galantamine hydrobromide / Generic mfg. - LARVOL DELTA

Chronic Administration of Carvone-Rich Mentha spicata L. Essential Oil Attenuates Cognitive Dysfunction and Oxidative Stress in Zebrafish. (PubMed, Plants (Basel)) - "Scopolamine hydrobromide trihydrate (SCO, 100 µM) was administered for 30 min before each behavioral assessment and again before euthanasia, whereas galantamine (GAL, 1 mg/L) was administered 30 min before each SCO challenge. In silico descriptors were treated as hypothesis-generating and do not demonstrate zebrafish brain exposure. These findings support further investigation of carvone-rich MEO within a rescue/protection framework, with confirmation in independently replicated exposure tanks and inclusion of MEO-only controls."

Journal • Cognitive Disorders • Mood Disorders • Pain • Psychiatry

Galantamine Reverses Habitual Responding Induced by Adolescent Binge Alcohol Exposure in Female Rats (Neuroscience 2026) - "Preliminary data shows that Galantamine recovered AIE induced suppression of ChAT cells in the NbM. These results suggest that Galantamine rescue AIE-induced impairments in behavioral flexibility by enhancing cholinergic signaling in female rats."

Preclinical • Alzheimer's Disease • CNS Disorders • Dementia • CHAT

Chemical profiling and in silico target prediction of Lippia alba leaf essential oil supported by in vitro bioactivity assessment. (PubMed, Comput Biol Chem) - "In silico docking revealed that among the tested constituents, only cubebol (-7.8 kcal/mol) exhibited a higher calculated binding affinity for hAChE than the standard galantamine (-7.6 kcal/mol), whereas β-myrcene (-6.7 kcal/mol) showed weaker binding affinity, indicating cubebol's targeted potential against neurodegenerative disorders linked to AChE imbalance. For COX-2, caryophyllene (-6.3 kcal/mol)) and cubebol (-6.2 kcal/mol) demonstrated comparable, though slightly lower, binding affinities relative to the standard sodium diclofenac ((-6.4 kcal/mol), highlighting their potential as preliminary computational lead hits for multi-target virtual screening. The present study suggests that LALEO has potential for further research and the development of natural medicines, after having scientific validation."

Journal • Preclinical • CNS Disorders • Pain • Tyrosinase

Autonomic-Immune Crosstalk in Lupus: Impaired Cholinergic Signaling and Consequences for Cardiovascular-Renal Physiology. (PubMed, Am J Physiol Cell Physiol) - "We found that pharmacological enhancement of vagal activity and engagement of the parasympathetically-mediated cholinergic anti-inflammatory pathway via systemic administration of galantamine attenuated pathogenic autoantibodies, blood pressure and inflammatory mediators in murine lupus...Disruption of this balance may contribute to chronic inflammatory diseases such as SLE and others. This review highlights emerging opportunities for cholinergic anti-inflammatory pathway-based pharmacological and neuromodulatory strategies to mitigate inflammation-driven autoimmune, cardiovascular, and renal disease."

Journal • Review • Cardiovascular • Fibrosis • Hypertension • Immunology • Inflammation • Inflammatory Arthritis • Lupus • Nephrology • Renal Disease • Systemic Lupus Erythematosus

Comparison of the Utility of Amplitude-Spectral and Coherence Features of Psychotropic Drugs' Action on ECoG Signal for Pharmaco-EEG Based Drug Screening in Rats. (PubMed, Methods Protoc) - "The training set, relative to which the effects of the pharmacological agents from the test set were classified, were the matrices of effects of 12 pharmacological agents: the NMDA antagonist dizocilpine, the D2/D3 antagonists haloperidol and sulpiride, the M-anticholinergic tropicamide, the H1/5HT2A receptor blocker hydroxyzine, the acetylcholinesterase inhibitor galantamine, the alpha-2 adrenergic agonist dexmedetomidine, the alpha-2 adrenergic antagonist atipamezole, the adenosine receptor blocker caffeine and the GABA-mimetics aminophenylbutyric acid (phenibut), bromdihydrochlorophenylbenzodiazepine (phenazepam) and 5-ethyl-5-phenyl-2,4,6(1H,3H,5H)-pyrimidinetrione. The test set included various drugs with tropism for the targets of the training set drugs: dopamine receptor antagonists chlorpromazine, droperidol, tiapride and raclopride, H1-histamine blockers diphenhydramine and promethazine, 5-HT2-receptor blockers ritanserin and glemenserin, acetylcholinesterase..."

Journal • Preclinical • Pain

Modulatory effects of α7-nicotinic cholinergic receptors on perceptual sensitivity in a visual signal detection task. (PubMed, Psychopharmacology (Berl)) - "These findings demonstrate that α7 nAChR modulation bidirectionally and dose-dependently regulates perceptual sensitivity, irrespective of attentional distraction. These findings have implications for targeted cognitive enhancement in disorders of attention."

Journal • COMT

Isatin derivatives as potent cholinesterase inhibitors: recent developments and future challenges. (PubMed, RSC Adv) - "However, the currently approved small molecules, including tacrine, donepezil, rivastigmine, and galantamine, are limited by their modest efficacy, poor selectivity, and adverse effects, necessitating the development of improved therapeutic agents. Structure-activity relationship studies have revealed the critical influence of electronic effects, linker optimization, N-substitution, and molecular hybridization on inhibitory potency and selectivity. This review summarizes the most promising isatin-based cholinesterase inhibitors reported from 2020 to the present, highlighting their biological activities, structure-activity relationships, and potential for the development of next-generation anti-Alzheimer therapeutics."

Journal • Review • Alzheimer's Disease • CNS Disorders • Pain

Single-cell transcriptomics reveals distinct microglial state remodeling associated with the (R)-nicotine/diosmetin combination and galantamine in LPS-challenged BV2 cells. (PubMed, Front Immunol) - "These findings indicate that the DR condition was associated with remodeling of LPS-challenged BV2 microglial-like states, attenuation of inflammatory programs, and increased neurotrophic outputs relative to LPS, without significantly reducing CCK-8-assessed metabolic activity. This study provides a single-cell characterization of distinct treatment-associated responses to (R)-nicotine, diosmetin, their combined administration, and galantamine."

Journal • CNS Disorders • Inflammation • ATF3 • BDNF • ITGAE • NMUR1 • PLK4

Performance changes and neuromuscular alterations in sprague dawley rats following repeated occupational exposures to the pesticide malathion. (PubMed, PLoS One) - "Galantamine treatment protected against health effects associated with repeated occupational-like malathion exposure, indicating involvement of cholinergic mechanisms despite minimal changes in plasma cholinesterase activity. Overall, repeated low-concentration malathion exposure is associated with locomotor deficits and peripheral neuropathy."

Journal • Preclinical • CNS Disorders • Pain

Beyond the fruit: phenolic composition, cytotoxicity, antioxidant, and multi-enzyme inhibitory activity of twig and leaf extracts from four understudied Turkish Rosa species. (PubMed, RSC Adv) - "In enzyme inhibition assays, EA extracts demonstrated consistent multi-target activity: AChE inhibition (up to 2.49 mg galantamine equivalent (GALAE) per g), BChE inhibition (up to 4.44 mg GALAE per g), tyrosinase inhibition (up to 63.58 mg kojic acid equivalent (KAE) per g), α-amylase inhibition (up to 0.72 mmol acarbose equivalent ACAE per g), and carbonic anhydrase inhibition (CA I IC50 as low as 12.17 µg mL-1). This is the first report of carbonic anhydrase inhibition, BChE-selective activity, cytotoxicity, and comprehensive enzyme-inhibitory data for R. hemisphaerica, R. horrida, and R. pulverulenta. These findings reframe the phytopharmacological potential of Turkish Rosa species beyond their traditionally studied fruit."

Journal • Pain • Tyrosinase

Improvement in Delusional Jealousy and Caregiver Distress After Switching From Oral Galantamine to a Donepezil Transdermal Patch in Alzheimer's Disease: A Case Report. (PubMed, Psychogeriatrics) - "This case suggests that switching from oral galantamine to a donepezil transdermal patch may be associated with improvement in delusional jealousy, selected caregiver-rated NPS domains and caregiver distress in some patients, although causal inference is not possible in a single case and responses may vary."

Journal • Alzheimer's Disease • CNS Disorders • Psychiatry

Treatment Duration of Cholinesterase Inhibitor Formulations in Alzheimer's Disease. (PubMed, J Am Med Dir Assoc) - "In older adults with severe AD, oral cholinesterase inhibitor formulations were continued substantially longer than transdermal patches. Given the limited evidence supporting prolonged cholinesterase inhibitor use in severe AD, these findings raise concerns regarding long-term prescribing practices in advanced dementia care."

Journal • Alzheimer's Disease • CNS Disorders • Dementia

Integrated computational and automated flow synthesis platform for the rapid discovery of N-benzylpiperidine acetylcholinesterase inhibitors. (PubMed, Eur J Med Chem) - "Single-point screening at 5 μM identified ten compounds with ≥70% AChE inhibition, and dose-response determination against electric eel AChE (eeAChE) gave three sub-200 nM inhibitors: 69 (91 nM), 8 (93 nM) and 12 (117 nM), each exceeding galantamine (237 nM) and approaching donepezil (1, 42 nM) under identical assay conditions. The complete cycle was executed in under three months by a three-person team. We report this as a measured platform capability rather than as accelerated drug discovery allowing the rapid generation of first-round leads."

Journal • Alzheimer's Disease • CNS Disorders • Pain

Synthesis of 4-Hydroxyacetophenone-Derived Bis-Schiff Bases as Potent Cholinesterase Inhibitors: In Vitro Evaluation, Molecular Docking, DFT, and ADMET Analysis. (PubMed, Chem Biodivers) - "In the series, compound (2i) was identified as the most promising inhibitor of AChE (IC50 = 14.82 ± 0.09 µM) and BuChE (IC50 = 27.91 ± 0.16 µM) enzymes surpassing the standard drug galantamine, while the remaining derivatives showed good to moderate inhibition...Comprehensive in silico ADMET profiling predicted excellent pharmacokinetic properties for all derivatives, with 96%-100% human oral absorption, moderate blood-brain barrier (BBB) penetration for 2i, and low cardiac toxicity risk. The integrated computational-experimental approach provides supportive evidence for rational design of next-generation cholinesterase inhibitors with optimized efficacy and safety profiles."

Journal • Preclinical • Pain

Biomarkers, Diagnostics, and Emerging Therapies in Alzheimer's Disease: A Comprehensive Systematic Review (2015-2025). (PubMed, Cent Nerv Syst Agents Med Chem) - "This review highlights the critical need for future AD research to bridge identified gaps in early detection, focus on improving early diagnosis, developing more effective treatments, refining existing drugs and therapies, and understanding the underlying disease progression mechanisms."

Biomarker • IO biomarker • Journal • Alzheimer's Disease • CNS Disorders • Gene Therapies • Infectious Disease • Vascular Neurology

Pharmacological interventions targeting cognition and related clinical outcomes in vascular dementia: a systematic review and meta-analysis of randomized controlled trials. (PubMed, Eur J Clin Pharmacol) - "Galantamine and memantine showed small short-term cognitive effects; EGb 761® suggested a fragile, very low-certainty signal; patient-important benefits remain uncertain."

Clinical • Clinical data • Journal • Retrospective data • Review • Alzheimer's Disease • CNS Disorders • Dementia

Safety Comparison of Acetylcholinesterase Inhibitors Using FAERS Spontaneous-Reporting Data: Drug-Specific Reporting Signals and Time-to-Onset Dynamics. (PubMed, Curr Alzheimer Res) - "Donepezil, galantamine, and rivastigmine showed distinct FAERS reporting profiles and early post-initiation TTO patterns. These findings are hypothesis-generating and require confirmation in independent pharmacovigilance or clinical datasets."

Journal • Alzheimer's Disease • Cardiovascular • CNS Disorders • Dermatology • Pruritus

Design, synthesis, biological activity and computational simulation evaluation of pyrimidine-2-aminoacetamide derivatives as cholinesterase inhibitors. (PubMed, Med Chem Res) - "Among them, compound 17v had the most excellent activity, with IC50 values of 0.96 and 7.12 μM for AChE and BuChE, respectively, which were superior to the positive control galantamine (AChE: IC50 = 5.10 μM, BuChE: IC50 = 14.76 μM)...SwissADMET prediction indicated favorable physicochemical properties and drug-likeness profiles. In conclusion, compound 17v represents a promising lead compound for anti-Alzheimer's therapy."

Journal • Alzheimer's Disease • CNS Disorders • Pain

Cholinesterase inhibitors and sexual disinhibition in dementia: a FAERS disproportionality study. (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "Sexual disinhibition under cholinesterase inhibitors (CHEIs; donepezil, rivastigmine, galantamine) appears only as scattered case reports and is largely absent from product labels. The sexual disinhibition signal was reproducible and consistent across all three CHEIs relative to memantine, stronger than for other impulse/reward behaviours and largely absent from current labels. Disproportional reporting reflects relative frequency in the database, not actual harm, and is subject to channelling and detection bias; this exploratory signal warrants prospective study with individual-level temporality and dechallenge/rechallenge data."

Journal • CNS Disorders • Dementia • ROR1

Docking Analysis of Drugs Used in the Treatment of Alzheimer's Disease, Using Cell Membrane Receptors and Enzymes of the Kynurenine Pathway: A Pilot Study. (PubMed, Int J Mol Sci) - "All the drugs tested docked to the kainic acid receptor for glutamate, whereas donepezil, galantamine, tropisetron and N-acetylcysteine docked to the glutamate-NMDA receptor, but none docked to the glutamate-AMPA receptor...Donepezil docked to kynurenine monooxygenase, while rivastigmine, memantine and tropisetron docked to kynurenine aminotransferase-2...Despite their strong docking ability to IDO1 and TDO, none of the compounds tested inhibited their enzyme activity in an assay of kynurenine production. This pilot study highlights the varied pharmacological profile of drugs used in AlzD and suggests that a detailed examination of their functional effects should be considered to assist understanding of their different profiles at on- and off- target sites in human treatment."

Journal • Alzheimer's Disease • CNS Disorders • Pain • IDO1 • PCK2 • TDO2

Dual inhibitory potential of N-methylcytisine against GSK-3β and AChE: implications for Alzheimer's disease treatment. (PubMed, Open Life Sci) - "The results of the integrated in silico workflow indicate that N-methylcytisine exhibited favorable binding to AChE (docking score -9.6 kcal/mol; MM-GBSA -70.2 kcal/mol), comparable to the reference inhibitor galantamine (-10.8 kcal/mol; -70.6 kcal/mol). In contrast, its interaction with GSK-3β was more moderate (-5.3 kcal/mol; -50.3 kcal/mol) relative to staurosporine (-8.5 kcal/mol; -82.6 kcal/mol), consistent with its smaller scaffold. Overall, the results support a flexible, mixed-type interaction profile and highlight N-methylcytisine as a promising dual-acting candidate for Alzheimer's disease."

Journal • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Pain

Novel C3-Aminated Galantamine Derivatives as Selective Butyrylcholinesterase Inhibitors With Neuroprotective Effects. (PubMed, ChemMedChem) - "Preliminary mechanistic study revealed that compound 6l could mitigate oxidative stress and suppress cellular apoptosis. This work not only offers a novel galantamine analog with promising in vitro cholinesterase inhibitory and neuroprotective effects for further anti-AD study, but also provides new insights into the structure optimization of natural drug galantamine."

Journal • Alzheimer's Disease • CNS Disorders • Pain

A Systematic Review of Effects of Cholinesterase Inhibitors and Memantine on Cognitive Domains in Alzheimer's Disease. (PubMed, J Geriatr Psychiatry Neurol) - "Cholinesterase inhibitors (ChEI) (donepezil, rivastigmine and galantamine) and memantine have been the mainstay treatment and have showed their effectiveness on total cognitive scores, but their effects on individual cognitive domains remain unclear. Overall, higher treatment doses were consistently associated with greater preservation of cognitive function across domains.DiscussionChEIs and memantine provide domain-specific cognitive benefits beyond global cognitive improvement. Future studies should examine whether treatment tailored to domain-specific deficits improves patient outcome.PROSPEROCRD42024493998."

Journal • Review • Alzheimer's Disease • CNS Disorders • Cognitive Disorders

A comprehensive assessment of cholinesterase inhibitors for the treatment of Alzheimer's disease based on drug selection recommendations for Chinese Medical Institutions. (PubMed, Expert Rev Pharmacoecon Outcomes Res) - "This study aimed to comprehensively evaluate the overall clinical value of seven ChEI formulations (donepezil tablets, rivastigmine capsules, rivastigmine patches, galantamine tablets, galantamine orally disintegrating tablets, and two huperzine A formulations) to provide evidence-based guidance for rational AD pharmacotherapy selection. The remaining four drugs may be prescribed according to individual patient conditions and institutional available resources. This evaluation provides evidence-based guidance for clinical and institutional decision-making in AD management and delivers a generalizable assessment framework adaptable to local real-world data for healthcare institutions globally."

Journal • Alzheimer's Disease • CNS Disorders

Structure-based identification of novel indole-fused polycyclic derivatives as potent acetylcholinesterase inhibitors. (PubMed, Bioorg Med Chem) - "Among them, compounds 8, 9, 21, and 26 showed leading AChE inhibitory activity with IC50 values of 0.29 μM, 1.5 μM, 1.2 μM, and 1 μM, respectively, which were superior to the positive control galantamine (IC50 = 2.2 μM)...Stable binding interactions between compound 8 and AChE were validated by the results of 100 ns molecular dynamics simulations. Overall, compound 8 was characterized as a potent and well-qualified AChE inhibitor, and further systematic investigations are warranted for its application in the treatment of AD-related diseases."

Journal • Alzheimer's Disease • CNS Disorders • Pain