Finding the Optimal Dosage for Nootropic Agent Noopept: an Analysis of Available Literature
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Nootropics: Boost Body and Brain? Report #2445
NOOTROPICS: BOOST BODY AND BRAIN? REPORT #2445 BACKGROUND: Nootropics were first discovered in 1960s, and were used to help people with motion sickness and then later were tested for memory enhancement. In 1971, the nootropic drug piracetam was studied to help improve memory. Romanian doctor Corneliu Giurgea was the one to coin the term for this drug: nootropics. His idea after testing piracetam was to use a Greek combination of “nous” meaning mind and “trepein” meaning to bend. Therefore the meaning is literally to bend the mind. Since then, studies on this drug have been done all around the world. One test in particular studied neuroprotective benefits with Alzheimer’s patients. More tests were done with analogues of piracetam and were equally upbeat. This is a small fraction of nootropic drugs studied over the past decade. Studies were done first on animals and rats and later after results from toxicity reports, on willing humans. (Source: https://www.purenootropics.net/general-nootropics/history-of-nootropics/) A COGNITIVE EDGE: Many decades of tests have convinced some people of how important the drugs can be for people who want an enhancement in life. These neuro-enhancing drugs are being used more and more in the modern world. Nootropics come in many forms and the main one is caffeine. Caffeine reduces physical fatigue by stimulating the body’s metabolism. The molecules can pass through the blood brain barrier to affect the neurotransmitters that play a role in inhibition. These molecule messengers can produce muscle relaxation, stress reduction, and onset of sleep. Caffeine is great for short–term focus and alertness, but piracetam is shown to work for long-term memory. -
Transcript of “Hacking Your Ph, LED Lighting, and Smart Drugs with Steve Fowkes Part 2”
Transcript of “Hacking Your pH, LED Lighting, and Smart Drugs with Steve Fowkes Part 2” Bulletproof Radio podcast #95 © The Bulletproof Executive 2013 Bulletproof Toolbox Podcast #95, Steve Fowkes Warning and Disclaimer The statements in this report have not been evaluated by the FDA (U.S. Food & Drug Administration). Information provided here and products sold on bulletproofexec.com and/or upgradedself.com and/or betterbabybook.com are not intended to diagnose, treat, cure, or prevent any disease. The information provided by these sites and/or by this report is not a substitute for a face-to-face consultation with your physician, and should not be construed as medical advice of any sort. It is a list of resources for further self-research and work with your physician. We certify that at least one statement on the above-mentioned web sites and/or in this report is wrong. By using any of this information, or reading it, you are accepting responsibility for your own health and health decisions and expressly release The Bulletproof Executive and its employees, partners, and vendors from from any and all liability whatsoever, including that arising from negligence. Do not run with scissors. Hot drinks may be hot and burn you. If you do not agree to the above conditions, please do not read further and delete this document. 2 Bulletproof Toolbox Podcast #95, Steve Fowkes Dave: Hey, everyone, Dave Asprey, Bulletproof Executive Radio. You’re listening to a special episode. If you caught the last one, in fact, if you’re haven’t caught the episode before this one, you need to go back and listen to it, because this is part two of my epic interview with Steve Fowkes who doesn’t like it when I call him a bio-hacking badass, even though that's what he is. -
The Use and Impact of Cognitive Enhancers Among University Students: a Systematic Review
brain sciences Systematic Review The Use and Impact of Cognitive Enhancers among University Students: A Systematic Review Safia Sharif 1 , Amira Guirguis 1,2,* , Suzanne Fergus 1,* and Fabrizio Schifano 1 1 Psychopharmacology, Substance Misuse and Novel Psychoactive Substances Research Unit, School of Life and Medical Sciences, University of Hertfordshire, Hatfield AL10 9AB, UK; [email protected] (S.S.); [email protected] (F.S.) 2 Institute of Life Sciences 2, Swansea University, Swansea SA2 8PP, Wales, UK * Correspondence: [email protected] (A.G.); [email protected] (S.F.) Abstract: Introduction: Cognitive enhancers (CEs), also known as “smart drugs”, “study aids” or “nootropics” are a cause of concern. Recent research studies investigated the use of CEs being taken as study aids by university students. This manuscript provides an overview of popular CEs, focusing on a range of drugs/substances (e.g., prescription CEs including amphetamine salt mixtures, methylphenidate, modafinil and piracetam; and non-prescription CEs including caffeine, cobalamin (vitamin B12), guarana, pyridoxine (vitamin B6) and vinpocetine) that have emerged as being misused. The diverted non-prescription use of these molecules and the related potential for dependence and/or addiction is being reported. It has been demonstrated that healthy students (i.e., those without any diagnosed mental disorders) are increasingly using drugs such as methylphenidate, a mixture of dextroamphetamine/amphetamine, and modafinil, for the purpose of increasing their alertness, concentration or memory. Aim: To investigate the level of knowledge, perception and impact of the use of a range of CEs within Higher Education Institutions. -
Cognitive Enhancers
Cognitive enhancers Memory enhancers are often referred to as "smart drugs", "study drugs",[1] "smart nutrients", "cognitive enhancers", "brain enhancers" or in the scientific literature as nootropics.[2] They are drugs that are purported to improve human cognitive abilities.[3][4] The term covers a broad range of substances including drugs, nutrients and herbs with purported cognitive enhancing effects. The word nootropic was coined in 1964 by Dr. Corneliu E. Giurgea, derived from the Greek words noos, or "mind," and tropein meaning "to bend/turn". Typically, nootropics are thought to work by altering the availability of the brain's supply of neurochemicals (neurotransmitters, enzymes, and hormones), by improving the brain's oxygen supply, or by stimulating nerve growth. However the efficacy of nootropic substances in most cases has not been conclusively determined. This is complicated by the difficulty of defining and quantifying cognition and intelligence. Contents 1 Availability 2 Examples 2.1 Stimulants 2.2 Replenishing and increasing neurotransmitters 2.2.1 Cholinergics 2.2.1.1 Piracetam 2.2.1.2 Aniracetam 2.2.1.3 Other cholinergics 2.2.1.4 Acetylcholinesterase inhibitors 2.2.2 Dopaminergics 2.2.3 Serotonergics 2.3 Anti-depression, adaptogenic (antistress), and mood stabilization 2.4 Brain function and improved oxygen supply 2.5 Purported memory enhancement and learning improvement 2.6 Nerve growth stimulation and brain cell protection 2.7 Recreational drugs with purported nootropic effects 2.8 Dietary nootropics 2.9 Other nootropics 2.9.1 Contentious or possibly unsafe nootropics 3 See also 3.1 Brain and neurology 3.2 Thought and thinking (what nootropics are used for) 3.3 Health 4 References 5 External links Availability Currently there are several drugs on the market that improve memory, concentration, planning and reduce impulsive behavior. -
World of Cognitive Enhancers
ORIGINAL RESEARCH published: 11 September 2020 doi: 10.3389/fpsyt.2020.546796 The Psychonauts’ World of Cognitive Enhancers Flavia Napoletano 1,2, Fabrizio Schifano 2*, John Martin Corkery 2, Amira Guirguis 2,3, Davide Arillotta 2,4, Caroline Zangani 2,5 and Alessandro Vento 6,7,8 1 Department of Mental Health, Homerton University Hospital, East London Foundation Trust, London, United Kingdom, 2 Psychopharmacology, Drug Misuse, and Novel Psychoactive Substances Research Unit, School of Life and Medical Sciences, University of Hertfordshire, Hatfield, United Kingdom, 3 Swansea University Medical School, Institute of Life Sciences 2, Swansea University, Swansea, United Kingdom, 4 Psychiatry Unit, Department of Clinical and Experimental Medicine, University of Catania, Catania, Italy, 5 Department of Health Sciences, University of Milan, Milan, Italy, 6 Department of Mental Health, Addictions’ Observatory (ODDPSS), Rome, Italy, 7 Department of Mental Health, Guglielmo Marconi” University, Rome, Italy, 8 Department of Mental Health, ASL Roma 2, Rome, Italy Background: There is growing availability of novel psychoactive substances (NPS), including cognitive enhancers (CEs) which can be used in the treatment of certain mental health disorders. While treating cognitive deficit symptoms in neuropsychiatric or neurodegenerative disorders using CEs might have significant benefits for patients, the increasing recreational use of these substances by healthy individuals raises many clinical, medico-legal, and ethical issues. Moreover, it has become very challenging for clinicians to Edited by: keep up-to-date with CEs currently available as comprehensive official lists do not exist. Simona Pichini, Methods: Using a web crawler (NPSfinder®), the present study aimed at assessing National Institute of Health (ISS), Italy Reviewed by: psychonaut fora/platforms to better understand the online situation regarding CEs. -
Discovery of E1r: a Novel Positive Allosteric Modulator of Sigma-1 Receptor
Edijs Vāvers DISCOVERY OF E1R: A NOVEL POSITIVE ALLOSTERIC MODULATOR OF SIGMA-1 RECEPTOR Doctoral Thesis for obtaining the degree of Doctor of Pharmacy Speciality − Pharmaceutical Pharmacology Scientific supervisor: Dr. pharm., Professor Maija Dambrova Riga, 2017 ANNOTATION Sigma-1 receptor (Sig1R) is a new drug target. Notably, the International Union of Basic and Clinical Pharmacology included Sig1R in its list of receptors only in 2013. It is believed that Sig1R ligands are potential novel drug candidates for the treatment of central and peripheral nervous system diseases. The aim of this thesis was to evaluate the pharmacological activity of novel Sig1R ligands and to search for their possible clinical applications. Methylphenylpiracetam (2-(5-methyl-2-oxo-4-phenyl-pyrrolidin-1-yl)-acetamide) was synthesised in the Latvian Institute of Organic Synthesis. There are two chiral centres in the molecular structure of methylphenylpiracetam; therefore, it is possible to isolate four individual stereoisomers, which are denoted E1R, T1R, E1S and T1S. The activity of E1R was profiled using commercially available screening assays, which showed that the compound selectively modulates Sig1R activity but does not affect the other investigated neuronal receptors and ion channels. The following detailed in vitro studies, in which more selective Sig1R ligands were used, provided solid evidence that E1R is a positive allosteric modulator of Sig1R. It was found that the enantiomers with the R-configuration at the C-4 chiral centre in the 2-pyrrolidone ring (E1R and T1R) are more effective positive allosteric modulators of Sig1R than their optical antipodes. Since Sig1R agonists demonstrate neuroprotective properties and are effective in the treatment of cognitive disorders of various origins, the activity of E1R was tested in experimental models in vivo. -
Effects of Nebracetam (WEB 1881 FU), a Novel Nootropic, As a Mi-Muscarinic Agonist
Short Communications Japan. J. Pharmacol. 55, 177 (1991) Effects of Nebracetam (WEB 1881 FU), a Novel Nootropic, as a Mi-Muscarinic Agonist Yoshihisa Kitamura, Toshio Kaneda and Yasuyuki Nomura * Department of Pharmacology, Faculty of Pharmaceutical Sciences, Hokkaido University, Sapporo 060, Japan Received August 28, 1990 Accepted November 21, 1990 ABSTRACT-We here investigated the effects of nebracetam (WEB 1881 FU, 4- aminomethyl-1-benzylpyrrolidin-2-one-hemifumarate), a novel pyrrolidinone nootro- pic, on the rise of intracellular Ca2+ concentration ([Ca 2+]i) in Jurkat cells, a human leukemic T cell line. Nebracetam induced a rise of [Ca2+]i in the medium with 1 mM Ca2+ and without Ca 2+ (plus 1 mM EGTA). The nebracetam-induced [Ca2+]i rise was blocked by atropine > pirenzepine > AF-DX 116. From these results, neb- racetam seems to act as an agonist for human M1-muscarinic receptors. Nebracetam (WEB 1881 FU, 4-aminomethyl- zepine and AF-DX 116 were generous gifts 1-benzylpyrrolidin-2-one-hemifumarate) has from Nippon Boehringer Ingelheim. Anirace- been developed as a novel nootropic drug (1). tam (Ro 13-5057) and calcium hopantenate Two pharmacological studies have showed that also were generous gifts from Roche and nebracetam ameliorates the impairment of Tanabe, respectively. Muscarine, nicotine and working memory induced by scopolamine and oxotremorine-M (Research Biochemicals by cerebral ischemia in rats (2) and facilitates Inc.); atropine, carbachol, phytohemagglutinin the muscarinic transmission via action on mus- (PHA) (Sigma) were used. carinic receptors in dogs (3). Recently, we re- Jurkat cells were maintained in Iscove's ported that nebracetam has binding activity modified Dulbecco's medium (IMDM) sup- for acetylcholine receptors in rat brain: the plemented with 10% (vol./vol.) heat-inacti- order of the potency of binding affinity was vated (56°C for 30 min) fetal calf serum M1-muscarinic > M2-muscarinic > nicotinic (FCS). -
Identification of the Antiepileptic Racetam Binding Site in the Synaptic Vesicle Protein 2A by Molecular Dynamics and Docking Si
ORIGINAL RESEARCH published: 10 April 2015 doi: 10.3389/fncel.2015.00125 Identification of the antiepileptic racetam binding site in the synaptic vesicle protein 2A by molecular dynamics and docking simulations José Correa-Basurto1, Roberto I. Cuevas-Hernández1, Bryan V. Phillips-Farfán2, Marlet Martínez-Archundia1, Antonio Romo-Mancillas3, Gema L. Ramírez-Salinas1, Óscar A. Pérez-González2, José Trujillo-Ferrara1 and Julieta G. Mendoza-Torreblanca2* 1 Laboratorio de Modelado Molecular y Diseño de fármacos, Departamento de Bioquímica de la Escuela Superior de Medicina del Instituto Politécnico Nacional, México City, Mexico, 2 Laboratorio de Nutrición Experimental, Laboratorio de Oncología Experimental and Laboratorio de Neuroquímica, Instituto Nacional de Pediatría, México City, Mexico, 3 División de Estudios de Posgrado, Facultad de Química, Universidad Autónoma de Querétaro, Santiago de Querétaro, Mexico Edited by: Victoria Campos-Peña, Synaptic vesicle protein 2A (SV2A) is an integral membrane protein necessary for the Instituto Nacional de Neurologia y Neurocirugia, Mexico proper function of the central nervous system and is associated to the physiopathology Reviewed by: of epilepsy. SV2A is the molecular target of the anti-epileptic drug levetiracetam and its Benjamín Florán, racetam analogs. The racetam binding site in SV2A and the non-covalent interactions Centro de Investigación y de Estudios Avanzados del Instituto Politécnico between racetams and SV2A are currently unknown; therefore, an in silico study was Nacional, Mexico performed to explore these issues. Since SV2A has not been structurally characterized Alan Talevi, with X-ray crystallography or nuclear magnetic resonance, a three-dimensional (3D) National University of La Plata, Argentina model was built. The model was refined by performing a molecular dynamics simulation *Correspondence: (MDS) and the interactions of SV2A with the racetams were determined by docking Julieta G. -
Pharmaceutical Composition with Synergistic Anticonvulsant Effect
(19) TZZ __T (11) EP 2 695 618 A1 (12) EUROPEAN PATENT APPLICATION (43) Date of publication: (51) Int Cl.: 12.02.2014 Bulletin 2014/07 A61K 38/04 (2006.01) A61P 21/00 (2006.01) A61P 19/00 (2006.01) A61P 25/14 (2006.01) (2006.01) (21) Application number: 13004798.8 A61K 31/40 (22) Date of filing: 15.06.2007 (84) Designated Contracting States: (71) Applicant: UCB Pharma GmbH AT BE BG CH CY CZ DE DK EE ES FI FR GB GR 40789 Monheim (DE) HU IE IS IT LI LT LU LV MC MT NL PL PT RO SE SI SK TR (72) Inventor: Stöhr, Thomas 2400 Mol (BE) (30) Priority: 15.06.2006 US 813967 P 12.10.2006 EP 06021470 (74) Representative: Dressen, Frank 12.10.2006 EP 06021469 UCB Pharma GmbH 22.11.2006 EP 06024241 Alfred-Nobel-Strasse 10 40789 Monheim (DE) (62) Document number(s) of the earlier application(s) in accordance with Art. 76 EPC: Remarks: 07764676.8 / 2 037 965 This application was filed on 04-10-2013 as a divisional application to the application mentioned under INID code 62. (54) PHARMACEUTICAL COMPOSITION WITH SYNERGISTIC ANTICONVULSANT EFFECT (57) The present invention is directed to a pharmaceutical composition comprising (a) lacosamide and (b) levetira- cetam for the prevention, alleviation or/and treatment of epileptic seizures. EP 2 695 618 A1 Printed by Jouve, 75001 PARIS (FR) EP 2 695 618 A1 Description [0001] The present application items the priorities of US 60/813.967 of 15 June 2006, EP 06 021 470.7 of 12 October 2006, EP 06 021 469.9 of 12 October 2006, and EP 06 024 241.9 of 22 November 2006, which are included herein by 5 reference. -
Treatment of Alzheimer's Disease
Inkblot: The Undergraduate Journal of Psychology • Vol. 2 • September 2013 | 43 Treatment of Alzheimer’s Disease: A Comparison of Racetam Compounds and Current Medication Jaeger Lam and Bryanna Graves Abstract The purpose of this paper is to examine whether oxiracetam and aniracetam are more effective than donepezil and tacrine, two drugs currently used to treat Alzheimer’s disease. Past research suggests that oxiracetam and aniracetam are more therapeutically efficacious than donepezil and tacrine in the treatment of Alzheimer’s dis- ease symptoms (i.e., cognitive deterioration, tolerability, and quality of life). Oxiracetam and aniracetam appear to reverse the cognitive deficits of Alzheimer’s disease, whereas donepezil and tacrine seem to only slow down the deterioration of cognitive abilities. Research also suggests that oxiracetam and aniracetam may cause improve- ments in quality of life, whereas donepezil and tacrine provide mild, if any, improvement in quality of life. Future research on Alzheimer’s treatment should be conducted on large populations and focus on direct comparisons of the efficacy between Racetam and non-Racetam compounds. This literature review will discuss the effects of anirace- n.d.). The use of aniracetam and oxiracetam in treating tam and oxiracetam on patients afflicted with Alzheim- Alzheimer’s disease was researched heavily in the 1990s er’s disease. Alzheimer’s disease is an irreversible and (Bottini, Vallar, Cappa, Monza, Scarpini, Baron, & Scar- progressive disease. Symptoms of the disease include lato, 1992; Dager, Loebel, Claypool, Case, Budech, & deterioration in memory, dysfunctional daily living, Dunner, 1992; Davis, Thal, Gamzu, Davis, Woolson, changes in mood and personality, confusion, impaired Gracon, & Doody, 1992; Gouliaev, & Senning, 1994). -
Seletracetam (UCB 44212)
Neurotherapeutics: The Journal of the American Society for Experimental NeuroTherapeutics Seletracetam (UCB 44212) Barbara Bennett,* Alain Matagne,† Philippe Michel,‡ Michèle Leonard,§ Miranda Cornet,§ Marie-Anne Meeus,¶ and Nathalie Toublanc¶ *CNS Clinical Development, UCB Atlanta, Smyrna, Georgia 30080; †Preclinical CNS, ‡Chemistry, §Non-clinical Development, and ¶Clinical Pharmacology, UCB Braine-l’Alleud, Belgium Summary: Better pharmacotherapies for epilepsy are needed demonstrates low plasma protein binding (Ͻ10%), which sug- for patients who are refractory to or have tolerability difficulties gests a low potential for drug–drug interactions. Initial studies with current treatments. Seletracetam, a new drug in epilepsy in humans demonstrated first-order monocompartmental kinet- development, is a pyrrolidone derivative structurally related to ics with a half-life of 8 h and an oral bioavailability of Ͼ90%. levetiracetam (trade name Keppra). It was discovered because Studies in healthy volunteers showed that the treatment emer- of its high binding affinity to the synaptic vesicle 2A (SV2A) gent adverse events were of mild to moderate severity, were protein, which is now known to be the binding site for this mostly of CNS origin and were resolved within 24 h. Alto- family of compounds. Seletracetam shows very potent seizure gether, these results suggest that seletracetam represents a suppression in models of acquired or genetic epilepsy, as well promising new antiepileptic drug candidate, one that demon- as high CNS tolerability in various animal models. Pharmaco- strates a potent, broad spectrum of seizure protection and a high kinetic studies in animals suggest that seletracetam is rapidly CNS tolerability in animal models, with initial clinical findings and highly absorbed, with linear and time-independent phar- suggestive of straightforward pharmacokinetics and good tol- macokinetics. -
Psychoactive Medications Grouped by Drug Class and Foods Studied Tor Psychoactive Effects
Psychoactive Medications Grouped by Drug Class and Foods Studied tor Psychoactive Effects Drug and class Trade name(s) CNS stimulants amphetamine Benzedrine® deanol Deaner® dextroamphetamine (D-amphetamine) Dexedrine® dextroamphetamine/amphetamine" Adderall® levoamphetamine (L-amphetamine) Cydril® methamphetamine Desoxyn® methylphenidate Ritalin® pemoline Cylert® Neuroleptics (antipsychotics, "major tranquilizers") Phenothiazines chlorpromazine Largactil®, Thorazine® ftuphenazine (decanoate) Prolixin®, Modecate® mesoridazine Serentil® peracetazine Quide® pericyazine Neulactil® perphenazine Trilafon® pipothiazine palrnitate Piportil® prochlorperazine Compazine®, Stemetil® promazine Sparine® thioridazine Mellaril® triftuoperazine Stelazine® Thioxanthenes chlorprothixene Taractan®, Tarasan® ftupenthixol (decanoate) Depixol® thiothixene Navane® Benzisothiazolyl piperazines ziprasidone Zeldox® Practitioner's Guide to Psychoactive Drugs for Children and Adolescents (Second Edition), Werry and Aman, eds. Plenum Publishing Corporation, New York, 1999. 471 472 Psychoactive Medications Grouped by Drug Class Drug and class Trade name(s) Neuroleptics (antipsychotics, "major tranquilizers") (cont.) Benzisoxazoles risperidone Risperdal® Butyrophenones droperidol Droleptan® haloperidol Haldol®, Serenace® pipamperon Dipiperon® Dibenzothiazepines quetiapine Seroquel® Dibenzoxazepines loxapine Loxitane® Dihydroindolones molindone Moban® Diphenylbutylpiperidines pimozide Orap® Dibenzodiazepines clozapine Clozaril®, Leponex® Thienobenzodiazepines olanzapine