fenoterol / Generic mfg. - LARVOL DELTA

Beta2-adrenergic stimulation by fenoterol increases energy expenditure without activating human brown adipose tissue. (PubMed, Cell Metab) - "RNA sequencing (RNA-seq) analysis of human BAT revealed that the expression of beta3-AR, but not of beta2-AR, correlates with the expression of UCP1, the hallmark of thermogenic brown adipocytes. Our data indicate that the beta2-AR is not the main activating receptor of human BAT and suggest that beta2-AR agonism increases EE in tissues other than BAT."

Journal • Metabolic Disorders

Role of myometrial relaxants (acute tocolytics) in intrauterine fetal resuscitation at term: why, when, what, How, and why-not? (PubMed, J Matern Fetal Neonatal Med) - "Based on current evidence, and pharmacokinetics, 250 mcg of subcutaneous terbutaline (or another beta-sympathomimetic such as intravenous fenoterol) is the recommended first line tocolytic, unless there are specific maternal contraindications. In the absence of maternal hypotension, 100 mg of intravenous glyceryl trinitrate (GTN) may be administered as an alternative. Acute tocolytics are not recommended to treat myometrial irritability observed in chorioamnionitis or in acute feto-maternal hemorrhage."

Journal • Review • Hematological Disorders • Hypotension

Agonist-specific conformational dynamics at the β2-adrenoceptor dictate allosteric modulation of Gαs signalling and bronchodilation. (PubMed, Br J Pharmacol) - "These findings establish orthosteric ligand-dependent allostery as a fundamental feature of β2AR pharmacology. PAM37 represents a tool to selectively enhance bronchodilation by β-agonists in asthma."

Journal • Asthma • Immunology • Pulmonary Disease • Respiratory Diseases

An advanced GC method for comprehensive residual solvent analysis: overcoming co-elution with orthogonal columns and quantification by mass spectrometry. (PubMed, Anal Methods) - "The real sample applicability was confirmed through analysis of a spiked fenoterol hydrobromide sample, establishing the method's robustness and suitability for testing the 57 residual solvents in pharmaceutical matrices. Additional evaluation with verapamil hydrochloride, amitriptyline hydrochloride, and their commercial formulations (tablets) further validated its broad applicability."

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Development and validation of an LC-MS/MS/MS method for the sensitive quantification of trace β-agonists in complex animal-derived food matrices. (PubMed, Anal Methods) - "To address this drawback, we developed a highly selective and specific liquid chromatography triple-stage tandem mass spectrometry (LC-MS/MS/MS, LC-MS3) method via systematic comparison of MRM and MRM3 modes for the determination of nine β-agonists (ractopamine, penbutolol, cimaterol, salbutamol, clenbuterol, tulobuterol, clorprenaline, terbutaline, and fenoterol) in high-fat milk and pork. In comparison, the conventional LC-MS/MS method showed higher LODs (0.1-0.15 µg kg-1) and LOQs (0.3-0.45 µg kg-1) and broader matrix effects (-18.12-19.35%), confirming the superior sensitivity of the LC-MS3 method. This is the first study to employ MRM3 mode for the determination of β-agonists in high-fat milk and pork matrices."

Journal

Predicting the potential for organic cation transporter 1-mediated drug-drug interactions with fenoterol by amitriptyline, fluoxetine, selegiline, metformin, and verapamil. (PubMed, Expert Opin Drug Metab Toxicol) - "An in vitro OCT1 inhibition assay using fenoterol as probe substrate was validated and identified that verapamil may pose a clinically relevant interaction risk, predicting a minimum 2-fold increase in fenoterol exposure. This highlights the need for caution when coadministrating verapamil with fenoterol and supports incorporating OCT1 inhibition profiling into preclinical evaluation of new drug entities to better inform clinical development and ensure patient safety."

Journal • Asthma • Immunology • Pulmonary Disease • Respiratory Diseases • SLC22A1

SERS fingerprinting of β2-agonists for anti-doping based on Au-COF substrate. (PubMed, Anal Chim Acta) - "This study develops a novel analytical method utilizing Au-COF composites for highly sensitive SERS detection. It pioneers the application of this strategy in the qualitative and quantitative analysis of trace β2-agonists. The research not only significantly expands the scope of Au-COF composites but also provides a technologically promising approach with substantial practical value for ensuring medical safety through clinical medication monitoring and for detecting banned substances in sports."

Journal • Asthma • Fatigue • Immunology • Pulmonary Disease • Respiratory Diseases

A new HPTLC-image analysis approach for assessing interactions and antioxidant profiles of adrenergic drugs. (PubMed, J Chromatogr A) - "Results revealed that highly polar compounds, that is norepinephrine, etilefrine, metaraminol and midodrine exhibited strong interactions with silica gel but limited retention on reversed-phase, while lipophilic derivatives, namely naphazoline, xylometazoline, clenbuterol and bambuterol demonstrated strong affinity for non-polar and moderately polar phases, predicting good membrane penetration and blood-brain barrier permeability. Interestingly, some β-agonists (bambuterol, fenoterol, buphenine and irsoxsuprine) with polar groups showed unexpectedly weak silica gel retention, highlighting their dominant lipophilic contributions...Thus, the polar phases (silica gel, DIOL) enhanced radical scavenging activity, whereas non-polar phases often reduced it. The developed HPTLC-IA method, integrating selective stationary phases and two-radical assays, offers a novel and cost-effective approach for screening the possible variation of antioxidant activity of drugs after their..."

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Risk assessment and bioaccumulation of β-agonists in the Yellow River Delta of China: Implications for environmental safety. (PubMed, Ecotoxicol Environ Saf) - "Fenoterol was the dominant residue in all samples, 7596.67 ng/kg in sediments, 3657.00 ng/kg in aquatic animals and 65.39 ng/L in water. -terol-type β-agonists exhibited potential bioaccumulation in crab, and notably, tulobuterol exhibited markedly high bioaccumulation in fish...These results indicate the division of functional zones is effective in mitigate the β-agonists pollution. Based on the contamination status of β-agonists in various zones, this study recommends that: Maintain a minimum 2 km buffer between "core zones" and "experimental zones", maintain a minimum 40 km separation between core zones and human activity areas."

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Veterinary Drug Residues in Animal-Origin Food: a UPLC-MS/MS Screening Method for the Determination of 21 Beta-Agonists in Animal Lung and Liver According to Commission Implementing Regulation (EU) 2021/808. (PubMed, J Mass Spectrom) - "With regard to detection capability CCβ, the results obtained permitted the qualitative determination of 11 clenbuterol-like beta-agonists (Clenbuterol, Bromchlorbuterol, Brombuterol, Cimaterol, Cimbuterol, Clenpenterol, Clenproperol, Hydroxymethylclenbuterol, Mabuterol, Mapenterol, Tulobuterol) at 0.05 μg/kg and for 10 salbutamol-like beta-agonists (Carbuterol, Isoxsuprine, Clencyclohexerol, Ractopamine, Ritodrine, Salbutamol, Terbutaline, Zilpaterol, Fenoterol, Salmeterol) at 0.25 μg/kg. The method was validated for lungs and livers of different animal species (cattle, chicken, sheep, and swine): following the requirements of the above-mentioned Regulation. The method was found to be robust and specific."

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Investigating organic cation transporter 1 in drug interactions: New findings from in vitro and in vivo cynomolgus monkey studies. (PubMed, Drug Metab Dispos) - "Transport assays in transfected human embryonic kidney 293 cells showed that sumatriptan, fenoterol, metformin, quinidine, and 1-methyl-4-phenylpyridinium were transported by cOCT1 at rates comparable to hOCT1 (less than 2-fold difference)...Consistent with our in vitro findings, coadministration of OCT1 inhibitors (axitinib, nintedanib, and erlotinib) significantly increased the systemic exposure of sumatriptan in monkeys. These findings offer valuable insights into the role of OCT1 in drug-drug interactions and highlight the potential of cynomolgus monkeys as a useful and potentially translational model for OCT1-mediated disposition and interactions."

Journal • Preclinical • SLC22A1

Investigation of In-Trap High-Energy Collision Dissociation Methodology and Dissociation Conditions Using Dual-Pressure Linear Ion Trap Mass Spectrometry. (PubMed, Rapid Commun Mass Spectrom) - "Validation experiments using veterinary drug residues fenoterol and ractopamine demonstrated the method's universality by comparing its dissociation results with those from conventional ion trap collision-induced dissociation (CID) and triple quadrupole method. The findings confirm that this strategy can be extended to other ion trap mass spectrometry platforms, offering broader applicability."

Journal

The divergent roles of tryptophans W354 and W217 in OCT1 transport: similar localization, distinct functions. (PubMed, J Biol Chem) - "Hepatic organic cation transporter 1 (OCT1, SLC22A1) has a broad spectrum of structurally diverse substrates, including drugs like morphine, metformin, sumatriptan, and fenoterol. Our data suggest that W354 is crucial for OCT1 function by mediating the switch from an inward- occluded to inward-open conformation but is not directly involved in substrate interaction. In contrast, W217, along with the previously known F244, contributes to the substrate specificity of OCT1."

Journal • SLC22A1

Age-related changes in adrenergic regulation of contractility and redox status of glycolytic and oxidative skeletal muscles. (PubMed, Geroscience) - "Fenoterol, a β-AR agonist, exerted a negative inotropic action in EDL and soleus muscles of young adult and middle-aged mice...Accordingly, the age-related shift of balance from positive to negative inotropic action of adrenaline might be partially dependent on the interplay of β2- and β3-adrenergic signaling in the skeletal muscles. Despite the commonalities in the changes in adrenergic regulation of contractions in both muscles, oxidative stress, decline in antioxidant enzyme activities, and ultrastructural disturbances were much more clearly expressed in aged EDL versus soleus muscles."

Journal • Sarcopenia • AR

POSTOPERATIVE EUGLYCEMIC KETOACIDOSIS IN THIRD TRIMESTER REQUIRING EMERGENCY CAESAREAN SECTION (FIGO 2025) - "On day 3 mild uterine contractions were treated with β-sympathomimetic fenoterol hydrobromide... This case highlights the rare occurrence of euglycemic ketoacidosis in pregnancy, emphasizing the need for monitoring and rapid correction of acidosis to mitigate maternal and fetal complications. Written informed consent was obtained from the patient."

Acute Respiratory Distress Syndrome • Cardiovascular • Diabetes • Gastroenterology • Gastrointestinal Disorder • Gestational Diabetes • Metabolic Disorders • Respiratory Diseases

A Comparison of the Molecular Pharmacological Properties of Current Short, Long, and Ultra-Long-Acting β2-Agonists Used for Asthma and COPD. (PubMed, Pharmacol Res Perspect) - "Few studies directly compare the molecular pharmacological properties of short (salbutamol, terbutaline, fenoterol), long (formoterol, salmeterol), and ultra-long-acting (indacaterol, olodaterol, vilanterol) β2-agonists. Comparison with other β-ligands suggests that affinity and duration could both be improved further. However, given the very wide range of molecular pharmacological properties of β-agonists that are clinically effective and widely used, non-pharmacological properties (physiochemical, patient factors, devices and combination inhaler availability) may be as important in final clinical patient outcomes as the molecular pharmacological properties of the individual β2-agonists themselves."

Clinical • Journal • Asthma • Chronic Obstructive Pulmonary Disease • Immunology • Pulmonary Disease • Respiratory Diseases

Effect of Dual Bronchodilation on the Exercise Capacity of Individuals With Non-Cystic Fibrosis Bronchiectasis: Protocol for a Randomized Controlled Double-Blind Crossover Study. (PubMed, JMIR Res Protoc) - P=N/A | "There is no evidence that BDs can improve the exercise capacity of patients with NCFB. This trial will compare the endurance exercise capacity of the same individual with and without dual bronchodilation. If successful, this study will demonstrate that exercise capacity can be improved with the use of BDs in adults with NCFB."

Journal • Bronchiectasis • Genetic Disorders • Immunology • Infectious Disease • Non‐Cystic Fibrosis Bronchiectasis • Novel Coronavirus Disease • Pulmonary Disease • Respiratory Diseases

Augmenting Beneficial β2-adrenergic Receptor Signaling and Function Using a Biased Allosteric Modulator (ATS 2025) - " Human ASM (HASM) cells were stimulated with different β-agonists including isoproterenol (ISO), formoterol (FORM), epinephrine (EPI), norepinephrine (NE), albuterol (ALB), salmeterol (SALM), terbutaline (TERB), and fenoterol (FENO) in the presence/absence of PAM 37. Our results demonstrate that the PAM 37 augments beneficial β2AR-Gαs-signaling, airway relaxation, and bronchodilation without affecting detrimental β-arrestin-mediated signaling by multiple clinically relevant β-agonists."

Respiratory Diseases • ARRB1

Adrenergic Modulation of Acetylcholine Release at the Mouse Neuromuscular Junctions of Fast-Twitch Skeletal Muscle. (PubMed, Neurochem Res) - "Effects of β2-AR activation were dependent on the type of agonist: Procaterol decreased both ACh release and Ca2+ entry into the nerve terminals, whereas fenoterol promoted ACh release in a Gi protein-dependent manner. Thus, synaptic transmission in the "fast" NMJs had specific features of adrenergic regulation engaging Gi protein, adenylyl cyclase, phospholipase A2, protein kinases A and C. The positive effect of natural agonist adrenaline was reproduced only by β2-AR activation with fenoterol, but not α1-, α2-, β1-agonists and β2-agonist procaterol."

Journal • Preclinical • Review

Substrate-specific inhibition of organic cation transporter 1 revealed using a multisubstrate drug cocktail. (PubMed, Drug Metab Dispos) - "Here, we describe a multisubstrate drug cocktail that allows for the simultaneous testing of drug-drug interactions using 8 different victim drugs: fenoterol, salbutamol, sumatriptan, zolmitriptan, ipratropium, trospium, methylnaltrexone, and metformin...Group 1 comprised verapamil, quinidine, fenoterol, and ipratropium, and group 2 comprised metformin, sumatriptan, and trimethoprim...Here, we demonstrate this for organic cation transporter 1 (OCT1, SLC22A1) and presents a drug cocktail designed to identify varying inhibitory potencies in vitro and prevent false-negative drug-drug interaction results during early drug development. This approach can be extended to other polyspecific drug transporters."

Journal • SLC22A1

Distinct Response of the Human Plasma Lipidome to Cold and Fenoterol (ESPE-ESE 2025) - "Both cold exposure and stimulation of the β2-AR increase lipolysis and REE in humans. Our findings indicate that enhanced lipolysis is a key mechanism driving β2-AR-stimulated thermogenesis. However, the distinct lipidomic profile points towards different molecular mechanisms in response to cold."

Genetic Disorders • Obesity

The beta-2-adrenoreceptor agonist fenoterol increases resting enery expenditure without activation of brown adipose tissue in humans. (ESPE-ESE 2025) - "We found no evidence that β2-ARs play a major role in activation of human BAT. A reason for the observed fenoterol-induced increase in REE could be futile metabolic cycles e.g. lipid cycling in skeletal muscle or white adipose tissue."

Genetic Disorders • Obesity • ADRB2

Substrate-specific effects point to the important role of Y361 as part of the YER motif in closing the binding pocket of OCT1. (PubMed, J Biol Chem) - "OCT1 has a broad spectrum of structurally diverse substrates like metformin, sumatriptan, trospium, and fenoterol. Only tryptophan at codon 361 efficiently rescued the transport of the Y361A mutant supporting hydrogen bound interaction with E386 and R439. Our study confirms that the YER motif is essential for OCT1 transport and points to Y361 as a lever that interacts with E386 and R439 to trigger the closing of the binding pocket of human OCT1."

Journal • SLC22A1

Ecofriendly colorimetric set-up coupled with mathematical filtration strategy for simultaneous determination of ipratropium and fenoterol in their novel anti-asthmatic metered dose inhaler. (PubMed, BMC Chem) - "Using cutting-edge software metric tools, namely the analytical greenness (AGREE), and complementary green analytical procedure index (ComplexGAPI), the greenness profile of the suggested method was clearly evaluated. The method also conformed well to the recently published blueness (BAGI tool) and whiteness (RGB12 tool) concepts."

Journal • Asthma • Chronic Obstructive Pulmonary Disease • Immunology • Pulmonary Disease • Respiratory Diseases

Neuroprotective effects of phenylacetylglycine via β2AR on cerebral ischemia/reperfusion injury in rats. (PubMed, Saudi Pharm J) - "Furthermore, the protective effect of PAGly diminished after the administration of β2AR-specific agonist fenoterol (P = 0.0055). These data indicate that PAGly mitigates cerebral I/R injury by inhibiting microglial inflammation via β2AR, highlighting its potential as a therapeutic agent. These findings position PAGly as a promising candidate for therapeutic intervention in cerebrovascular injuries, warranting further exploration in clinical settings."

Journal • Preclinical • Atherosclerosis • Cardiovascular • Inflammation • Reperfusion Injury • IL1B • IL6 • TNFA