Bambec (bambuterol) / Teva - LARVOL DELTA

Extensive electronic investigation of BMBH structure and adsorption locator on graphene with molecular dynamics of human serum albumin interaction. (PubMed, Sci Rep) - "A comprehensive electronic investigation of Bambuterol Hydrochloride (BMBH) was conducted to explore its structural properties, adsorption behavior on graphene, molecular docking interactions, and molecular dynamics perturbations...Additionally, molecular dynamics simulations were employed to evaluate the structural perturbations and dynamic behaviour of the BMBH/graphene and BMB/target complexes over time. The study offers a detailed understanding of the electronic and interactional properties of BMB, contributing to its potential applications in nanomaterial-based drug delivery and therapeutic interventions."

Journal • Alzheimer's Disease • CNS Disorders • Dementia

Evidence from a mouse model supports repurposing an anti-asthmatic drug, bambuterol, against Alzheimer's disease by administration through an intranasal route. (PubMed, Commun Biol) - "Indeed, even if the latter is more selective than other β2-mimetics towards bronchial β2-AR, cardiovascular effects (tachycardia, arrhythmias…) could occur upon cardiac β1-AR activation. Finally, intranasal administration of low doses of bambuterol gel in mice intoxicated with Aβ peptides, prevented long-term spatial memory impairment and showed beneficial effects on the survival of neurons and on synapse preservation."

Journal • Preclinical • Alzheimer's Disease • Asthma • Cardiovascular • CNS Disorders • Immunology • Respiratory Diseases

Determination of 13 potential anti-obesity agents in hair by dispersive liquid-liquid microextraction-assisted UHPLC-MS/MS. (PubMed, J Pharm Biomed Anal) - "The developed method successfully detected 13 anti-obesity agents within 11 min, including bambuterol, clenbuterol, ractopamine, clorprenaline, formoterol, salbutamol, terbutaline, procaterol, phentermine, bupropion, sibutramine, desmethyl sibutramine, and N,N-didesmethyl sibutramine, which improved the screening efficiency. The validated method was successfully applied to 369 real cases and detected six analytes, including bambuterol, salbutamol, terbutaline, sibutramine, desmethyl sibutramine, and N,N-didesmethyl sibutramine. This method offers several advantages, including simple pretreatment, high extraction efficiency, rapid extraction, solvent economy, and pollution mitigation, making it highly suitable for large-scale surveillance of usage of added anti-obesity agents."

Journal • Cardiovascular • Genetic Disorders • Obesity

Stability indicating eco-friendly quantitation of terbutaline and its pro-drug bambuterol using quantitative proton nuclear magnetic spectroscopy. (PubMed, BMC Chem) - "The method enables the assay of the two drugs in pure drug and pharmaceutical preparations. The method also enables the assay of the two drugs in the presence of each other; thus, it is considered a stability-indicating method where terbutaline is an acid degradation product of bambuterol."

Journal

Rivastigmine-Bambuterol Hybrids as Selective Butyrylcholinesterase Inhibitors. (PubMed, Molecules) - "Further investigations indicated that MTR-3 (IC > 100,000 nM, IC = 78 nM) was the best compound in the series, showing high butyrylcholinesterase selectivity and inhibition potency, the potential to permeate the blood-brain barrier, and longer-lasting BChE inhibition than bambuterol. These compounds could be used to discover novel specific BChE inhibitors for the treatment of Alzheimer's disease."

Journal • Alzheimer's Disease • CNS Disorders • Pain

Determination of 14 β-agonists in animal meat by ultra high performance liquid chromatography-tandem mass spectrometry (PubMed, Se Pu) - "In this study, a method based on ultra high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) was established for the rapid detection of 14 β-agonists (clenbuterol, salbutamol, ractopamine, clorprenaline, terbutaline, tulobuterol, bromobuterol, bambuterol, zilpaterol, mabuterol, fenoterol, arformoterol, cimaterol, and cimbuterol) in animal food sources. The results were close to those of the national standard method, indicating that the method is accurate and reliable. Moreover, the proposed method has good stability and high accuracy; thus, it is suitable for the qualitative and quantitative determination of β-agonists in animal meat."

Journal • Cardiovascular • Movement Disorders

Application of wastewater-based epidemiology to estimate the usage of beta-agonists in 31 cities in China. (PubMed, Sci Total Environ) - "Salbutamol, clorprenaline and terbutaline were observed in practically all wastewater samples at concentrations of up to several ng/L, whereas the formoterol and bambuterol concentrations were below the detection limit in all samples...Beta-agonist consumption based on WBE was higher in some cities than that based on medical survey data, indicating potential illegal use. These results show that WBE can be a straightforward and supplementary method for monitoring beta-agonist usage at the population level and spatially."

Journal

Idiopathic systemic capillary leak syndrome: a case report. (PubMed, BMC Nephrol) - "ISCLS is an extremely infrequent and commonly misdiagnosed disease. However, early diagnosis, treatment and prophylaxis through accumulated clinical data can prevent ISCLS recurrence and the development of related fatal complications. Therefore, clinicians need to be well aware of the variety of clinical characteristics and treatment options of this disease."

Journal • Acute Kidney Injury • Infectious Disease • Nephrology • Novel Coronavirus Disease • Pain • Rare Diseases • Renal Disease

Investigating the Effect of Silver Nanoparticles on the Fluorescence Intensity of Bambuterol and its Active Metabolite Terbutaline Using FRET. (PubMed, J Fluoresc) - "The estimated Stern-Volmer quenching constant at several temperature settings proved that the quenching mechanism of the two drugs was dynamic quenching in case of BAM while it was static quenching in case of TER. The number of binding sites, binding constants, and corresponding thermodynamic parameters depending on the interaction system were estimated at 293, 313, and 333 °K and the results obtained were interpreted."

Journal

Micelle-enhanced spectrofluorimetric method for the rapid determination of bronchodilator terbutaline and its prodrug bambuterol: Application for content uniformity test. (PubMed, Luminescence) - "The high sensitivity of the proposed approach allows its application in evaluating the content uniformity testing of the studied drugs in their tablets through using the official United States Pharmacopeia criteria (USP). Statistical analogies of the findings with that of the reported methods showed really good harmony and indicated no major differences in precision and accuracy."

Journal

(RS)-bambuterol and its enantiomers: Potential improvement of (R)-bambuterol in mice with colitis. (PubMed, Int Immunopharmacol) - "The efficacy of (R)-BMB was more notable than aminosalicylic acid (5-ASA). (R)-BMB is either butyrilcholinesterase inhibitor or β2AR agonist which offers new treatment of colitis."

Journal • Preclinical • Asthma • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Pulmonary Disease • Respiratory Diseases • Ulcerative Colitis • IL17A • IL6

Identification of Compounds for Butyrylcholinesterase Inhibition. (PubMed, SLAS Discov) - "From the primary screening, we identified a group of 125 compounds that were further confirmed to inhibit BChE activity, including previously reported BChE inhibitors (e.g., bambuterol and rivastigmine) and potential novel BChE inhibitors (e.g., pancuronium bromide and NNC 756), representing diverse structural classes. The binding modes of these compounds were further studied using molecular docking analyses to identify the differences between the interactions of these BChE inhibitors within the active sites of AChE and BChE. Our qHTS approach allowed us to establish a robust and reliable process to screen large compound collections for potential BChE inhibitors."

Journal • Alzheimer's Disease • CNS Disorders • Pain

Enhancement of Fear Extinction Memory and Resistance to Age-Related Cognitive Decline in Butyrylcholinesterase Knockout Mice and (R)-Bambuterol Treated Mice. (PubMed, Biology (Basel)) - "In conclusion, this study found that inhibition of BChE ameliorated episodic and spatial memories. This study also suggested that (R)-bambuterol as a BChE inhibitor has the potential application in the treatment of post-traumatic stress disorder (PTSD) and early cognitive decline."

Journal • Preclinical • Alzheimer's Disease • CNS Disorders • Mood Disorders • Post-traumatic Stress Disorder • Solid Tumor

Rapid Detection of Ractopamine and Salbutamol in Swine Urine by Immunochromatography Based on Selenium Nanoparticles. (PubMed, Int J Nanomedicine) - "No cross-reaction occurred with clenbuterol, bambuterol and phenylethanolamine A. Samples were tested consistently across different batches of kits for swine urine...It is easy to operate, sensitive, specific, and stable This kit is suitable for the rapid and real-time detection of RAC and SAL residues in swine urine samples. Swine urines samples were used under approval from the Experimental Animal Ethics committee of the Joint National Laboratory for Antibody Drug Engineering, Henan University."

Journal

Quick simultaneous analysis of bambuterol and montelukast based on synchronous spectrofluorimetric technique. (PubMed, R Soc Open Sci) - "Additionally, the validation criteria were assessed in accordance with International Council of Harmonization (ICH) guidelines. The method was used for the estimation of both drugs in their raw materials, synthetic mixtures as well their combined tablets with good agreement between its results and those from the comparison method."

Journal

G protein-coupled receptor-in-paper, a versatile chromatographic platform to study receptor-drug interaction. (PubMed, J Chromatogr A) - "The association constants of salbutamol, terbutaline and bambuterol to β-AR were calculated to be 2.02 × 10 M, 1.15 × 10 M, 1.75 × 10 M by adsorption energy distribution, which were in good line with the values from frontal analysis, zonal elution and previous literatures. We demonstrated that the GPCR-in-paper platform was cost-effective, easy to be modified for protein immobilization, and applicable in the receptor-drug interaction analysis. We believe such a platform sheds new light on paper chromatography for receptor-drug interaction analysis and other applications."

Journal

β2- Adrenergic Signaling Regulates Graft Versus Host Disease after Allogenic Transplantation While Preserving Graft Versus Leukemia Effect (ASH 2019) - "There was no difference in BP and HR at day 21 and 28 after allo-HCT between mice receiving Bambuterol compared to mice receiving vehicle. In conclusion, these data reveal how β-AR signaling can influence donor T cell differentiation and function in murine GvHD models without decreasing GvL effect pointing to the feasibility of manipulation of β2-AR signaling to ameliorate clinical GvHD."

Graft versus Host Disease • Hematological Disorders • Hematological Malignancies • Leukemia • Oncology • Transplantation • CD44 • FOXP3 • IFNG • IL10 • IL17A

β2-adrenergic receptor activation on donor cells ameliorates acute GvHD. (PubMed, JCI Insight) - "Bambuterol preserved the GvT effect by inducing NKG2D+ effector cells and central memory T cells. These data reveal how β-AR signaling can be targeted to ameliorate GvHD severity while preserving GvT effect."

Journal • Graft versus Host Disease • Transplantation • NKG2D

Interactions of Paraoxonase-1 with Pharmacologically Relevant Carbamates. (PubMed, Molecules) - "Carbamates were selected having a variety of applications: bambuterol and physostigmine are drugs, carbofuran is used as a pesticide, while Ro 02-0683 is diagnostic reagent...Molecular modelling of rePON1-carbamate complexes suggested non-covalent interactions with residues of the rePON1 active site that could lead to competitive inhibition of its arylesterase activity. In conclusion, carbamates can reduce the level of PON1 activity, which should be kept in mind, especially in medical conditions characterized by reduced PON1 levels."

Journal

Reversible and site-specific immobilization of β-adrenergic receptor by aptamer-directed method for receptor-drug interaction analysis. (PubMed, J Chromatogr A) - "Salbutamol, methoxyphenamine, ephedrine hydrochloride, clorprenaline, tulobuterol, bambuterol, propranolol and ICI 118551 bound to the receptor through one type of binding sites. The association constants presented good agreement within the three methods but exhibited clear differences from the data by radio-ligand binding assay. Regarding these results, we concluded that the aptamer-directed method will probably become an alternative for reversible and site-specific immobilization of GPCRs directly from complex matrices; the immobilized receptor is qualitative for drug-receptor interaction analysis."

Journal

Detection of β-agonists in pork tissue with novel electrospun nanofibers-based solid-phase extraction followed ultra-high performance liquid chromatography/tandem mass spectrometry. (PubMed) - Food Chem - "A selective analytical method based on packed-fiber solid-phase extraction and ultra-high performance liquid chromatography-tandem mass spectrometry (PFSPE-UPLC-MS/MS) has been developed for determination of six β-agonists (clorprenaline, bambuterol, clenbuterol, brombuterol, mabuterol, and penbuterol) in pork tissue...Above all, only 5mg of sorbent and 200μL of elution solvent were favorable to directly extract all analytes in a complex matrix. The method is simple and cost-effective, and has the potential to be applied to quantitatively analyze the concentrations of polar species in food samples containing complex matrix."

Journal • Biosimilar

Determinants of response to bronchodilator in patients with cough variant asthma- A randomized, single-blinded, placebo-controlled study. (PubMed, Pulm Pharmacol Ther) - "More than one-third of patients with CVA do not respond to bronchodilator treatment, indicating that the response to bronchodilator should not be a diagnostic requirement of CVA. CVA patients with higher airway responsiveness will more likely respond to bronchodilator. Cough of CVA might be elicited by different mechanisms, which suggests that CVA could be divided into two phenotypes according to the response to bronchodilators."

Clinical • Journal

Design, synthesis and biological evaluation of novel carbamates as potential inhibitors of acetylcholinesterase and butyrylcholinesterase. (PubMed, Bioorg Med Chem) - "Rivastigmine, a dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), has been approved by U.S. Food and Drug Administration to treat Alzheimer's disease (AD) and Parkinson's disease (PD) dementia. In the current work, a bambuterol derivative lacking one of the carbamoyloxy groups on the benzene ring (BMC-1) and its analogues were synthesized using 1-(3-hydroxyphenyl) ethan-1-one and 1-(4-hydroxyphenyl) ethan-1-one as starting materials...Further study confirmed that among the nine carbamates, BMC-3 (IC = 792 nM, IC = 2.2 nM) and BMC-16 (IC = 266 nM, IC = 10.6 nM) were excellent cholinesterase inhibitors with potential of permeating through the blood-brain barrier. These carbamates could be used as potential dual inhibitors of AChE and BChE and to discover novel drugs for the treatment of AD and PD dementia."

Journal

Response to Bronchodilator and Clinical, Pathophysiological Features in Patients with Nonasthmatic Eosinophilic Bronchitis. (PubMed, Clin Respir J) - "One third of patients with NAEB respond well to bronchodilator treatment, which are related wtih lower cough reflex sensitivity and increased airway responsiveness. The relationship between NAEB and asthma needs to be investigated further."

Clinical • Journal

Impurity profile of bronchodilators used in asthma: A critical review. (PubMed, Curr Drug Discov Technol) - "After a thorough literature search, LC-MS and LC-MS-NMR techniques are found most useful for impurity profiling. In future, LC-DAD-NMR-MS, CE-ESI-FT-ICR-MS can also be explored for the isolation and characterization of impurities."

Journal