moclobemide / Generic mfg. - LARVOL DELTA

Design and Computational Evaluation of Isatin Derivatives as Dual MAO-A/IDO1 Inhibitors: Molecular Docking and Molecular Dynamics Insights. (PubMed, Curr Med Chem) - "SDI-107 and SDI-113 emerged as promising dual MAO-A/IDO1 inhibitors, demonstrating favorable binding affinity, stable protein-ligand interactions, and encouraging binding free energy profiles. These findings support further experimental validation and structural optimization toward the development of multitarget-directed antidepressant agents."

Journal • CNS Disorders • Depression • Major Depressive Disorder • Mood Disorders • Psychiatry

Amidation of Quinolin-2-yl Esters: Base‑, Catalyst‑, Metal‑, and Solvent-Free Conditions. (PubMed, ACS Omega) - "The practical utility of the method was demonstrated with the synthesis of the drug molecule moclobemide and two natural products, piperlotine A and piperlotine C. A comparative amidation study was conducted to find a possible factor for the high reactivity of quinolin-2-yl esters. The findings presented above reveal that the quinolin-2-yl ester scaffold can be exploited for the synthesis of amides and peptides under environmentally benign conditions."

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Comparative Pharmacological Profiling of Psychotherapeutic Drugs Reveals a Functional Taxonomy Based on Direct Inhibition of Smooth Muscle Excitability. (PubMed, Pharmaceuticals (Basel)) - "Integrative analysis stratified compounds into four distinct functional profiles: (i) High Inhibitory Liability (e.g., nortriptyline, paroxetine), characterized by low micromolar IC50 values and dose-dependent inhibition across multiple tissues; (ii) Non-Selective Inhibition (e.g., flunarizine, cinnarizine), showing consistent but dose-independent inhibition; (iii) Tissue-Dependent Inhibition (e.g., risperidone, reboxetine); and (iv) Minimal Inhibition (e.g., moclobemide). This study reveals a previously underrecognized pharmacodynamic dimension of psychotherapeutic drugs and establishes a comparative functional taxonomy based on their direct, non-receptor-mediated inhibition of smooth muscle excitability. The identified profiles provide a mechanism-informed framework for contextualizing autonomic side-effect liability and may support improved safety evaluation in psychotherapeutic drug development."

Journal • CNS Disorders

Recommendations from the Clinical Toxicology Recommendations Collaborative on the administration of activated charcoal in acute oral overdose. (PubMed, Clin Toxicol (Phila)) - "The Workgroup concluded that there is no role for activated charcoal in poisoning from arsenic, caesium, copper, ethanol, methanol, ethylene glycol, iron, lead, lithium, and metformin. Activated charcoal is appropriate after ingestion of antidysrhythmics (types I and III not discussed specifically), beta-adrenergic antagonists, bupropion, calcium-channel blockers, carbamazepine, cardiac glycosides, chloroquine, cocaine, colchicine, cyanide, dapsone, diphenhydramine, disopyramide, factor Xa inhibitors, ibuprofen, isoniazid, lamotrigine, methotrexate, moclobemide, opioids, organophosphorus insecticides, paracetamol (acetaminophen), paraquat, phenobarbital, phenytoin, quinidine and quinine, salicylates, selective serotonin reuptake inhibitors, sulfonylureas, thallium, theophylline, tricyclic antidepressants, valproic acid, venlafaxine, and warfarin. An additional dose of activated charcoal to complete gastrointestinal decontamination is appropriate after ingestion of..."

Journal • Cardiovascular • CNS Disorders • Epilepsy • Gastrointestinal Disorder • Hypotension • Respiratory Diseases

Prioritizing Contaminants of Emerging Concern in the Yangtze River Basin: An Integrated Assessment Combining Exposure-Activity Ratios and Adverse Outcome Pathways. (PubMed, Environ Toxicol Chem) - "Results showed that among all target CECs (nd-12,300 ng/L), 11 chemicals exhibited a 100% detection rate, with moclobemide (12,510 ng/L) and venlafaxine (12,300 ng/L) having the highest concentrations. Based on EAR and detection status, triisobutyl phosphate, aldicarb, methomyl, acetamiprid, perfluorodecanoic acid, nalidixic acid, and moclobemide were identified as "Level 1" priority chemicals. By linking high-exposure-activity ratio (high-EAR) molecular targets to validated AOPs, we connected analytical chemistry data with predictions of specific adverse outcomes, including endocrine-disruption-associated reproductive failure, porphyria-like metabolic disorders, and impairments in cognitive function and growth, which not only provide a mechanistic basis for analyzing the diverse biological effects induced by high-risk chemicals but also facilitate the screening-level prediction of potential associated ecological and human health risks."

Adverse events • Journal • Cognitive Disorders • Genetic Disorders • Hematological Disorders • Metabolic Disorders

Bayesian Optimization of Solvent-Free Thermal Amidation via Reactive Extrusion. (PubMed, Chemistry) - "Optimized conditions facilitated the product isolation, some of them were obtained essentially pure from the extruder, others purified by extraction or crystallization. Notably, moclobemide could be synthesized at larger scale and isolated in the complete absence of organic solvent."

Journal

Comparing affective bias modification by first- and second-generation antidepressants in male rats using a translational behavioural task. (PubMed, Neuropsychopharmacology) - "Dose-response experiments using the tricyclic antidepressant, amitriptyline (0.3-3.0 mg/kg), monoamine oxidase inhibitor, moclobemide (3.0-10.0 mg/kg) and serotonin specific re-uptake inhibitor, sertraline (1.0-10.0 mg/kg) were performed. Previous work has shown that variations in affective bias modification are linked to both the time course of clinical effects and their interaction with experience-dependent plasticity. Integrating understanding of these neuropsychological differences within clinical practice has the potential to improve clinical outcomes for patients."

Journal • Preclinical • CNS Disorders • Depression • Major Depressive Disorder • Mood Disorders • Psychiatry

Mechanistic Dichotomy in Sulfate Radical Anion-Mediated Oxidative Synthesis of Activated N-Hydroxysuccinimide Esters. (PubMed, J Org Chem) - "The synthetic utility was demonstrated by the preparation of marketed drugs, including moclobemide, procainamide, acecainide, and bezafibrate, with moclobemide further synthesized on a 100 g scale, highlighting the practicality and industrial relevance of the process. The results suggest that the generation and subsequent radical-radical coupling of acyl and succinimide-N-oxyl radicals constitute the most favorable pathway, while alternative radical and cationic routes may also contribute under reaction conditions. This study not only advances an efficient and scalable amide synthesis but also broadens the mechanistic understanding of sulfate radical anion reactivity in aromatic systems."

Journal

Antidepressants and the risk of hyponatremia: A multi-institutional cohort study using observational medical outcomes partnership-Common Data Model. (PubMed, Br J Clin Pharmacol) - "Close monitoring of serum sodium levels is essential for SSRI users, especially those aged ≥60 years."

Journal • Licensing / partnership • Cardiovascular • CNS Disorders • Depression • Heart Failure • Psychiatry

Comparative effects of antidepressants on cocaine-induced hyperthermia in rats: a preclinical study. (PubMed, Neurosci Lett) - "Mirtazapine may be a safer antidepressant option for managing depression in cocaine users because of its capacity to suppress hyperthermia without enhancing monoamine reuptake inhibition. Notably, caution should be exercised when prescribing monoamine oxidase inhibitors and SNRIs to this population. However, further clinical studies are required to validate these findings."

Journal • Preclinical • CNS Disorders • Depression • Psychiatry

Redressing long-term antidepressant use in general practice (RELEASE) (ECNP 2025) - "Antidepressants include selective serotonin reuptake inhibitors (sertraline, escitalopram fluoxetine, paroxetine, fluvoxamine and citalopram); serotonin and norepinephrine reuptake inhibitors (venlafaxine, desvenlafaxine, duloxetine); and other antidepressants (mirtazapine, vortioxetine, mianserin, moclobemide, reboxetine, agomelatine). 26 practices and 485 participants randomised. Data collection complete November 2025. Implications: This study will develop new knowledge applicable internationally on the effectiveness, cost-effectiveness, and implementation of the RELEASE multi-strategy intervention in prompting review of antidepressant medication and supporting informed decision-making and safe cessation via hyperbolic tapering to minimise withdrawal symptoms to improve primary mental health care and outcomes for patients."

Alzheimer's Disease • CNS Disorders • Dementia • Mood Disorders • Neuralgia • Psychiatry

Behavioral effects of psychedelic and non-psychedelic serotonin 2A receptor agonist drugs in pigs (ECNP 2025) - "Here, we have determined the relationship between plasma concentration and cerebral 5-HT2AR occupancy of N,N-dimethyltryptamine (DMT), psilocybin, lysergic acid diethylamide (LSD) and lisuride in pigs, and measured psychedelic-induced behavior (headshakes) at doses generating 60-70% occupancy...The behavioral study was done in 8 awake female pigs each receiving IV DMT, 0.4 mg/kg (injected 30 min after monoamine oxidase inhibitor, moclobemide, 0.85 mg/kg), psilocybin, 30 µg/kg, LSD, 0.6 µg/kg, and lisuride, 5.8 µg/kg, in a randomized order, with 3-4 days separating each drug... We have for the first time established relationships between cerebral 5-HT2AR occupancy, drug plasma concentrations and drug dose for 5-HT2AR agonists in vivo in pigs, and subsequently compared psychedelic-induced behavior in awake pigs on the basis of the cerebral 5-HT2AR occupancy."

CNS Disorders

Utilization of psychotropic drugs in Serbia from 2006 to 2021: Patterns before and during the COVID-19 pandemic. (PubMed, PLoS One) - "The COVID-19 pandemic did not contribute to change in consumption of psychotropic drugs in Serbia. Still, the use of antidepressants, atypical antipsychotics, anxiolytics, sedatives, hypnotics, anti-dementia drugs and gabapentinoids increased from 2006 to 2021."

Journal • Alzheimer's Disease • CNS Disorders • Dementia • Infectious Disease • Mental Retardation • Novel Coronavirus Disease • Psychiatry

MAO-A inhibition alleviates sepsis-driven lung injury via Nrf2/HO-1 pathway activation and suppression of pyroptosis. (PubMed, J Mol Histol) - "Additionally, human alveolar epithelial cells (HPAEpiC) treated with MAO-A inhibitor RO11-11639 were subjected to lipopolysaccharide (LPS) stimulation in vitro...Mechanistically, MAO-A inhibition promoted the nuclear translocation of Nrf2, thereby activating the downstream regulatory proteins HO-1, quinone oxidoreductase 1 (NQO-1) and glutathione s-transferase (CST). These data cumulatively indicate that pharmacological targeting of MAO-A may offer therapeutic benefits in septic ALI by attenuating pathophysiological processes involving oxidative damage and inflammasome-mediated pyroptosis."

Journal • Acute Lung Injury • Infectious Disease • Inflammation • Respiratory Diseases • Septic Shock • HMOX1 • IL16 • NQO1

An Overview of the Systematic Reviews About the Efficacy of Fluvoxamine on Depression. (PubMed, Pharmaceuticals (Basel)) - "Comparisons with imipramine, clomipramine, amitriptyline, dothiepin, paroxetine, fluoxetine, citalopram, mianserin, nortriptyline, and moclobemide generally revealed no significant differences in efficacy. However, some reviews indicated that venlafaxine and mirtazapine were superior to fluvoxamine in certain outcomes, while fluvoxamine demonstrated greater efficacy than desipramine in one review. Sertraline and milnacipran showed mixed or review-quality-dependent results, with one low-quality review favoring milnacipran...While no single antidepressant was universally superior, fluvoxamine's unique pharmacological profile and favourable safety characteristics support its clinical utility. Further research is needed to explore its role in personalized treatment strategies and emerging therapeutic contexts, such as comorbid anxiety and post-traumatic stress disorder."

Journal • Review • CNS Disorders • Depression • Mental Retardation • Mood Disorders • Post-traumatic Stress Disorder • Psychiatry

Pharmacological treatments for atypical depression: A systematic review and network meta-analysis of randomized controlled trials. (PubMed, Eur Neuropsychopharmacol) - "Phenelzine might perform better than other compounds, but several drugs outperformed placebo in response. Nortriptyline performed worse than other treatments. High-quality studies are needed."

Journal • Retrospective data • CNS Disorders • Depression • Major Depressive Disorder • Mood Disorders • Psychiatry • Sleep Disorder

Did Serendipity Contribute to the Discovery of New Antidepressant Drugs? Historical Analysis Using Operational Criteria. (PubMed, Alpha Psychiatry) - "Selective serotonin reuptake inhibitors (fluoxetine, fluvoxamine, citalopram, paroxetine, sertraline, and escitalopram), selective dopamine and noradrenaline reuptake inhibitors (bupropion), noradrenaline and serotonin reuptake inhibitors (venlafaxine, milnacipram, duloxetine, and desvenlafaxine), selective noradrenaline reuptake inhibitors (reboxetine), noradrenergic and specific serotonergic antidepressants (mirtazapine), melatonergic agonists (agomelatine), and serotonin modulators and stimulators (vortioxetine, vilazodone, tianeptine) correspond to the type IV pattern. Ketamine, a glutamatergic modulator, corresponds to the type III pattern, characterized by a non-serendipitous origin (initial development as an anesthetic agent) leading to a serendipitous observation (the discovery of antidepressant efficacy in individuals illicitly using). The majority of new antidepressants adhere to a type IV pattern, characterized by a rational and targeted design process where..."

Journal • Anesthesia

A fatal intoxication case due to the serotonin syndrome induced by dextromethorphan and moclobemide overdose. (PubMed, Leg Med (Tokyo)) - "In this case, the diagnosis of serotonin syndrome was made on the basis of autopsy findings and additional drug testing. In cases of suspected death due to serotonin syndrome, additional drug testing and quantitative evaluation to identify the causative agent would be helpful in the diagnosis."

Journal • Mood Disorders

Preparation, In Vivo and Molecular Docking Study of Nano-Emulsion Obtained from the Isolated Phytoconstituents of Symplocos racemosa for Mitigating Depression. (PubMed, Chem Biodivers) - "A chitosan-loaded herbal nano-emulsion containing these phytoconstituents was formulated for enhanced brain delivery tested using animal studies using forced swim test and actophotometer models.  Docking studies confirmed that all the components exhibit a good binding towards MAO-A, comparable to standard moclobemide and among all salireposide has the most significant and better binding affinity higher than moclobemide. Nano-emulsion, at both the dosages, reduced the immobility time in FST and increased the locomotor activity in actophotometer of depressed mice.  Nano-emulsion of isolated phytoconstituents from S. racemosa exhibited synergistic effects, effectively managing depression by inhibiting MAO-A."

Journal • Preclinical • CNS Disorders • Depression • Mood Disorders • Psychiatry

Heterocyclic Antidepressants with Antimicrobial and Fungicide Activity. (PubMed, Molecules) - "In addition, there is a serious problem of increasing resistance of microorganisms to antibiotics. In this article, we found that almost all of the antidepressants considered (except moclobemide, haloperidol, and doxepin) have antimicrobial activity and can suppress the growth of not only pathogenic microorganisms but also the growth of bacteria that directly affect mental health (such as Lactobacillus, Lactococcus, Streptococcus, Enterococcus, and Bifidobacterium)."

Journal • Review

Aryl Borane as a Catalyst for Dehydrative Amide Synthesis. (PubMed, J Org Chem) - "This protocol is applicable across a wide range of >35 substrates, including aromatic and aliphatic amines and acids, resulting in amides in ≤92% yields. The scalability of the reaction up to 10 mmol, along with the synthesis of drugs such as ibuprofen amide, moclobemide, and phenacetin, demonstrates the industrial potential of our protocol."

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Innovative role of the antidepressant imipramine in esophageal squamous cell carcinoma treatment: Promoting apoptosis and protective autophagy. (PubMed, Int Immunopharmacol) - "Our findings provide the first reported evidence that IM triggers apoptosis and protective autophagy in ESCC cells via the Hippo signaling pathway, thus suggesting that IM may offer a promising therapeutic approach for patients with ESCC and depression."

Journal • CNS Disorders • Depression • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Oncology • Psychiatry • Solid Tumor • Squamous Cell Carcinoma • ANXA5 • CASP3

Photocatalytic oxidative hydroacylation with alcohols. (PubMed, Org Biomol Chem) - "Under photoirradiation and a catalytic amount of TBADT, different electrophiles (azodicarboxylates, N-phenylmaleimide, benzylidenemalononitrile and phenyl vinyl sulfone) underwent hydroacylation with alcohols in good yields. The method was also applied to achieve a convenient synthesis of the anti-depressant drug moclobemide."

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Exploring mechanisms of dependence and pharmacological interventions for Arecanut/BetelQuid cessation: a review (ECNP 2024) - "In another RCT, the effects of antidepressants, escitalopram and moclobemide were studied for cessation therapy in betel quid disorder...This study postulated that the common link between AN/ Betel Quid and tobacco suggests that partial agonist therapies with cytisine or varenicline may potentially also help in AN/ Betel Quid cessation5.Another study postulated the potential role of nicotine gum with pilocarpine for treatment. Rationale for nicotine gum was that arecoline acts on the same receptor proteins in the brain as nicotine and hence would help in reducing cravings while the pilocarpine potentially would recreate the Betel Quid's salivation experience6. Conclusion There is an urgent need to explore the neurological and neurochemical mechanisms of AN/ Betel Quid addiction and further evaluating pharmacological interventions for its cessation."

Review • CNS Disorders • Depression • Mood Disorders • Psychiatry • Tobacco Cessation

Exploring the correlation between cardiovascular adverse events and antidepressant use: A retrospective pharmacovigilance analysis based on the FDA Adverse Event Reporting System database. (PubMed, J Affect Disord) - "The retrospective analysis revealed that cardiovascular AEs were connected with antidepressant use, and the binding/uptake inhibitory potency and selectivity of neurotransmitters of antidepressants played an important role, providing a preliminary basis for further in-depth study of antidepressant-related cardiovascular toxicity. However, as an exploratory study, prospective studies are needed to validate our findings in the future."

Adverse events • Journal • Retrospective data • Atrial Fibrillation • Cardiomyopathy • Cardiovascular • CNS Disorders • Coronary Artery Disease • Depression • Heart Failure • Hypertension • Psychiatry • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases