- |||||||||| fenoterol / Generic mfg.
Journal: ?2-Adrenergic Regulation of the Neuromuscular Transmission and Its Lipid-Dependent Switch. (Pubmed Central) - Aug 21, 2024
Using electrophysiological recordings and fluorescent FM dyes, we found that ?2-AR activation with fenoterol enhanced an involvement of synaptic vesicles in exocytosis and neurotransmitter release during intense activity at the neuromuscular junctions of mouse diaphragm...Sphingomyelin hydrolysis inversed the effects of ?2-AR agonist on neurotransmission probably via switching to Gi protein-dependent signaling. This phenomenon may reflect a dependence of the ?2-AR signaling on lipid raft integrity in the neuromuscular junctions.
- |||||||||| fenoterol / Generic mfg.
Prospective Testing Bronchial Obstruction Reversibility in Preterm Children: Inhaled betamimetics versus parasympatholytics (PS-18; Poster board no. 6) - May 31, 2024 - Abstract #ERS2024ERS_3165;
Following the administration of salbutamol, ipratropium, and ipratropium combined with fenoterol, significant improvements were observed in all spirometric parameters (p<0.000), except for FVC. The highest improvement of FEF25-75 and FEF75 z-score was observed after inhalation of ipratropium compared to salbutamol (p<0.005 and p<0.0017, respectively), but the difference between the combination of ipratropium plus fenoterol over ipratropium alone was not statistically significant (p<0.998 and p<0.54; ANOVA repeated measures).
- |||||||||| fenoterol / Generic mfg.
Cytokine Production profiles of CD4+ T cell subsets in stressed beta2-adrenergic receptor knockout and wildtype mice during Chlamydia muridarum genital infection (Exhibit Hall F1; Poster Board Number: B696) - Mar 29, 2024 - Abstract #IMMUNOLOGY2024IMMUNOLOGY_1553;
In vitro proliferation of CD4 T cells in the presence of b2-AR antagonists, ICI 118, 551 stimulated the production of Th1 cytokines, whereas b2-AR agonist, Fenoterol, decreased the production of Th1-type cytokines but increased GATA-3, STAT-6, IL-17, IL-10, b2-AR, decreased T-bet, and STAT-4 in CD4+ T cell productions during Chlamydia muridarum genital infection was observed. Overall, Th1 cytokine and T bet responses are reduced in stressed mice, suggesting that the cytokine status was polarized toward a Th2 immune response that can be restored by removing b2-AR from immune cells.
- |||||||||| prednisone / Generic mfg., fenoterol / Generic mfg.
Psyllium Husk (Metamucil) Induced Non-atopic Perennial Asthma: A Case Report (San Diego Convention Center, Area E (Hall A-B2, Ground Level)) - Feb 20, 2024 - Abstract #ATS2024ATS_6341;
Information about psyllium-induced asthma's long-term clinical manifestations is sparse. This case report of a patient followed for 30 years adds to this limited body of evidence, illustrating that a single Metamucil exposure can lead to life-long disabling and poorly controlled asthma in a patient without a history of asthma.
- |||||||||| fenoterol / Generic mfg.
Sales Trend Analysis of SABA, LABA/ICS and ICS Isolated in Brazil: A 2019-2022 Series (San Diego Convention Center, Area B (Hall A-B2, Ground Level)) - Feb 20, 2024 - Abstract #ATS2024ATS_996;
This case report of a patient followed for 30 years adds to this limited body of evidence, illustrating that a single Metamucil exposure can lead to life-long disabling and poorly controlled asthma in a patient without a history of asthma. Methods Data from the IQVIA
- |||||||||| ipratropium bromide / Generic mfg., fenoterol / Generic mfg.
Enrollment open, Trial completion date, Trial primary completion date: Bronchodilators on the Exercise Capacity of Bronchiectasis Patients (clinicaltrials.gov) - Dec 11, 2023
P=N/A, N=40, Enrolling by invitation,
Moreover, the proposed method has good stability and high accuracy; thus, it is suitable for the qualitative and quantitative determination of ?-agonists in animal meat. Suspended --> Enrolling by invitation | Trial completion date: Nov 2024 --> Nov 2025 | Trial primary completion date: Nov 2023 --> Nov 2024
- |||||||||| fenoterol / Generic mfg.
Trial completion, Enrollment change, Trial completion date: ASCENT: Beta 2 Adrenergic Stimulation vs Cold Exposure to Activate Human Brown Adipose Tissue (clinicaltrials.gov) - Sep 26, 2023
P1, N=12, Completed,
Suspended --> Enrolling by invitation | Trial completion date: Nov 2024 --> Nov 2025 | Trial primary completion date: Nov 2023 --> Nov 2024 Active, not recruiting --> Completed | N=20 --> 12 | Trial completion date: Jun 2023 --> Mar 2023
- |||||||||| Daliresp (roflumilast) / AstraZeneca, Takeda, AbbVie, Miostat (carbachol) / Novartis
Journal: Impact of the cAMP efflux and extracellular cAMP-adenosine pathway on airway smooth muscle relaxation induced by formoterol and phosphodiesterase inhibitors. (Pubmed Central) - Jul 14, 2023
We have shown that increment of intracellular cAMP induced by ?-adrenoceptors agonist fenoterol is followed by efflux of cAMP, which is converted by ecto-PDE and ecto-5'-nucleotidases (ecto-5'NT) to adenosine, leading to ASM contraction...Our results showed that ?-adrenoceptor agonists formoterol and PDE inhibitors IBMX, aminophylline and roflumilast induced cAMP efflux and a concentration-dependent relaxation of rat trachea precontracted with carbachol...These data showed that all bronchodilators tested were able to induce cAMP efflux. However, only ?-adrenoceptor-induced relaxation of tracheal smooth muscle was affected by cAMP efflux and extracellular cAMP adenosine pathway.
- |||||||||| fenoterol / Generic mfg.
Enrollment closed, Trial primary completion date: ASCENT: Beta 2 Adrenergic Stimulation vs Cold Exposure to Activate Human Brown Adipose Tissue (clinicaltrials.gov) - Apr 3, 2023
P1, N=20, Active, not recruiting,
However, only ?-adrenoceptor-induced relaxation of tracheal smooth muscle was affected by cAMP efflux and extracellular cAMP adenosine pathway. Recruiting --> Active, not recruiting | Trial primary completion date: Jun 2023 --> Mar 2023
- |||||||||| fenoterol / Generic mfg.
Journal: A comprehensive pharmacological analysis of fenoterol and its derivatives to unravel the role of ?-adrenergic receptor in zebrafish. (Pubmed Central) - Mar 2, 2023
(R,R)-MNFen displays the highest affinity for subtype B of zebrafish ?AR and modulation of this receptor might be associated with the development of malformations, increases locomotor activity and induces a negative chronotropic effect. Taken together, the presented data offer insights into the functional responses of the zebrafish ?ARs confirming their intraspecies conservation, and support the translation of the zebrafish model in pharmacological and toxicological research.
- |||||||||| fenoterol / Generic mfg.
Retrospective data, Review, Journal, Monotherapy: Safety of SABA Monotherapy in Asthma Management: a Systematic Review and Meta-analysis. (Pubmed Central) - Nov 10, 2022
Meta-analysis of data from RCTs showed that deaths were rare with SABA reliever monotherapy, and rates of SAEs and DAEs were comparable between SABA reliever and ICS treatment groups. When used appropriately within prescribed limits as reliever therapy, SABA does not contribute to excess rates of mortality, SAEs, or DAEs.
- |||||||||| fenoterol / Generic mfg.
Early Histopathological Changes of the Salivary Glands Associated with the Development of Primary Sjögren's Syndrome (Virtual Poster Hall) - Sep 17, 2022 - Abstract #ACRConvergence2022ACR_CONVERGENCE_3469;
We conclude that subtle damage of salivary epithelial cells concur in the activation of the mTOR pathway which is involved in the regulation of cell size, growth, proliferation and autophagy. These early changes in the mucous acini are sufficient to initiate B-cell infiltration and autoantibody response conditioning the appearance of Sjögren´s Syndrome-like manifestations in our murine model
- |||||||||| carvedilol / Generic mfg.
Journal: Impact of R-Carvedilol on β2-Adrenergic Receptor-Mediated Spontaneous Calcium Release in Human Atrial Myocytes. (Pubmed Central) - Jul 29, 2022
R-Carvedilol also reversed the fenoterol-induced phosphorylation of the RyR2 at Ser-2808 dose-dependently, and 1 µM of either R- or S-Carvedilol fully reversed the effect of fenoterol. Together, these findings demonstrate that β2-adrenergic stimulation alone stimulates RyR2 phosphorylation at Ser-2808 and spontaneous calcium release maximally, and points to carvedilol as a tool to attenuate the pathological activation of β2-receptors.
- |||||||||| ipratropium bromide / Generic mfg., fenoterol / Generic mfg.
Effects of acute bronchodilators on ventilatory constraint and dyspnoea during exercise in patients with pulmonary arterial hypertension (PAH) (TP-4 in thematic poster area) - Jun 22, 2022 - Abstract #ERS2022ERS_3737;
In a double-blind, randomized, single-dose and placebo-controlled study, 20 patients with PAH (18♀, 39.4 ± 12.3 yrs, FEV1/FVC= 0.80 ± 0.05, and mean pulmonary arterial pressure= 46.7 ± 15.8 mmHg) performed, at least 48hrs apart, high intensity (75% peak work rate) cycling exercise tests 1 hour after ipratropium+fenoterol MDI (BD) or placebo. The acute use of BD did not translate into improved ventilatory mechanics, dyspnoea perception, or exercise tolerance in patients with PAH.
- |||||||||| fenoterol / Generic mfg.
Journal: Diesel exhaust particles alter cAMP dynamics in human bronchial epithelial cells. (Pubmed Central) - May 14, 2022
Our findings suggest that DEP promotes oxidative stress, inflammation, and EMT. These profound alterations in cellular behavior were accompanied by changes in mitochondrial dysfunction and real-time cAMP dynamics, which may contribute to lung dysfunction induced by air pollution exposure.
- |||||||||| fenoterol / Generic mfg.
Characterization of immune cells of stressed beta2-adrenergic receptor homozygous knockout mouse model during Chlamydia muridarum genital infection (Exhibit Hall; P632) - Apr 8, 2022 - Abstract #IMMUNOLOGY2022IMMUNOLOGY_1281;
This study was undertaken to determine whether cold-induced stress (CIS) results in differential viability percent of immune cells β2-AR KO and WT C57BL/6J treated with NE, β2-AR agonist(Fenoterol), or antagonist(ICI 118,551), and patterns of cytokine production...The secretion of TNF-a by CD8+ cells and bone marrow cells treated with NE and β2-AR agonist or antagonist was high in all treatment groups. This study provides insights for the first time to better understand the NE-β2-AR pathway during chlamydia genital infection.
- |||||||||| sumatriptan succinate / Generic mfg.
Journal: Relationships between Inhibition, Transport and Enhanced Transport via the Organic Cation Transporter 1. (Pubmed Central) - Mar 16, 2022
Interestingly, OCT1 substrates exhibiting stronger OCT1 inhibition were mainly biaromatic β-agonistic drugs, such as dobutamine, fenoterol, ractopamine and ritodrine...Surprisingly, sumatriptan did significantly enhance dobutamine uptake...OCT1 transport stimulation was already observed earlier but is still poorly understood. Low OCT1 uptake inhibition and strong OCT1 efflux inhibition could be mechanisms exploitable for enhancing transport.
- |||||||||| fenoterol / Generic mfg.
Journal: Molecular basis for stereoselective transport of fenoterol by the organic cation transporters 1 and 2. (Pubmed Central) - Mar 3, 2022
Unlike for OCT1, both fenoterol enantiomers bind in the same region in OCT2 but in different conformations. Mutating THR246, predicted to interact with (S,S)-fenoterol in OCT2, led to an 11-fold decreased v. Altogether, our mutagenesis results correlate relatively well with our computational predictions and thereby provide an experimentally-corroborated hypothesis for the strong and contrasting enantiopreference in fenoterol uptake by OCT1 and OCT2.
- |||||||||| Ventavis (iloprost) / Bayer, J&J, University of Copenhagen
Journal: Inhibitory Potentiality of Secondary Metabolites Extracted from Marine Fungus Target on Avian Influenza Virus-A Subtype H5N8 (Neuraminidase) and H5N1 (Nucleoprotein): A Rational Virtual Screening. (Pubmed Central) - Jan 26, 2022
In case of drug prediction, the study recommends Estramustine and Iloprost against both nucleoprotein and neuraminidase. Besides these, Butorphanol, Desvenlafaxine, Zidovudine and Nadolol are the best drug candidates for nucleoprotein inhibitors, meanwhile, Sitaxentan, Ergoloid mesylate, Capecitabine and Fenoterol act as speculated candidates against neuraminidase.
- |||||||||| fenoterol / Generic mfg.
Journal: Short-acting inhaled β2-agonists: why, whom, what, how? (Pubmed Central) - Oct 7, 2021
Our work discusses major mechanisms of action, clinical effects, possible side effects and indications of inhaled SABA. We presented current recommendations for the position of SABA in the therapy of obstructive diseases in children and adults, particularly in asthma and chronic obstructive pulmonary disease.
- |||||||||| fenoterol / Generic mfg.
Clinical, Journal: Safety of bronchodilator reversibility test in elderly subjects: a prospective study. (Pubmed Central) - Aug 20, 2021
However, there was a significant increase in the number of supraventricular beats in the subjects who were not taking β-blockers. The use of 400 mg fenoterol in a bronchodilator reversibility test in elderly subjects does not entail any significant cardiovascular risk.
- |||||||||| propranolol / Generic mfg., fenoterol / Generic mfg.
Journal: Release of secretory immunoglobulin A by submandibular gland via β adrenergic receptor stimulation. (Pubmed Central) - Aug 18, 2021
The use of 400 mg fenoterol in a bronchodilator reversibility test in elderly subjects does not entail any significant cardiovascular risk. Stimulation of β receptors could result in more secretion of intracellularly accumulated sIgA compared with stimulation of other autonomic receptors in the autonomic modulation of mucosal immunity.
- |||||||||| Inavir (laninamivir) / Daiichi Sankyo, Rapivab (peramivir) / BioCryst, Relenza (zanamivir) / GSK, Vaxart
Journal: Quantitative structure-activity relationships, molecular docking and molecular dynamics simulations reveal drug repurposing candidates as potent SARS-CoV-2 main protease inhibitors. (Pubmed Central) - Aug 10, 2021
We simulated the stability of Acarbose-derived hexasaccharide, Naratriptan, Peramivir, Dihydrostreptomycin, Enviomycin, Rolitetracycline, Viomycin, Angiotensin II, Angiotensin 1-7, Angiotensinamide, Fenoterol, Zanamivir, Laninamivir and Laninamivir octanoate with 3CL by 100 ns and calculated binding free energy using molecular mechanics combined with Poisson-Boltzmann surface area (MM-PBSA)...Glu166 is a potential pharmacophore for drug design and inhibitors that interact with this residue may be critical to avoid dimerization of 3CL. Our results will contribute to future investigations of novel chemical scaffolds and the discovery of novel hits in high-throughput screening as potential anti-SARS-CoV-2 properties.Communicated by Ramaswamy H. Sarma.
- |||||||||| fenoterol / Generic mfg.
Journal: Chirality Effects in Biomolecular Systems: Calculation of the Relative Free Energies by Molecular Dynamics Simulations. (Pubmed Central) - Jun 22, 2021
In particular, we have proposed and tested the following strategies relying on the application of general, enhanced sampling (i) biased sampling in the two-dimensional space, along the coordinates defined by the values of the selected torsional angles; (ii) biased sampling in the one- or two-dimensional space, along the path-based coordinate(s); (iii) rational alteration of the system's Hamiltonian in order to enable the interconversion between stereoisomers and reweighting the biased distribution of configurations; (iv) using the free energy landscape generated within approaches (i) or (ii) as time-independent bias in order to further improve sampling efficiency and simultaneously account for multiple chiral centers. All approaches have been tested on a set of model compounds (fenoterol, fructofuranose and bromochlorofluoromethane), demonstrating the good performance but also some differences in the range of their applicabilities.
- |||||||||| sumatriptan succinate / Generic mfg.
Biomarker, Journal: Isobutyrylcarnitine as a Biomarker of OCT1 Activity and Interspecies Differences in its Membrane Transport. (Pubmed Central) - May 28, 2021
However, in contrast to mice, the mechanisms underlying the IBC-OCT1 correlation in humans is apparently not directly the OCT1-mediated efflux of IBC. A plausible explanation could be that hOCT1 mediates cellular concentrations of specific regulators or co-substrates in lipid and energy metabolism, which is supported by our in vitro finding that at baseline intracellular IBC concentration is about 6-fold lower alone by OCT1 overexpression.
- |||||||||| sumatriptan succinate / Generic mfg.
Journal: Effects of a Common Eight Base Pairs Duplication at the Exon 7-Intron 7 Junction on Splicing, Expression, and Function of OCT1. (Pubmed Central) - May 25, 2021
The 8 bp duplication was associated with a significant reduction of OCT1 expression in the human liver, but explained only 9% of the general variability in OCT1 expression and was not associated with significant changes in the pharmacokinetics of sumatriptan and fenoterol. Therefore, the rs35854239 variant only partially changes splicing, causing moderate changes in OCT1 expression and may be of only limited therapeutic relevance.
- |||||||||| HOKUNALIN patch (tulobuterol) / Maruho, Abbott
Journal: A highly selective and simple fluorescent probe for salbutamol detection based on thioglycolic acid-capped CdTe quantum dots. (Pubmed Central) - May 15, 2021
The quenching mechanism has been investigated by absorption spectroscopy and K at different temperatures, and shew a static quenching process than dynamic quenching. Under the optimal conditions, respectively the straight line equation (F/F = 0.1491 × 10 C + 1.3078) was found between the relative fluorescence intensity and the concentration of SAL was in the range of 6.27 × 10 to 2.09 × 10 mol L, and the limit of detection was 4.2 × 10 mol L. The proposed method has been applied to the determination of SAL in pig urine samples.
- |||||||||| metformin / Generic mfg., fenoterol / Generic mfg.
Review, Journal: Transport of Drugs and Endogenous Compounds Mediated by Human OCT1: Studies in Single- and Double-Transfected Cell Models. (Pubmed Central) - May 11, 2021
Due to the important role of OCT1 for the transport of endogenous compounds and drugs, in vitro cell systems are important for the determination of the substrate spectrum of OCT1, the understanding of the molecular mechanisms of polarized transport, and the investigation of potential drug-drug interactions. Therefore, the aim of this review article is to summarize the current knowledge on cell systems recombinantly overexpressing human OCT1.
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