galantamine hydrobromide / Generic mfg. - LARVOL DELTA

Galantamine-loaded PLGA nanoparticles reduce oxidative stress and inflammation in a rat model of spinal cord injury. (PubMed, Sci Rep) - "Flow cytometry analysis revealed reduced GFAP expression in PLGA and PG-treated groups, indicating decreased astrocyte activation, while neuronal markers (neurofilament-M, βIII-tubulin) and oligodendrocyte markers (O4) showed no significant changes between groups. These results demonstrate that galantamine-loaded PLGA nanoparticles provide superior therapeutic outcomes through targeted anti-inflammatory, antioxidant, and glial modulation mechanisms."

Journal • Preclinical • CNS Disorders • Inflammation • Orthopedics • Solid Tumor • FAP • GFAP • IL1B • IL6

Creatine and Taurine as Novel Competitive Inhibitors of Acetylcholinesterase: A Biochemical Basis for Nutritional Modulation of Brain Function. (PubMed, Int J Mol Sci) - "While clinically approved AChE inhibitors such as donepezil, rivastigmine, and galantamine are used in the symptomatic treatment of Alzheimer's disease and related dementias, little is known about the modulatory effects of common dietary compounds on AChE activity. Docking confirmed that both ligands preferentially occupy the active-site region in a manner consistent with competitive inhibition, with CR showing more favorable binding scores than TA. Although markedly weaker than clinical drugs, these findings provide the first biochemical and in silico evidence that CR and TA directly interact with AChE, suggesting subtle cholinergic modulation relevant to cognitive function and neuroprotection."

Journal • CNS Disorders • Dementia • Pain

Determination of optimum extraction conditions and evaluation of biological activities of Prunus Armeniaca L. (Apricot) fruit. (PubMed, Sci Rep) - "However, when compared to galantamine used as reference inhibitor, it was found that the inhibitory effect of the obtained extracts was lower...In conclusion, the ANN-GA method increases the extraction efficiency of biologically active components of P. armeniaca fruit, strengthening their antioxidant, antiproliferative and anticholinesterase activities. These findings indicate that AI-supported extraction methods have the potential to be used in functional food and pharmaceutical applications."

Journal • Lung Cancer • Oncology • Pain • Solid Tumor

Syzydyerin A, a new unusual C-methylated chalcone isolated from the leaves of Syzygium dyerianum (King) Chantar. & J.Parn. (PubMed, Z Naturforsch C J Biosci) - "Compound 1 exhibited inhibitory activity against acetylcholinesterase (AChE) and lipoxygenase (LOX) with IC50 values of 50.4 ± 0.2 µm and 30.7 ± 0.25 µm, respectively, compared to the reference inhibitors galantamine (IC50 = 40.7 ± 0.12 µm) for AChE and quercetin (IC50 = 3.5 ± 0.13 µm) 5-LOX. Molecular docking analysis revealed that compound 1 exhibits strong binding affinities toward AChE (-11.0 kcal/mol) and 5-LOX (-9.1 kcal/mol), comparable to standard inhibitors, with key π-π stacking and hydrogen bonding interactions stabilizing its binding at both active sites, highlighting its promising dual inhibitory potential. The study underscores the value of S. dyerianum as a source of bioactive compounds with potential applications in treating neuroinflammatory diseases."

Journal • Inflammation • Pain

An Updated Comprehensive Review on Phytochemical Crinum L. genus Alkaloids (2013-2025): Unlocking Their Anticancer Potential. (PubMed, Phytochemistry) - "These organs are rich in lycorine-, crinine-, and galantamine-type alkaloids, which exhibit potent cytotoxicity against various cancer cell lines...It provides a holistic and updated overview of Crinum L. alkaloids from 2013 to 2025, including their biosynthetic pathways, structural classification, and biological activities, with an emphasis on their potential in cancer therapeutics. Additionally, future research directions are proposed, including the development of advanced drug delivery systems, synthetic modifications, and clinical applications, to bridge the gap between phytochemical studies and medical applications."

Journal • Review • Oncology

Novel Assembling of Furano-Fused Azepinone Derivatives for Inhibition of Acetylcholinesterase Responsible for Alzheimer's Disease: Synthesis, Molecular Docking, DFT, In Vitro, and In Silico Studies. (PubMed, ACS Chem Neurosci) - "In vitro antiacetylcholinesterase (AchE) activity revealed that compound 5n (IC50= 2.38 ± 0.02 nM) showed higher inhibitory activity than reference drugs galantamine (IC50 = 2.84 ± 0.01 nM)...The combined experimental and computational investigation revealed that 5n exhibits significant anti-AchE activity and warrants further exploration for its medicinal utility in Alzheimer's disease and related challenges. The design, synthesis, and AchE inhibitory properties of the synthesized furano-azepinone derivatives were patented under Indian patent number 202511048244."

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

Synthesis, biological evaluation and molecular docking of novel 2-pyrazoline-1-carboxamides as anti-Alzheimer agents. (PubMed, Future Med Chem) - "In silico studies showed that compound 7 binds to both targets with higher affinity than the reference compound, galantamine. ADME studies also showed that compound 7 can cross the blood-brain barrier."

Journal • Alzheimer's Disease • CNS Disorders • Pain

Exploring the selective butyrylcholinesterase inhibition potential of phenol carbamates: Experimental and computational study. (PubMed, Eur J Med Chem) - "The most potent inhibitor, compound 13, bearing a pyrrolidine moiety, exhibited an IC50 value of 0.045 μM, outperforming the reference drug galantamine by more than two orders of magnitude...In vitro cytotoxicity assays in HepG2 cells confirmed the absence of toxicity at concentrations up to 30 μM. These results highlight methoxy-substituted phenol carbamates, particularly compound 13, as promising lead structures for the design of selective BChE inhibitors and potential therapeutic agents for the treatment of AD."

Journal • Alzheimer's Disease • CNS Disorders • Pain

Metabolomic Based Insight Reveals a few Metabolites at Various Germination Stages of Black Rice, Demonstrating Potential Efficacy Against Dementia and Other Neurodegenerative Conditions. (PubMed, Appl Biochem Biotechnol) - "Among the compounds identified in the black rice extract, benzene-1,2,4-triol, pyrogallol, hydroquinone, and phloroglucinol* (reported for the first time) exhibited superior activity than the standard drug galantamine. Furthermore, the combination of these authentic compounds with the standard drug (galantamine) showed promising results in reducing the complications associated with the synthetic drug in both in vitro and in silico studies."

Journal • CNS Disorders • Dementia

Comparative safety of cholinesterase inhibitors and memantine for dementia: a protocol for a network meta-analysis of randomized controlled trials. (PubMed, Syst Rev) - "By addressing gaps in prior NMAs, this study aims to provide an in-depth evaluation of safety outcomes associated with different ChEI and memantine doses and formulations across various dementia types. The findings will support clinicians in making informed treatment decisions and guide future research and policy development for dementia management."

Journal • Retrospective data • CNS Disorders • Dementia

Sustainable Extraction of Alkaloids from Worsleya procera: Improving the Method with Green Chemistry. (PubMed, ACS Omega) - "Galantamine, used as a positive control, inhibited both enzymes by >97%, validating the bioassay. These findings demonstrate that greener extraction strategies not only reduce environmental impact but also preserve biological activity, positioning the proposed methodology as a sustainable alternative for natural product research."

Journal

Dual targeting of neuroblastoma and cholinesterase by morpholino/pyrrolidino-sulfonyl-indole thiosemicarbazones: Synthesis, characterization, enzyme inhibition, cytotoxicity, docking and dynamics studies. (PubMed, Bioorg Chem) - "Compounds 6h and 7h stood out as the most potent inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 values as low as 0.15 μM and 0.12 μM, respectively, outperforming reference drugs tacrine and galantamine. Molecular dynamics simulations over 250 ns confirmed complex stability with low RMSD and RMSF values. These combined results highlight 6h and 7h as promising multitarget therapeutic candidates for neurodegenerative diseases and cancer."

Journal • CNS Disorders • Neuroblastoma • Oncology • Pain • Solid Tumor

Effect of Alzheimer's disease medications on neurocognitive outcomes in children and adolescents with autism spectrum disorder and low IQ: a scoping review. (PubMed, Transl Psychiatry) - "This scoping review identified promising evidence of neurocognitive improvement in children and adolescents with ASD and low IQ following treatment with either a cholinesterase inhibitor or an NMDA receptor antagonist. Considering the lack of FDA-approved treatments for the cognitive deficits associated with ASD and an absence of medications approved to treat core features of ASD, our findings highlight an opportunity for innovative directions in autism research and treatment."

Journal • Review • Alzheimer's Disease • Autism Spectrum Disorder • CNS Disorders • Cognitive Disorders • Developmental Disorders • Genetic Disorders • Mental Retardation

Functional characterization of aldo-keto reductase genes from Lycoris aurea that participate in galantamine biosynthesis. (PubMed, Plant Sci) - "LauAKR1 and LauAKR2 facilitated the NADPH-dependent reduction of the substrates demethylnarwedine and narwedine. This study provides direct evidence that LauAKR catalyzes the crucial reduction reactions involved in the formation of galantamine."

Journal

Exploring chemical composition, anti-acetylcholinesterase, and anticancer activities of Pistacia atlantica Desf. (PubMed, Pharm Biol) - "The results, compared with galantamine, showed a close inhibition activity...atlantica extracts also showed the most optimal antiproliferative and cytotoxic effect against cancer cell lines compared to positive control 5FU (Fluorouracil); the best antiproliferative activity was obtained for the fruit extracts compared to the leaf extracts...This study demonstrated moderate anticholinesterase and suitable antiproliferative activities of P. atlantica Desf. extracts, which opens up new possibilities for the pharmaceutical and food industries.This study suggests that the concentrations of phenolic compounds, along with the results of anticholinesterase and antiproliferative activities found in the fruit and leaf extracts of P. atlantica Desf, indicate this plant holds promise for pharmaceutical and food application industries."

Journal • Oncology • Pain

Galantamine reverses habitual responding induced by adolescent binge alcohol exposure in rats (Neuroscience 2025) - "Rats received either banana or chocolate flavored sucrose pellets during these training sessions, then the reward was devalued by a sensory-specific satiation procedure in which rats received access to either the same training flavor for devaluation or a novel flavor ad libitum before an extinction session.Behavior during the extinction session revealed that saline-treated AIE rats did not decrease responding to the devalued flavor, whereas galantamine treated AIE rats and saline-treated control rats showed the traditional suppression of lever pressing for the devalued flavor. These results suggest that galantamine may rescue AIE-induced impairments in behavioral flexibility by enhancing cholinergic signaling in the OFC."

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

Neuroprotective effects of the neurotrophic factors carbamoylated erythropoietin and insulin-like growth factor-1 in Alzheimer's disease (Neuroscience 2025) - "To do this work, male and female 5xFAD mice bred from both maternal and paternal origin were intraperitoneally injected with CEPO, IGF-1, CEPO+IGF-1, Galantamine, or vehicle starting at two months of age, before cognitive deficits are present, until nine months of age...These results demonstrate a clear sex-specific difference in the neuroprotective effects of CEPO and IGF-1 in protecting against cognitive decline, with these neurotrophic factors being effective in male but not female mice. Our data also suggest that combining two neurotrophic factors may not be more effective than their individual treatment; however, more studies looking at different dosing and timing regimens should be pursued in the future."

Alzheimer's Disease • CNS Disorders • Cognitive Disorders • IGF1

Galantamine-Induced Akathisia in a Patient With Alzheimer Dementia. (PubMed, Am J Ther) - No abstract available

Journal • Alzheimer's Disease • CNS Disorders • Dementia

Persistence With Antidementia Therapy in Germany: A Retrospective Cohort Study of 212,850 Patients (ISPOR-EU 2025) - "In this large-scale retrospective cohort study, two-thirds of patients discontinued antidementia therapy within three years, with younger age, female sex, and use of rivastigmine, donepezil, or galantamine linked to higher discontinuation risks. Initiation by a neuropsychiatrist was associated with improved persistence among the oldest patients, highlighting the potential impact of prescriber specialty on long-term therapy adherence."

Retrospective data • CNS Disorders • Psychiatry

Care Dependency and Sick Leave Patterns in Early Alzheimer's Disease: A Retrospective Claims Data Analysis in Germany (ISPOR-EU 2025) - "Early AD was defined as de-novo prescriptions of AChE inhibitor (AChEIs: donepezil, galantamine, or rivastigmine) in individuals aged ≥50 years (index), without memantine prescriptions within 100-days. Care dependency emerges early in AD. Sick leave - especially related to psychiatric comorbidities - may serve as early indicators. Earlier recognition and intervention may delay care dependency and preserve independence."

Retrospective data • Alzheimer's Disease • CNS Disorders • Depression • Psychiatry

Application of Artificial Neural Network to Determine Optimum Formulation Development and In Vitro Characterization of Methylene Blue and Galantamine Loaded Polymeric Nanoparticles for the Treatment of Alzheimer's Disease. (PubMed, Eur J Pharm Sci) - "Artificial neural network models demonstrated high predictive accuracy, serving as a valuable tool for formulation optimization. This dual-drug, surface-modified nanoparticle approach offers promising potential for multi-target therapy in Alzheimer's disease."

Journal • Preclinical • Alzheimer's Disease • CNS Disorders

Melissa officinalis essential oil modulates oxidative balance, cholinergic activity, and cognitive performance in a scopolamine-induced zebrafish model: implications for neuroprotective strategies in cognitive disorders. (PubMed, Sci Rep) - "MEO was administered daily for 21 days, whereas SCO and the reference drug galantamine (GAL, 1 mg/L) were administered acutely before behavioral testing. In silico ADMET predictions for MEO's major constituents (citral, β-caryophyllene, limonene, and α-pinene) indicated high gastrointestinal absorption, blood-brain barrier permeability, and favorable safety profiles, with no predicted mutagenic or hepatotoxic effects. Collectively, these findings support the neuroprotective and anxiolytic potential of MEO in a zebrafish model of cognitive dysfunction and suggest its promise as a candidate for further investigation in neurodegenerative disease research."

Journal • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Developmental Disorders • Mood Disorders • Pain • Psychiatry

Differential cognitive enhancer effects of acetylcholinesterase inhibitors and memantine on age-related deficits in vigilance and sustained attention: a preclinical validation study. (PubMed, Behav Brain Funct) - "Here, we showed that PVT is suitable for addressing pharmacological effects on various cognitive domains in a single behavioral paradigm. Our findings also indicate that different cognitive enhancer compounds (even when their targets are thought to be the same) may differentially influence distinct cognitive domains and modulate task performance."

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

Megastigmane and guaiane-type glycosides with cholinesterase inhibitory effects from Ceriscoides campanulata leaves. (PubMed, Fitoterapia) - "Both compounds were less potent than the reference drug galantamine. Notably, for the first time, the acetylcholinesterase inhibitory activities of compounds 1 and 2 were also confirmed in cellular model using SH-SY5Y human neuroblastoma cells, further supporting their potential neuroprotective effects."

Journal • Diabetes • Metabolic Disorders • Neuroblastoma • Oncology • Pain • Solid Tumor

Metabolite Profiling and Bioactivity of Eastern Algerian Posidonia oceanica: Cholinesterase and Urease Inhibition with Low Cytotoxicity. (PubMed, ACS Omega) - "The rhizome extract showed IC50 values of 20.52 ± 0.75 μg/mL for urease and 33.59 ± 0.73/11.82 ± 0.73 μg/mL for AChE and BChE, respectively, demonstrating comparable or even superior activity to reference inhibitors such as thiourea and galantamine...The phenolic compounds in P. oceanica exhibited promising multitarget inhibitory activity, particularly in the medical field for treating neurodegenerative diseases and urease-related infections. The observed moderate cytotoxicity indicates an acceptable safety margin, enhancing their value as a natural source for applications in medical, veterinary, agricultural, and environmental fields."

Journal • CNS Disorders • Infectious Disease • Pain