maintenance and reliever therapy (MRT) is as effective as higher, fixed-dose budesonide plus as-needed terbutaline in patients requiring step-up from Step 2 treatment (low-dose inhaled corticosteroids), stratified by baseline reliever use. METHODS: A post-hoc analysis utilized data from three clinical trials of 6-12 months' duration. Patients aged ≥12 years with symptomatic asthma uncontrolled despite Step 2 treatment were included. Severe exacerbation rate, lung function and reliever use were analysed, stratified by baseline reliever use (<1, 1-2 and >2 occasions/day). RESULTS: Overall, 1239 patients were included. Reductions in severe exacerbation rate with budesonide/formoterol MRT versus fixed-dose budesonide were similar across baseline reliever use levels, and were statistically significant in patients using 1-2 (42%, p = 0.01) and >2 (39%, p = 0.02) reliever occasions/day, but not <1 reliever occasion/day (35%, p = 0.11). Both treatments significantly increased mean FEV from baseline; improvements were significantly greater for budesonide/formoterol MRT in all reliever use groups. Reductions in reliever use from baseline were significantly greater with budesonide/formoterol MRT versus fixed-dose budesonide in patients using 1-2 and >2 reliever occasions/day (-0.33 and -0.74 occasions/day, respectively). CONCLUSIONS: Treatment benefit with budesonide/formoterol MRT versus higher, fixed-dose budesonide plus short-acting ß -agonist was found in Step 2 patients with relatively low reliever use, supporting the proposal that budesonide/formoterol MRT may be useful when asthma is uncontrolled with low-dose inhaled corticosteroid.
Publication type:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
Name of substance:0 (Adrenal Cortex Hormones); 0 (Adrenergic beta-2 Receptor Agonists); 0 (Anti-Asthmatic Agents); 0 (Drug Combinations); 51333-22-3 (Budesonide); N8ONU3L3PG (Terbutaline); W34SHF8J2K (Formoterol Fumarate)


  5 / 3030 MEDLINE  
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PMID:28409497
Author:Szucs KF; Grosz G; Süle M; Nagy A; Tiszai Z; Samavati R; Gáspár R
Title:Identification of myoelectric signals of pregnant rat uterus: new method to detect myometrial contraction.
Source:Croat Med J; 58(2):141-148, 2017 Apr 14.
ISSN:1332-8166
Country of publication:Croatia
Language:eng
Abstract:AIM: To develop an electromyography method for pregnant rat uterus in vivo and to separate myometrial signals from the gastrointestinal tract signals. METHODS: Pregnant Sprague-Dawley rats (n=8) were anaesthetized and their stomach, small intestine, and large intestine were removed from the abdomen. A pair of thread electrodes was inserted into the uterus, while a pair of disk electrodes was placed subcutaneously above the myometrium. Additionally, a strain gauge sensor was fixed on the surface of the myometrium and cecum for the parallel detection of mechanical contractions in rats (n=18) with intact gastrointestinal tract. The filtered electric signals were amplified and recorded by an online computer system and analyzed by fast Fourier transformation. The frequency of the electric activity was characterized by cycle per minute (cpm), the magnitude of the activity was described as power spectrum density maximum (PsDmax). RESULTS: The frequency of the pregnant uterine activity was 1-3 cpm, which falls within the same range as that of cecum. Measuring by both electrodes, oxytocin (1 µg/kg) increased and terbutaline (50 µg/kg) decreased the PsDmax by 25%-50% (P<0.001) and 25%-40% (P<0.01), respectively. We found a strong positive correlation between the alterations of PsDmax values and the strain gauge sensor-detected mechanical contractions (area under curve). The GI specific compounds (neostigmine, atropine) mainly affected the cecal activity, while myometrium specific drugs (oxytocin, terbutaline) influenced the myometrial signals only. Conclusion Our method proved to be able to detect the myoelectric activity that reflects the mechanical contraction. The overlapping myometrial and cecal signals are not separable, but they can be distinguished based on the much higher activity and different pharmacological reactivity of the pregnant uterus. Thus, the early signs of contractions can be detected and labor may be predicted in a fast and sensitive way.
Publication type:JOURNAL ARTICLE
Name of substance:50-56-6 (Oxytocin); N8ONU3L3PG (Terbutaline)


  6 / 3030 MEDLINE  
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PMID:28381680
Author:Uchimoto H; Ikeda M; Tanida S; Ohhashi K; Chihara Y; Shigeta T; Arimitsu K; Yamashita M; Nishide K; Kawasaki I
Address:School of Pharmaceutical Sciences, Mukogawa Women's University.
Title:Green Synthesis of (R)-Terbutaline for Recyclable Catalytic Asymmetric Transfer Hydrogenation in Ionic Liquids.
Source:Chem Pharm Bull (Tokyo); 65(4):389-395, 2017.
ISSN:1347-5223
Country of publication:Japan
Language:eng
Abstract:We synthesize optically active (R)-terbutaline 2, which is an anti-asthmatic drug, through recyclable catalytic asymmetric transfer hydrogenation (RCATH). Various chloroketones 4 were prepared and RCATH was performed on them. The products exhibit moderate to high enantioselectivity. In particular, the hydrogenation of acyl substituted substrates 4c yields chiral secondary alcohols 5c in good yield and enantioselectivity. Furthermore, (R)-terbutaline 2 can be synthesized in one step from the resulting secondary alcohol 5 without racemization.
Publication type:JOURNAL ARTICLE
Name of substance:0 (Anti-Asthmatic Agents); 0 (Ionic Liquids); N8ONU3L3PG (Terbutaline)


  7 / 3030 MEDLINE  
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PMID:28062365
Author:Pourchez J; de Oliveira F; Perinel-Ragey S; Basset T; Vergnon JM; Prévôt N
Address:Ecole Nationale Supérieure des Mines de Saint-Etienne, CIS-EMSE, SAINBIOSE, F-42023 Saint Etienne, France; INSERM, U1059, F-42023 Saint Etienne, France; Université de Lyon, F-69000 Lyon, France. Electronic address: pourchez@emse.fr.
Title:Assessment of new-generation high-power electronic nicotine delivery system as thermal aerosol generation device for inhaled bronchodilators.
Source:Int J Pharm; 518(1-2):264-269, 2017 Feb 25.
ISSN:1873-3476
Country of publication:Netherlands
Language:eng
Abstract:PURPOSE: A need remains for alternative devices for aerosol drug delivery that are low cost, convenient and easy to use for the patient, but also capable of producing small-sized aerosol particles. This study investigated the potential of recent high power electronic nicotine delivery systems (ENDS) as aerosol generation devices for inhaled bronchodilators. METHODS: The particle size distribution was measured using a cascade impactor. The delivery of terbutaline sulfate, a current bronchodilator used for asthma or COPD therapy by inhalation, was studied. This drug was quantified by liquid chromatography coupled with tandem mass spectrometry. RESULTS: The particle size distribution in terms of mass frequency (in two ways, gravimetrically and quantitatively through drug assay on each stage) and the terbutaline sulfate concentration in the aerosol were elucidated. The mass median aerodynamic diameter (MMAD) and the drug delivery rose when the power level increased, to reach 5.6±0.4µg/puff with a MMAD of 0.78±0.03µm at 25W. CONCLUSION: New generation high-power ENDS are very efficient to generate carrier-droplets in the submicron range containing drug molecules with a constant drug concentration whatever the size-fractions. ENDS appear to be highly patient-adaptive.
Publication type:JOURNAL ARTICLE
Name of substance:0 (Aerosols); 0 (Bronchodilator Agents); 6M3C89ZY6R (Nicotine); N8ONU3L3PG (Terbutaline)


  8 / 3030 MEDLINE  
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PMID:27744187
Author:Wu J; Tian Y; Wang S; Pistolozzi M; Jin Y; Zhou T; Roy G; Xu L; Tan W
Address:School of Bioscience and Bioengineering, South China University of Technology, Guangzhou, Guangdong, People's Republic of China; Pre-Incubator for Innovative Drug and Medicine, South China University of Technology, Guangzhou, Guangdong, People's Republic of China.
Title:Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
Source:Eur J Med Chem; 126:61-71, 2017 Jan 27.
ISSN:1768-3254
Country of publication:France
Language:eng
Abstract:An increase activity of butyrylcholinesterase is believed to contribute to Alzheimer's disease. Bambuterol is a known potent inhibitor of butyrylcholinesterase, but it has undesired cardiac effects and less lipophilicity. Thirteen bambuterol analogues were synthesized using 1-(3, 5-dihydroxyphenyl) ethanone as a starting material. In-vitro cholinesterase assay established that the majority of the compounds are specific butyrylcholinesterase inhibitors. Out of the 13 compounds, two bambuterol derivatives, BD-6 and BD-11 exhibited similar efficacies in inhibiting butyrylcholinesterase with fewer effects on heart and enhanced possibilities of permeating through the blood-brain barrier as compared to bambuterol. These bambuterol analogues may provide better alternatives for treatments of Alzheimer's disease.
Publication type:JOURNAL ARTICLE
Name of substance:0 (Cholinesterase Inhibitors); EC 3.1.1.7 (Acetylcholinesterase); EC 3.1.1.8 (Butyrylcholinesterase); N8ONU3L3PG (Terbutaline); Y1850G1OVC (bambuterol)


  9 / 3030 MEDLINE  
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PMID:27718262
Author:Inoue H; Niimi A; Matsumoto H; Ito I; Oguma T; Otsuka K; Takeda T; Nakaji H; Tajiri T; Iwata T; Nagasaki T; Mishima M
Address:Department of Respiratory Medicine, Graduate School of Medicine, Kyoto University, Kyoto, Japan.
Title:A 12-week, randomized, parallel-group, proof-of-concept study of tulobuterol patch and salmeterol inhaler as add-on therapy in adult-onset mild-to-moderate asthma.
Source:Clin Exp Pharmacol Physiol; 44(1):21-29, 2017 Jan.
ISSN:1440-1681
Country of publication:Australia
Language:eng
Abstract:Patch formulation of tulobuterol has been used in asthma treatment as a long-acting ß -agonist (LABA) through sustained skin absorption. Its treatment efficacy, especially in small airways, remains poorly understood. The study aim was to investigate LABA add-on effects of tulobuterol patch (TP) and salmeterol inhaler (SA) on pulmonary function, asthma control and health status. Patients who had adult-onset under-control asthma, despite taking inhaled corticosteroids, were enrolled in a randomized, open-label, parallel-group, proof-of-concept study of 12-week add-on treatment with TP (n=16) or SA (n=17). Spirometry, impulse oscillometry (IOS), exhaled nitric oxide levels, and clinical questionnaires of asthma control, health status (St. George's Respiratory Questionnaire: SGRQ), and symptoms were evaluated every 4 weeks. Add-on treatment of SA significantly improved the spirometric indices of small airway obstruction (forced expiratory flow between 25% and 75% of FVC: FEF , and maximum expiratory flow at 25% of FVC: MEF ) and IOS indices of whole respiratory resistance (resistance at 5 Hz) as compared to TP. In intra-group comparisons, add-on treatment of TP improved the scores of the asthma control test and the total SGRQ, as well as the symptom and impact components of the SGRQ. SA add-on treatment improved FEV and IOS parameters of resistance at 20 Hz and reactance at 5 Hz. Neither of the treatments improved exhaled nitric oxide levels. In conclusion, add-on treatment of TP improved asthma control and health status, whereas SA improved pulmonary function measures associated with large and small airway involvement among patients with adult-onset mild-to-moderate asthma.
Publication type:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
Name of substance:0 (Bronchodilator Agents); 591I9SU0F7 (tulobuterol); 6EW8Q962A5 (Salmeterol Xinafoate); N8ONU3L3PG (Terbutaline)


  10 / 3030 MEDLINE  
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PMID:27589403
Author:Zhou Y; Wang P; Xiong J; Yue H; He Y; Ouyang H; Wang L; Fu Z
Address:Key Laboratory of Luminescence and Real-Time Analytical Chemistry (Southwest University), Ministry of Education, College of Pharmaceutical Sciences, Southwest University, Chongqing 400716, China.
Title:A label-free strategy for measuring the affinity between monoclonal antibody and hapten using microdialysis sampling combined with chemiluminescent detection.
Source:Biosens Bioelectron; 87:404-409, 2017 Jan 15.
ISSN:1873-4235
Country of publication:England
Language:eng
Abstract:It is of great importance to measure antibody affinity in the course of screening monoclonal antibody (McAb) for immunotherapy, immunoassay and immunological purification. Herein, by using terbutaline mouse McAb as a model, a novel label-free strategy based on on-line microdialysis (MD) sampling combined with flow injection chemiluminescent detection was designed for measuring antibody affinity to hapten in a homogeneous system. After this McAb incubated with its hapten, the unbound hapten was sampled on-line by the MD probe and injected into the chemiluminescent detection system for quantification. The obtained concentrations of the unbound hapten were treated with Scatchard analysis and Klotz analysis to calculate the affinity constant. The MD probe showed a recovery of 26.2% for terbutaline under the chosen conditions. The affinity constants obtained using Scatchard analysis and Klotz analysis were 4.9×10 M and 4.9×10 M , respectively, showing negligible difference. The obtained affinity constants indicated that the investigated McAb was an antibody with medium affinity. The designed strategy provided a simple, rapid and low-cost approach for direct measurement of antibody affinity. Furthermore, it avoided the decrease of affinity, which was encountered frequently in the conventional approaches based on probe labeling of McAb and protein conjugation of hapten.
Publication type:JOURNAL ARTICLE
Name of substance:0 (Antibodies, Monoclonal); 0 (Haptens); N8ONU3L3PG (Terbutaline)



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