• Besides the first-line sleepiness-battling formulations, such psychostimulants as dextroamphetamine sulfate ( Dexedrine , Dextrostat ), methamphetamines ( Deoxin ), methylphenidate ( Ritalin ), pemoline ( Zillert ), and mazindol ( sanorex ) are used. (rxshop.md)
  • Mazindol (brand names Mazanor, Sanorex) is a stimulant drug which is used as an appetite suppressant. (wikipedia.org)
  • Several stimulants that are also marketed for weight loss and appetite suppression, including fenproporex, mazindol, amfepramone and diethylpropion, are classified under Schedule IV. (therecoveryvillage.com)
  • Benztropine, mazindol, and vanoxerine also bind to these sites and have similar properties. (wee1signals.com)
  • Like other sympathomimetic appetite suppressants, mazindol is thought to act as a reuptake inhibitor of norepinephrine. (wikipedia.org)
  • Mazindol is a triple monoamine reuptake inhibitor and partial Orexin-2 Receptor agonist, which was used for many years to treat patients diagnosed with narcolepsy in compassionate use programs. (raleightimes.com)
  • Mazindol is a sympathomimetic amine, which is similar to amphetamine. (wikipedia.org)
  • The Company's lead product candidate, Quilience®, is a proprietary extended-release formulation of Mazindol (Mazindol ER) and is being developed for the treatment of narcolepsy, and potentially other sleep-wake disorders such as IH, for which NLS recently obtained ODD from the FDA and the European Medicines Agency (EMA). (raleightimes.com)
  • Mazindol mimics the effects of a brain chemical called orexin, which modulates wakefulness and appetite. (newscientist.com)
  • These symptoms were most probably due to its effect on appetite - mazindol has previously been used as a weight loss drug because it reduces feelings of hunger. (newscientist.com)
  • An alternative synthesis was described: 2-Phenyl-2-Imidazoline [936-49-2] (3) Methyl 4-Chlorobenzoate [1126-46-1] (4) As of 2016 mazindol was being studied in clinical trials for attention-deficit hyperactivity disorder. (wikipedia.org)
  • Mazindol CR is under clinical development by NLS Pharmaceutics and currently in Phase II for Opium (Opioid) Addiction. (pharmaceutical-technology.com)
  • In their clinical trial, Konofal and his colleagues gave either mazindol or a placebo to 85 adults aged between 18 and 65, all of whom had previously been diagnosed with ADHD. (newscientist.com)
  • Mazindol is under development for the treatment of attention deficit hyperactivity disorder and opioid use disorder. (pharmaceutical-technology.com)
  • Previously, Mazindol ER was granted ODD for IH in Europe on July 21, 2022. (raleightimes.com)
  • NLS also successfully completed a Phase 2 study in the U.S. evaluating Nolazol (Mazindol Controlled-Release) in adult subjects suffering from ADHD. (raleightimes.com)
  • Mazindol is the first new ADHD drug for decades to work in a novel way, says Efron. (newscientist.com)
  • However, although mazindol improved many ADHD symptoms, it did not boost the quality of the volunteers' sleep, nor reduce the daytime sleepiness they experienced. (newscientist.com)
  • Removal of the p-chlorine atom from the phenyl ring of mazindol increases NET affinity and substantially reduces DAT and SERT affinity. (wikipedia.org)
  • Mazindol is used in short-term (i.e., a few weeks) treatment of obesity, in combination with a regimen of weight reduction based on caloric restriction, exercise, and behavior modification in people with a body mass index greater than 30, or in those with a body mass index greater than 27 in the presence of risk factors such as hypertension, diabetes, or hyperlipidemia. (wikipedia.org)
  • Mazindol is not currently available as a commercially marketed and FDA-regulated prescription agent for the treatment of obesity. (wikipedia.org)
  • The NPP will provide access to Mazindol ER for the treatment of IH where this medication would not otherwise be available for this indication in certain countries. (raleightimes.com)
  • On November 2, 2022, the U.S. Food and Drug Administration (FDA) granted Orphan Drug Designation (ODD) for Mazindol ER for the treatment of IH. (raleightimes.com)
  • Future trials should directly compare the effects of these drugs with mazindol, to see if it really is superior, says Efron. (newscientist.com)
  • Mazindol exists in the tricycic (-ol) form in neutral media and undergoes protonation to the benzophenone tautomer in acidic media. (wikipedia.org)
  • Mazindol attenuates the 3,4-methylenedioxymethamphetamine-induced form. (erowid.org)
  • Diethylpropion, a congener of amphetamine, mazindol, which is chemically unrelated to amphetamine, and ciclazindol, an experimental drug structurally similar to mazindol, were given in graded doses to determine their effect on food and oxygen consumption (VO2). (nih.gov)
  • Anorectic effects exhibited by diethylpropion and mazindol were similar and more potent than ciclazindol. (nih.gov)
  • Mazindol, but not diethylpropion or ciclazindol, produced a dose response increase in resting VO2. (nih.gov)
  • Mazindol and diethylpropion, but not ciclazindol, caused a dose-related increase in anesthetized VO2. (nih.gov)
  • The anesthetized VO2 response to amphetamine at 1 mg/kg was greater than the responses of mazindol and diethylpropion at 3.0 mg/kg. (nih.gov)
  • These findings confirm the previously recognized anorectic effects of mazindol and diethylpropion and also demonstrate that mazindol and diethylpropion but not ciclazindol (at the doses used) produced dose-related increases in VO2 (energy expenditure) by stimulating directly peripheral mechanisms and in the case of mazindol central mechanisms as well. (nih.gov)
  • Some examples of prescription appetite suppressants include: benzphetamine, diethylpropion, mazindol and phentermine. (nopainweightloss.com)
  • Weight-loss drugs called Mazindol Lose Mazindol, the generic name (MA zin doll) MZ1 is a brand. (acutepharmacy.com)
  • Mazindol is a sympathomimetic amine, which is similar to amphetamine. (wikipedia.org)
  • As a sympathomimetic amine, mazindol is similar to amphetamine in many ways. (acutepharmacy.com)
  • Furthermore, Mazindol holds patents for various applications, including the treatment of schizophrenia, reducing cravings associated with cocaine use, and managing neurobehavioral disorders. (researchem.net)
  • Mazindol is not currently available as a commercially marketed and FDA-regulated prescription agent for the treatment of obesity. (wikipedia.org)
  • Currently, Mazindol is not available as a commercially marketed prescription drug regulated by the FDA for obesity treatment. (researchem.net)
  • There is thus obtained the anorectic agent mazindol (6). (wikipedia.org)
  • Removing the tertiary alcohol group in mazindol, a process known as desoxylation, enhances its binding to DAT (Dopamine Transporter) and SERT (Serotonin Transporter) receptors without significantly affecting NET (Norepinephrine Transporter) affinity. (researchem.net)
  • Triadimefon and triadimenol had similar affinity for [3H]mazindol binding sites on the dopamine transporter (IC50s approximately 1-1.5 microM, only two- to threefold greater than GBR12909). (nih.gov)
  • The drug was only slightly less potent than cocaine for displacing mazindol at the dopamine transporter (DAT). (thedrugclassroom.com)
  • From available QSAR data, the following trends are apparent: Desoxylation of the tertiary alcohol in mazindol improves DAT and SERT binding without substantially reducing NET affinity. (wikipedia.org)
  • Other inhibitors of transport, such as cocaine, mazindol, citalopram, and nisoxetine, failed to stimulate efflux from these cells at concentrations that inhibited influx. (erowid.org)
  • Halogenation of 3' and/or 4' position of the phenyl ring of mazindol results in increased potency at NET, DAT, and SERT. (wikipedia.org)
  • Introducing halogen atoms (e.g., chlorine or fluorine) at the 3′ and 4′ positions of the phenyl ring in mazindol enhances its potency in binding to NET, DAT, and SERT receptors. (researchem.net)
  • Results showed pEC50 (a logarithm measure of drug potency expressing a concentration that is effective in producing 50% of the maximal response) values of 4.7 to 5 for mazindol on the OX2R, indicating a strong OX2R partial agonist. (germanysun.com)
  • Like other sympathomimetic appetite suppressants, mazindol is thought to act as a reuptake inhibitor of norepinephrine. (wikipedia.org)
  • QSAR studies have indicated that the ability of mazindol to inhibit NE and DA reuptake may be mediated by the protonated (benzophenone) tautomer. (wikipedia.org)
  • Removal of the p-chlorine atom from the phenyl ring of mazindol increases NET affinity and substantially reduces DAT and SERT affinity. (wikipedia.org)
  • An alternative synthesis was described: 2-Phenyl-2-Imidazoline [936-49-2] (3) Methyl 4-Chlorobenzoate [1126-46-1] (4) As of 2016 mazindol was being studied in clinical trials for attention-deficit hyperactivity disorder. (wikipedia.org)
  • Eliminating the p-chlorine atom attached to the phenyl ring in mazindol results in increased NET affinity but significantly reduces affinity for DAT and SERT. (researchem.net)
  • The benefits of modafinil, sodium oxybate, mazindol, and pitolisant were found in mostly retrospective studies. (nih.gov)
  • Expansion of the imidazoline ring system in mazindol to the corresponding six-membered homolog increases DAT affinity by ~10 fold. (wikipedia.org)
  • Enlarging the imidazoline ring system in mazindol to its corresponding six-membered counterpart substantially boosts DAT affinity by approximately tenfold. (researchem.net)
  • ZURICH, SWITZERLAND / ACCESSWIRE / January 23, 2023 / NLS Pharmaceutics Ltd. (NASDAQ:NLSP)(NASDAQ:NLSPW) ('NLS' or the 'Company'), a Swiss clinical-stage biopharmaceutical company focused on the discovery and development of innovative therapies for patients with rare and complex central nervous system disorders, today announced new in vitro study results demonstrating the agonist effect of mazindol ER at the Orexin-2 Receptor (OX2R). (germanysun.com)
  • The Company's lead product candidate, Quilience ® , is a proprietary extended-release formulation of mazindol (mazindol ER) and is being developed for the treatment of narcolepsy, and potentially other sleep-wake disorders such as Idiopathic Hypersomnia (IH), for which NLS recently obtained Orphan Disease Designation (ODD) from the U. S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA). (germanysun.com)
  • The Phase 3 program for Quilience (mazindol ER) is currently on track to commence in mid- 2023. (germanysun.com)
  • The unique dual mechanism of action of mazindol ER seems to represent an advantage over previously studied compounds, as mazindol ER appears to be highly effective in reducing narcolepsy symptoms without the potential side effects of a full OX2R agonist. (germanysun.com)
  • alpha-Methylparatyrosine produced a robust increase in depressive symptoms on the Hamilton Depression Rating Scale, including depressed mood, decreased concentration, anhedonia, loss of interest, and feelings of worthlessness, helplessness, and hopelessness, in the desipramine-mazindol but not in the fluoxetine-sertraline group. (biopsychiatry.com)
  • Mazindol is used in short-term (i.e., a few weeks) treatment of obesity, in combination with a regimen of weight reduction based on caloric restriction, exercise, and behavior modification in people with a body mass index greater than 30, or in those with a body mass index greater than 27 in the presence of risk factors such as hypertension, diabetes, or hyperlipidemia. (wikipedia.org)
  • Mazindol is utilized in the short-term, typically lasting a few weeks, as part of a comprehensive obesity management strategy. (researchem.net)
  • In the short-term treatment of obesity, mazindol is used as an addition to a healthy diet and exercise. (acutepharmacy.com)
  • Notably, findings show that mazindol ER showed strong OX2R partial agonist activity by cellular and nuclear receptor functional assays. (germanysun.com)
  • Mazindol Lose Generic Name: mazindol (MA zin doll) Brand Names: IFA LOSE What is mazindol? (acutepharmacy.com)
  • 10. Effect of mazindol on body weight and insulin sensitivity in severely obese patients after a very-low-calorie diet therapy. (nih.gov)
  • The recommended dosage for mazindol varies from 2 mg daily for 90 days in patients with a body weight exceeding 40 kg but less than 50 kg and 4 mg per day in patients with a body weight exceeding 50 kg. (researchem.net)
  • A significant increase in the dose is fraught with the intoxication of the body with mazindol. (acutepharmacy.com)
  • Two identical studies measuring differing concentrations of mazindol ER confirmed significant OX2R partial agonist activity at 30μM or higher. (germanysun.com)