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Phenylpiracetam (PP) is a nootropic drug with additional pharmacological effects, including anxiolytic, antiasthenic, antidepressant, anti-inflammatory and anticonvulsant effects. The paper presents the results of an analysis of experimental and clinical studies, which indicate the prospects for the use of PP in cerebral ischemia, neurodegenerative pathologies, epilepsy, asthenia, and mental disorders. The adaptogenic properties and mitochondrial protective effect of PP are considered, assessments of the possible effect of PP on neurotransmitter systems, regulation of carbohydrate and fat metabolism with the prospects for the use of PP in patients with metabolic syndrome.

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Cognitive decline is commonly seen both in normal aging and in neurodegenerative and neuropsychiatric diseases. Various experimental animal models represent a valuable tool to study brain cognitive processes and their deficits. Equally important is the search for novel drugs to treat cognitive deficits and improve cognitions. Complementing rodent and clinical findings, studies utilizing zebrafish (Danio rerio) are rapidly gaining popularity in translational cognitive research and neuroactive drug screening. Here, we discuss the value of zebrafish models and assays for screening nootropic (cognitive enhancer) drugs and the discovery of novel nootropics. We also discuss the existing challenges, and outline future directions of research in this field.

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Molecular hydrogen (H2, dihydrogen) is an antioxidant and signaling molecule with potent antioxidative, antiapoptotic, and anti-inflammatory properties. Despite the growing interest in H2 as a potential therapeutic agent, the evidence regarding its potential as a nootropic remains limited. Only a handful of studies on the human population have evaluated its effects, although there are suggestive indications of its efficacy. The present paper overviews H2's potential as a novel agent for improving cognitive functions in health and disease contexts, highlighting its mechanisms of action and areas for further investigation. Current evidence suggests that H2 improves executive function, alertness and memory in several clinical trials, from healthy young and elderly individuals to individuals with altered circadian rhythms, neurodegenerative disorders, and cancer. Further investigations are needed to confirm the potential positive effects of dihydrogen as a nootropic agent in both health and disease.

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Leukocyte elastase is a marker of inflammation. Previously, a relationship was found between the severity of mental disorders in patients and elastase-like activity of blood plasma. The effect of various neurotropic drugs on leukocyte elastase activity was analyzed in an in vitro experiment. We revealed an inhibitory effect of the benzodiazepine tranquilizers diazepam and bromodihydrochlorophenylbenzodiazepine and immunomodulators aminodihydrophthalazinedione and diclofenac on the plasma elastase-like activity of healthy donors and pure human neutrophil elastase. The antipsychotics chlorpromazine and alimemazine, as well as the nootropic vinpocetine increased elastase-like activity in a dose-dependent manner. The activating effect of chlorpromazine and vinpocetine, but not alimemazine, was reproduced in neutrophil elastase. We hypothesized that these drugs can affect the development of inflammatory reactions in the complex therapy of mental disorders.

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OBJECTIVE: To explore the concept of, ethics surrounding, and arguments for and against cosmetic psychiatry. CONCLUSIONS: Cosmetic psychiatry may be defined as the science and practice of interventions that subjectively enhance the mental states of healthy people. Cosmetic medicine (including surgery) is a professionally and socially accepted part of contemporary medical practice; cosmetic psychiatry is not. Like cosmetic medicine, there are significant risks associated with cosmetic psychiatry. There is an urgent need for a broader conversation about this emerging clinical reality.

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OBJECTIVES: To examine the efficacy of acute consumption of a novel energy drink (C4S) versus placebo for improving cognitive and gaming performance and mood. Secondarily, we examined the cardiovascular safety profile of acute C4S consumption. METHODS: Forty-five healthy, young adult video gamers completed two experimental visits in randomized order where they consumed either C4S or a placebo and then completed a validated battery of neurocognitive tests, played five video games, and completed a mood state survey. Blood pressure (BP), heart rate (HR), oxygen saturation, and electrocardiogram measurements were taken at baseline and repeated throughout each visit. RESULTS: Acute consumption of C4S improved cognitive flexibility (absolute mean or median difference [95% CI] = +4.3 [2.2-6.4]; p < 0.001; d = 0.63), executive function (+4.3 [2.3-6.3]; p < 0.001; d = 0.63), sustained attention (+2.1 [0.6-3.6]; p = 0.01; d = 0.44), motor speed (+2.9 [0.8-4.9]; p < 0.001; d = 0.44), psychomotor speed (+3.9 [0.1-7.7]; p = 0.04; d = 0.32) working memory (+1.0 [0.1-1.9]; p = 0.02; d = 0.35), and performance in the two-dimensional visuospatial game Tetris (+463 [-419-2,065] pts; p = 0.049; d = 0.30) compared to placebo. C4S also improved Fatigue-Inertia (-1 [-3-0]; p = 0.004; d = 0.45), Vigor-Activity (+2.4 [1.3-3.6]; p < 0.001; d = 0.64), Friendliness (+0 [0-1]; p = 0.04; d = 0.32), and Total Mood Disturbance (-3 [-6-0]; p = 0.002; d = 0.44). BP increased slightly in C4S versus placebo, while HR decreased from baseline to post-drink in the C4S condition. Rate-pressure-product was higher in C4S versus placebo independent of time but did not increase from baseline. There was no effect on corrected QT interval. CONCLUSION: Acute consumption of C4S was efficacious for cognitive performance, visuospatial gaming performance, and mood enhancement, and had no effect on myocardial oxygen demand or ventricular repolarization, despite being associated with increases in BP.

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The aim of this study was to assess the effects of guayusa extract and Nordic Lion's Mane (LM) on cognition. Using a randomized, double-blind, placebo-controlled, crossover design, we examined the effects of a single dose of 650 mg guayusa extract (AMT: AmaTea® Max) vs. 1 g Nordic-grown Lion's Mane (LM) vs. placebo (PL). Participants attended three testing visits consisting of neuropsychological tests (Go/No-go, N-Back, and Serial 7 s tasks) assessing performance, subjective assessments of cognitive perception, and vital signs. Each assessment was measured at baseline (pre-ingestion) and 1 and 2 h post ingestion. AMT significantly (p ≤ 0.05) improved the number of attempts during Serial 7s, total score, number of correct responses, total number of responses, and reaction time during N-Back and improved Go stimulus reaction time, but it reduced the percentage of correct responses in the No-go stimulus response during Go/No-go. LM significantly (p ≤ 0.05) improved the number of attempts during Serial 7s and reaction time during N-Back and improved Go stimulus reaction time in Go/No-go. AMT improved mental clarity, focus, concentration, mood, and productivity at 1 and 2 h (p < 0.05); the ability to tolerate stress at 1 h; and had greater ratings than LM and PL for mental clarity, focus, concentration, and productivity. PL improved focus and concentration at 1 h from baseline (p ≤ 0.05). AMT and LM improved subjective ratings of "happiness compared to peers" and "getting the most out of everything" (p < 0.05); however, this occurred earlier in LM (i.e., 1 h post ingestion). AMT uniquely elevated blood pressure from baseline. AMT significantly improved cognitive performance and self-perceived cognitive indices of affect over a 2 h period and perceptions of happiness 2 h post ingestion. In comparison, LM helped improve working memory, complex attention, and reaction time 2 h post ingestion and perceptions of happiness over a 2 h period.

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BACKGROUND: Myrtus communis L. (MC) has been used in Mesopotamian medicine. Here, the cholinesterase (ChE) inhibitory potential of its methyl alcohol extracts has been investigated and computationally dissected. METHOD: The ChE inhibition has been measured based on usual Ellman's colorimetric method compared to a canonical ChE inhibitor, eserine. Through a deep text mining, the structures of phytocompounds (= ligands) of MC were curated from ChemSpider, PubChem, and ZINC databases and docked into protein targets, AChE (PDB 1EVE) and BChE (PDB 1P0I) after initial in silico preparedness and binding affinity (BA; kcal/mol) reported as an endpoint. The calculation of ADMET (absorption, distribution, metabolism, excretion, and toxicity) features of phytocompounds were retrieved from SwissADME ( http://www.swissadme.ch/ ) and admetSAR software to predict the drug-likeness or lead-likeness fitness. The Toxtree v2.5.1, software platforms ( http://toxtree.sourceforge.net/ ) have been used to predict the class of toxicity of phytocompounds. The STITCH platform ( http://stitch.embl.de ) has been employed to predict ChE-chemicals interactions. RESULTS: The possible inhibitory activities of AChE of extracts of leaves and berries were 37.33 and 70.00%, respectively as compared to that of eserine while inhibitory BChE activities of extracts of leaves and berries of MC were 19.00 and 50.67%, respectively as compared to that of eserine. Phytochemicals of MC had BA towards AChE ranging from -7.1 (carvacrol) to -9.9 (ellagic acid) kcal/mol. In this regard, alpha-bulnesene, (Z)-gamma-Bisabolene, and beta-bourbonene were top-listed low toxic binders of AChE, and (Z)-gamma-bisabolene was a more specific AChE binder. Alpha-cadinol, estragole, humulene epoxide II, (a)esculin, ellagic acid, patuletin, juniper camphor, linalyl anthranilate, and spathulenol were high class (Class III) toxic substances which among others, patuletin and alpha-cadinol were more specific AChE binders. Among intermediate class (Class II) toxic substances, beta-chamigrene was a more specific AChE binder while semimyrtucommulone and myrtucommulone A were more specific BChE binders. CONCLUSION: In sum, the AChE binders derived from MC were categorized mostly as antiinsectants (e.g., patuletin and alpha-cardinal) due to their predicted toxic classes. It seems that structural amendment and stereoselective synthesis like adding sulphonate or sulphamate groups to these phytocompounds may make them more suitable candidates for considering in preclinical investigations of Alzheimer's disease.

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This study assessed the acute effects of oral methylliberine (DynamineTM) supplementation on cognitive function and indices of well-being. This was a double-blind, randomized, within-subject crossover trial. In total, 25 healthy men and women (33.5 ± 10.7 yr, 172.7 ± 8.6 cm, 73.3 ± 11.0 kg) underwent pretesting before ingesting methylliberine (100 mg) or a placebo (PLA) for 3 days. On the fourth day, the participants were tested before their fourth dose (baseline) and every hour post-ingestion for 3 h. After a one-week washout period, the participants repeated testing with the alternate investigational product. The testing battery consisted of vitals, Stroop test, Trail Making Test-B, and visual analog scales that assessed various indices of well-being. Mixed factorial ANOVAs with repeated measures were used to assess all variables. There were significant (p ≤ 0.050) interactions in terms of concentration, motivation, and mood. Methylliberine improved concentration at 1 and 3 h, motivation at 3 h, and mood at 1, 2, and 3 h (p ≤ 0.050). Methylliberine improved energy, sustained energy, and mood in all participants to a greater extent than PLA at 1 h and 3 h relative to baseline (p ≤ 0.050). PLA improved motivation at 1 and 2 h and mood at 2 h (p ≤ 0.050). Methylliberine improved concentration, well-being, and the ability to tolerate stress to a greater extent than PLA at 3 h relative to baseline (p ≤ 0.050). Women observed elevations in sustained energy at 1 and 3 h (p ≤ 0.050) with methylliberine vs. PLA. Methylliberine had a negligible influence on cognitive function and vitals (p > 0.050), and no adverse events were reported. Methylliberine significantly improved subjective feelings of energy, concentration, motivation, and mood, but not cognitive function. PLA improved motivation and mood at hours 1 and 2, while methylliberine sustained these benefits for longer. Methylliberine also improved concentration, well-being, and the ability to tolerate stress to a greater degree than PLA, while having no detrimental effects on vital signs. Methylliberine also seemed to have a positive impact on sustained energy in women.

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Background: esports, or organized video game competitions, have been expanding quickly. The use of dietary supplements by esports players appears vulgarized but lacks supporting evidence. Objectives: To outline studies that tested the effects of dietary supplements on video gaming, summarize their findings, highlight knowledge gaps, and recommend future research. Eligibility criteria: Clinical trials published in English between 1990 and 2023 that assessed the effects of dietary supplements on the cognitive performance of video gamers. Sources of evidence: The Web of Science, PubMed, Scopus, and Google Scholar databases. Charting methods: PRISMA's (2020) flow diagram was used to create the data chart. Results: Sixteen studies were outlined. Thirteen were randomized, thirteen applied acute interventions, ten applied a crossover design and only three weren't placebo-controlled. Of the 10 studies that included caffeine (40-200 mg), four reported significant positive effects on cognition (attention, processing speed, working memory), two on first-person shooter video gaming performance (reaction time, hit accuracy, time to hit 60 targets), and one on Tetris game score. All 3 studies that included arginine silicate (1500 mg) reported significant improvements in one or more aspects of cognition (reaction time, attention, visual representation, and spatial planning). Two studies that tested sucrose (21 and 26.8 g) didn't report significant improvements, while one study that tested 26.1 g of glucose registered significant positive effects on processing speed and sustained attention. Conclusions: The published literature has focused on the effects of caffeine, which may exert both positive and negative effects on esports players. Additional, high-quality research is needed.

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Opioid Use Disorders (OUDs) are often associated with cognitive impairments, which may lead to an increased risk of relapse. These cognitive deficits do not resolve with abstinence or medication-assisted treatment and may require targeted management. While psychotherapies and neuromodulation techniques have been studied for their effectiveness, they have certain limitations and challenges. Cognition enhancing prescription drugs like donepezil and memantine, which are used in dementias, have shown promise in a small number of studies examining their role in the reversal of opioid-induced cognitive deficits. The authors explore the potential role of nootropics in improvement of cognitive decline associated with OUDs.

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The first nootropic prohibited in sport was fonturacetam (4-phenylpiracetam, carphedon) in 1998. Presented here 25 years later is a broad-scale consideration of the history, pharmacology, prevalence, regulations, and doping potential of nootropics viewed through a lens of 50 selected dietary supplements (DS) marketed as "cognitive enhancement," "brain health," "brain boosters," or "nootropics," with a focus on unauthorized ingredients. Nootropic DS have risen to prominence over the last decade often as multicomponent formulations of bioactive ingredients presenting compelling pharmacological questions and potential public health concerns. Many popular nootropics are unauthorized food or DS ingredients according to the European Commission including huperzine A, yohimbine, and dimethylaminoethanol; unapproved pharmaceuticals like phenibut or emoxypine (mexidol); previously registered drugs like meclofenoxate or reserpine; EU authorized pharmaceuticals like piracetam or vinpocetine; infamous doping agents like methylhexaneamine or dimethylbutylamine; and other investigational substances and peptides. Several are authorized DS ingredients in the United States resulting in significant global variability as to what qualifies as a legal nootropic. Prohibited stimulants or ß2-agonists commonly used in "pre-workout," "weight loss," or "thermogenic" DS such as octodrine, hordenine, or higenamine are often stacked with nootropic substances. While stimulants and ß2-agonists are defined as doping agents by the World Anti-Doping Agency (WADA), many nootropics are not, although some may qualify as non-approved substances or related substances under catch-all language in the WADA Prohibited List. Synergistic combinations, excessive dosing, or recently researched pharmacology may justify listing certain nootropics as doping agents or warrant additional attention in future regulations.

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OBJECTIVES: This study aimed to investigate the efficacy of taking Mind Lab Pro, a plant-based nootropic on memory in a group of healthy adults. Auditory, visual, visual working memory, immediate and delayed recall (DR) were assessed. METHODS: The study employed a pseudo randomised, double blinded, placebo-controlled design. A total of 49 healthy individuals completed the study with 36 in the experimental group and 13 in the control group. Participants ranged between 20 and 68 years with a mean age of 31.4 ± 14.4 years. Pre and post taking either the Mind Lab Pro supplement or placebo for 30 days. All participants completed the Wechsler Memory Scale Fourth UK Edition (WSM-IV UK). RESULTS: We found that the experimental group significantly improved in all memory subtests assessed (p < 0.05) whilst the control group only significantly improved in auditory memory and immediate recall (p = 0.004 and p = 0.014 respectively). A significant difference in immediate and DR was also found between the control and experimental group (p = 0.005 and 0.034 respectively). CONCLUSION: The use of Mind Lab Pro for 4 weeks improves memory with the experimental group significantly improving in all sub areas of memory as assessed by the WSM-IV UK.

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Substances with modulatory capabilities on certain aspects of human cognition have been revered as nootropics from the dawn of time. The plant kingdom provides most of the currently available nootropics of natural origin. Here, in this systematic review, we aim to provide state-of-the-art information regarding proven and unproven effects of plant-derived nootropics (PDNs) on human cognition in conditions of health and disease. Six independent searches, one for each neurocognitive domain (NCD), were performed in parallel using three independent scientific library databases: PubMed, Cochrane and Scopus. Only scientific studies and systematic reviews with humans published between January 2000 and November 2021 were reviewed, and 256 papers were included. Ginkgo biloba was the most relevant nootropic regarding perceptual and motor functions. Bacopa monnieri improves language, learning and memory. Withania somnifera (Ashwagandha) modulates anxiety and social-related cognitions. Caffeine enhances attention and executive functions. Together, the results from the compiled studies highlight the nootropic effects and the inconsistencies regarding PDNs that require further research.Supplemental data for this article is available online at https://doi.org/10.1080/10408398.2021.2021137.

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Phenibut is a misused substance which has shown an increase in use over the past decade. Marketed as a "dietary supplement," it is not approved in the United States for use and is not regulated by the Food and Drug Administration. The substance, however, is readily available for purchase through online markets. It has a similar drug profile as alcohol, gabapentin and benzodiazepines. Clinical effects of this drug include physiologic dependence, euphoria, anxiolysis, antispasticity, sedation, and possible nootropic properties. While there are emerging new cases of managing phenibut withdrawal, no cases currently feature phenibut addiction and withdrawal management in the geriatric population. Here we discuss such a case of phenibut addiction and withdrawal in a 68-year-old male who initially began misusing phenibut to alleviate anxiety and insomnia precipitated by worsening affective disorder, sedative, hypnotic, or anxiolytic use disorder, and alcohol use disorder.

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The objective of this paper is to look at how natural medicines can improve cognition and memory when used with sildenafil, a popular erectile dysfunction medicine that also has nootropic properties. Newer treatment strategies to treat the early stages of these diseases need to be developed. Multiple factors lead to complex pathophysiological conditions, which are responsible for various long-term complications. In this review, a combination of treatments targeting these pathologies is discussed. These combinations may help manage early and later phases of cognitive impairments. The purpose of this article is to discuss a link between these pathologies and a combinational approach with the objective of considering newer therapeutic strategies in the treatment of cognitive impairments. The natural drugs and their ingredients play a major role in the management of disease progression. Additionally, their combination with sildenafil allows for more efficacy and better response. Studies showing the effectiveness of natural drugs and sildenafil are mentioned, and how these combinations could be beneficial for the treatment of cognitive impairments and amnesia are summarised. Furthermore, preclinical and clinical trials are required to explore the medicinal potential of these drug combinations.

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Objetivos: analisar a qualidade do sono de estudantes de medicina em uma universidade privada brasileira e sua associação com o uso não prescrito de nootrópicos (metilfenidato, lisdexanfetamina e modafinil). Métodos: a qualidade do sono foi analisada utilizando-se o questionário de Pittsburgh (PSQI). Considerou-se um questionário sociodemográfico para identificação psicossocial dos participantes e uso de nootrópicos. Os resultados foram representados como média e desvio-padrão (para as variáveis quantitativas) ou frequência (para as qualitativas), e as associações foram analisadas pelo teste de qui-quadrado. Resultados: responderam ao questionário 362 alunos. Os níveis médios de PSQI global em estudantes com uso recente não prescrito de nootrópicos foi semelhante ao observado para estudantes que nunca usaram nootrópicos (7,76 vs. 7,73; p=0,96). A análise do PSQI por domínio específico também não mostrou diferença estatisticamente significativa. Observou-se que 23,6% das mulheres e 33,9% dos homens tiveram boa qualidade do sono, sendo essa diferença estatisticamente significativa (p=0,04). O uso de seis doses ou mais de bebida alcoólica esteve relacionado com níveis mais altos do PSQI (7,47 vs. 8,19; p=0,047). Alunos com qualidade do sono ruim apresentaram menor satisfação com a escolha profissional (OR = 1.84; IC95%= 1.09 - 3.11), menor percepção de aquisição de habilidades (OR = 1.96; IC95% = 1.16 - 3.31) e maior proporção de pensamentos relacionados a abandonar o curso (OR = 0,46; IC95% = 0,27 - 0,77). O uso recente e não prescrito de nootrópicos esteve associado ao uso de maconha e ao desejo de abandonar o curso. Conclusões: a qualidade do sono foi pior no sexo feminino e naqueles com maior ingestão de álcool; esteve associada à menor satisfação com escolha profissional e desejo de abandono do curso

Aims: analysing the quality of sleep of the medical students at a private university and its association with the non-prescription use of nootropics (methylphenidate, lisdexamfetamine and modafinil). Methods: the sleep quality was analyzed by using the Pittsburgh Sleep Quality Index. A sociodemographic questionnaire was considered to identify the psychosocial characteristics of the participants and the use of nootropics. Results were represented as mean and standard deviation (for quantitative variables) or frequency (for qualitative variables), and associations were analyzed using the chisquare test. Results: 362 students answered the questionnaire. The medium levels of global PSQI in students with recent unprescribed use of nootropics was like that observed for students who had never used nootropics (7.76 vs.7.73; p=0.96). The PSQI analysis by specific domain also showed no statistically significant difference for any domain. It was observed that 23.6% of women and 33,9% of men had good sleep quality, with this difference being statistically significant (p=0.04). The use of six doses or more of alcoholic beverages was related to higher levels of PSQI (7.47 vs. 8.19; p=0.047). Students with poor sleep quality had less satisfaction with their professional choice (OR = 1.84; 95% CI= 1.09 - 3.11), lower perception of skills acquisition (OR= 1.96; 95%CI = 1.16 - 3.31) and a higher proportion of thoughts related to dropping out of the course (OR = 0.46; 95%CI = 0.27 - 0.77). Recent and non-prescription use of nootropics was associated with marijuana use and the desire to drop out of the course. Conclusions: sleep quality was worse in females and in those with higher alcohol intake, and was associated with lower satisfaction with professional choice and desire to drop out of the course. No association was found between non-prescription use of nootropics and sleep quality in medical students

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Noopept (NP) is a proline-containing dipeptide with nootropic and neuroprotective properties. We have previously shown that NP significantly increased the frequency of spontaneous IPSCs in hippocampal CA1 pyramidal cells mediated by the activation of inhibitory interneurons in stratum radiatum. The cholinergic system plays an important role in the performance of cognitive functions, furthermore multiple behavioral and clinical facts link NP with the cholinergic system. The present study was undertaken to reveal the possible interaction of NP with neuronal nicotinic acetylcholine receptors (nAChRs). Currents were recorded from rat hippocampal neurons using the whole-cell, patch-clamp technique. NP (5 µM) increased the action potential firing frequency recorded from GABAergic interneurons in the stratum radiatum (SR) of CA1 region. This effect was almost completely abolished by the application of the α7 nAChR-selective antagonists α-bungarotoxin (α-BGT; 6 nM) and methyllycaconitine (MLA; 20 nM). The increase in the frequency of spontaneous IPSCs in CA1 pyramidal cells induced by NP was also eliminated by α7 nAChRs antagonists. These results imply the involvement of α7 nAChRs in the modulation of hippocampal neuronal activity caused by NP and indicate that a7 nAChRs are an important site of action of NP.

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BACKGROUND: The use of cognitive-enhancing medications and supplements among healthy adults continues to rise. Limited data exists on their use among resident physicians. Given their highly competitive and stressful lifestyle, we sought to evaluate the prevalence, motivations, and side effects of using cognitive-enhancing supplements and medications among resident physicians at a large United States academic institution. METHODS: An anonymous web-based survey was circulated to resident physicians inquiring about using cognitive-enhancing supplements and medications, as well as personal characteristics such as gender, marital and parental status, medical diagnoses, and medical specialty. Before circulation, we performed a pilot study. Weighted logistic regression analyses estimated the impact of personal characteristics on the probability of using both supplements and medications. RESULTS: Survey response rate was 46.4%. Of respondents, 48.6% were female, 45.9% were married, 70.9% were without children, and 67.2% were in a non-surgical medical specialty. Few respondents had a related medical diagnosis, with attention deficit hyperactivity disorder being the most common (7.1%). Male, non-married, surgical residents were more likely to take supplements (odds ratio (OR) = 1.06, 1.05, and 1.05). Males, without children, and those who felt pressure to perform well, were afraid of being left behind, felt pressure because colleagues take them, or felt they could not reach their current level of training without medications were more likely to take medications (OR = 1.11, 1.04, 1.05, and 1.08). Adverse effects with medications were common. CONCLUSION: Supplement and medication use for cognitive enhancement was high among resident physicians at a single institution despite few having a related medical diagnosis. This study raises awareness of the growing pressure in competitive residency environments to use cognitive enhancement regardless of the potential side effects.

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Glutamate is an excitatory neurotransmitter in the nervous system. Excessive glutamate transmission can lead to increased calcium ion expression, related to increased neurotoxicity. Memantine is used for treating patients with Alzheimer's disease (AD) due to its protective action on the neurons against toxicity caused by over activation of N-methyl-D-aspartate receptors. Nootropics, also called "smart drugs", are used for the treatment of cognitive deficits. In this work, we evaluate the neuroprotective action of four memantine analogues of glycine derivatives, including glycyl-glycine, glycyl-glycyl-glycine, sarcosine, dimethylglycine and three conjugates with nootropics, modafinil, piracetam and picamilon. The new structural memantine derivatives improved cell viability against copper-induced neurotoxicity in APPswe cells and glutamate-induced neurotoxicity in SH-SY5Y cells. Among these novel compounds, modafinil-memantine, piracetam-memantine, sarcosine-memantine, dimethylglycine-memantine, and glycyl-glycine-memantine were demonstrated with good EC50 values of the protective effects on APPswe cells, accompanied with moderate amelioration from glutamate-induced neurotoxicity. In conclusion, our study demonstrated that novel structural derivatives of memantine might have the potential to develop promising lead compounds for the treatment of AD. The solubility of memantine analogues with nootropics and memantine analogues with glycine derivatives in buffer solutions at pH 2.0 and pH 7.4 simulating the biological media at 298.15 K was determined and the mutual influence of the structural fragments in the molecules on the solubility behavior was analyzed. The significative correlation equations relating the solubility and biological properties with the structural HYBOT (Hydrogen Bond Thermodynamics) descriptors were derived. These equations would greatly simplify the task of the directed design of the memantine analogues with improved solubility and enhanced bioavailability.