mazindol

Summary

Summary: Tricyclic anorexigenic agent unrelated to and less toxic than AMPHETAMINE, but with some similar side effects. It inhibits uptake of catecholamines and blocks the binding of cocaine to the dopamine uptake transporter.

Top Publications

  1. ncbi Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter
    William J Houlihan
    Charles A Dana Research Institute, Drew University, Hall of Sciences, Madison, NJ 07940, USA
    J Med Chem 45:4110-8. 2002
  2. ncbi Mazindol attenuates ketamine-induced cognitive deficit in the attentional set shifting task in rats
    Agnieszka Nikiforuk
    Behavioral Neuroscience and Drug Development, Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Street, 31 343 Krakow, Poland
    Eur Neuropsychopharmacol 20:37-48. 2010
  3. ncbi Serial echocardiographic and clinical evaluation of valvular regurgitation before, during, and after treatment with fenfluramine or dexfenfluramine and mazindol or phentermine
    D H Ryan
    Pennington Biomedical Research Center, Baton Rouge, LA 70808 4124, USA
    Obes Res 7:313-22. 1999
  4. ncbi Tyr-95 and Ile-172 in transmembrane segments 1 and 3 of human serotonin transporters interact to establish high affinity recognition of antidepressants
    L Keith Henry
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University Medical Center, Nashville, TN 37232, USA
    J Biol Chem 281:2012-23. 2006
  5. ncbi Synergistic interaction between mazindol, an anorectic drug, and swim-stress on analgesic responses in the formalin test in mice
    Leandro Franco Vendruscolo
    Departamento de Farmacologia, Centro de Ciencias Biologicas, Universidade Federal de Santa Catarina, R Ferreira Lima, 82, Florianopolis, SC 88015 420, Brazil
    Neurosci Lett 355:13-6. 2004
  6. ncbi High affinity recognition of serotonin transporter antagonists defined by species-scanning mutagenesis. An aromatic residue in transmembrane domain I dictates species-selective recognition of citalopram and mazindol
    E L Barker
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 6600, USA
    J Biol Chem 273:19459-68. 1998
  7. ncbi Unilateral infusion of a dopamine transporter antisense into the substantia nigra protects against MDMA-induced serotonergic deficits in the ipsilateral striatum
    A Kanthasamy
    Department of Biomedical Sciences, School of Veterinary Medicine, Iowa State University, Ames 50011, USA
    Neuroscience 114:917-24. 2002
  8. ncbi Binding site of salsolinol: its properties in different regions of the brain and the pituitary gland of the rat
    Krisztián Gy Homicskó
    Neuroendocrine Research Laboratory, Department of Human Morphology and Developmental Biology, Semmelweis University, IX Tuzoltó u 58, Budapest H 1094, Hungary
    Neurochem Int 42:19-26. 2003
  9. ncbi 2,3-Disubstituted quinuclidines as a novel class of dopamine transporter inhibitors
    Sukumar Sakamuri
    Department of Neurology, Georgetown University Medical Center, 3900 Reservoir Rd, Washington, DC 20007, USA
    Bioorg Med Chem 11:1123-36. 2003
  10. ncbi Chronic intoxication with 3-nitropropionic acid in rats induces the loss of striatal dopamine terminals without affecting nigral cell viability
    David Blum
    Laboratory of Neurophysiology, Université Libre de Bruxelles Erasme, CP601, 808 Route de Lennik, 1070 Brussels, Belgium
    Neurosci Lett 354:234-8. 2004

Research Grants

  1. DOPAMINE TRANSPORTER LIGANDS AS COCAINE MEDICATIONS
    Alexandros Makriyannis; Fiscal Year: 2002
  2. Cocaine Withdrawal: A Window of Treatment Opportunity
    Tong Lee; Fiscal Year: 2009
  3. RADIOLIGANDS FOR CENTRAL NORADRENERGIC UPTAKE SITES
    Shanaz Tejani Butt; Fiscal Year: 1992
  4. STIMULUS PROPERTIES OF ANXIOLYTICS IN HUMANS
    Chris Ellyn Johanson; Fiscal Year: 1991
  5. COCAINE RECEPTORS AND ADDICTION
    MOHYEE ELDEFRAWI; Fiscal Year: 1993
  6. INHIBITION OF DOPAMINE RELEASE BY COCAINE AND OTHER DRUG
    DOROTHY DEMBIEC COHEN; Fiscal Year: 1990
  7. DOPAMINE TRANSPORTER IMAGING IN COCAINE ABUSE
    DEAN WONG; Fiscal Year: 1999
  8. Human Cocaine Discrimination
    CRAIG RUSH; Fiscal Year: 2006
  9. LOCALIZED NEUROTOXICITY OF METHAMPHETAMINE AND COCAINE
    DAVID BRUNSWICK; Fiscal Year: 1990
  10. DRUGS OF ABUSE--DOPAMINE RELEASE AND REUPTAKE
    JAMES SCHENK; Fiscal Year: 1999

Detail Information

Publications174 found, 100 shown here

  1. ncbi Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter
    William J Houlihan
    Charles A Dana Research Institute, Drew University, Hall of Sciences, Madison, NJ 07940, USA
    J Med Chem 45:4110-8. 2002
    A series of mazindol (1), homomazindol (2), and bishomomazindol (3) derivatives with a benzo or cyclohexano ring fused at various sites were prepared as part of an SAR study to determine the effect of increased aliphatic and aromatic ..
  2. ncbi Mazindol attenuates ketamine-induced cognitive deficit in the attentional set shifting task in rats
    Agnieszka Nikiforuk
    Behavioral Neuroscience and Drug Development, Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Street, 31 343 Krakow, Poland
    Eur Neuropsychopharmacol 20:37-48. 2010
    ..Next, we investigated whether the co-administration of mazindol, a dopamine and norepinephrine reuptake inhibitor would protect rats from ketamine-induced deficits...
  3. ncbi Serial echocardiographic and clinical evaluation of valvular regurgitation before, during, and after treatment with fenfluramine or dexfenfluramine and mazindol or phentermine
    D H Ryan
    Pennington Biomedical Research Center, Baton Rouge, LA 70808 4124, USA
    Obes Res 7:313-22. 1999
    ..We studied 86 patients who had echocardiograms before treatment with appetite suppressants to determine the incidence of new cases and to evaluate the clinical implication of the echocardiographic findings...
  4. ncbi Tyr-95 and Ile-172 in transmembrane segments 1 and 3 of human serotonin transporters interact to establish high affinity recognition of antidepressants
    L Keith Henry
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University Medical Center, Nashville, TN 37232, USA
    J Biol Chem 281:2012-23. 2006
    ..potency for multiple inhibitors such as (RS)-CIT, clomipramine, RTI-55, fluoxetine, cocaine, nisoxetine, mazindol, and nomifensine, whereas recognition of substrates, including serotonin and 3,4-methylenedioxymethamphetamine, ..
  5. ncbi Synergistic interaction between mazindol, an anorectic drug, and swim-stress on analgesic responses in the formalin test in mice
    Leandro Franco Vendruscolo
    Departamento de Farmacologia, Centro de Ciencias Biologicas, Universidade Federal de Santa Catarina, R Ferreira Lima, 82, Florianopolis, SC 88015 420, Brazil
    Neurosci Lett 355:13-6. 2004
    The present study examined the interaction between mazindol (MZ), an anorectic drug extensively used in Brazil and opioid/non-opioid endogenous analgesic systems activated by swim-stress...
  6. ncbi High affinity recognition of serotonin transporter antagonists defined by species-scanning mutagenesis. An aromatic residue in transmembrane domain I dictates species-selective recognition of citalopram and mazindol
    E L Barker
    Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 6600, USA
    J Biol Chem 273:19459-68. 1998
    ..By using human and Drosophila SERT chimeras, major determinants of potencies of two transporter antagonists, mazindol and citalopram, were tracked to the amino-terminal domains encompassing transmembrane domains I and II...
  7. ncbi Unilateral infusion of a dopamine transporter antisense into the substantia nigra protects against MDMA-induced serotonergic deficits in the ipsilateral striatum
    A Kanthasamy
    Department of Biomedical Sciences, School of Veterinary Medicine, Iowa State University, Ames 50011, USA
    Neuroscience 114:917-24. 2002
    ..in a 70% reduction in the density of the dopamine transporter in the ipsilateral striatum, as measured by [(3)H]mazindol binding. The effect of this transporter knockdown on MDMA-induced serotonergic neurotoxicity was then examined...
  8. ncbi Binding site of salsolinol: its properties in different regions of the brain and the pituitary gland of the rat
    Krisztián Gy Homicskó
    Neuroendocrine Research Laboratory, Department of Human Morphology and Developmental Biology, Semmelweis University, IX Tuzoltó u 58, Budapest H 1094, Hungary
    Neurochem Int 42:19-26. 2003
    ..Neither mazindol (a selective DA transporter inhibitor) nor clonidine (an alpha(2)-adrenoreceptor agonist) could alter SAL binding...
  9. ncbi 2,3-Disubstituted quinuclidines as a novel class of dopamine transporter inhibitors
    Sukumar Sakamuri
    Department of Neurology, Georgetown University Medical Center, 3900 Reservoir Rd, Washington, DC 20007, USA
    Bioorg Med Chem 11:1123-36. 2003
    ..3 and 8.9 microM in [3H]mazindol binding and in inhibition of dopamine reuptake, respectively...
  10. ncbi Chronic intoxication with 3-nitropropionic acid in rats induces the loss of striatal dopamine terminals without affecting nigral cell viability
    David Blum
    Laboratory of Neurophysiology, Université Libre de Bruxelles Erasme, CP601, 808 Route de Lennik, 1070 Brussels, Belgium
    Neurosci Lett 354:234-8. 2004
    ..In the present study, we found that a 5-day continuous chronic infusion of 3NP produces loss of [3H]mazindol binding and tyrosine hydroxylase (TH) immunoreactivity in the striatal area of degeneration...
  11. ncbi The inhibitory role of methylation on the binding characteristics of dopamine receptors and transporter
    Eun Sook Y Lee
    College of Pharmacy and Pharmaceutical Sciences, Florida A and M University, Tallahassee, FL 32307, USA
    Neurosci Res 48:335-44. 2004
    ..We propose that the SAM effect might be related to its ability to react with dopamine receptor proteins through methyl-ester formation and methanol production following the hydrolysis of the carboxyl-methylated receptor proteins...
  12. ncbi A model of L-DOPA-induced dyskinesia in 6-hydroxydopamine lesioned mice: relation to motor and cellular parameters of nigrostriatal function
    M Lundblad
    Department of Physiological Sciences, Neurobiology Division, Wallenberg Neuroscience Centre, Lund University, S 223 62 Lund, Sweden
    Neurobiol Dis 16:110-23. 2004
    ..The mouse model of L-DOPA-induced dyskinesia will provide a useful tool to study the molecular determinants of this movement disorder in transgenic mice strains...
  13. ncbi Dopamine neurons from transgenic mice with a knockout of the p53 gene resist MPTP neurotoxicity
    P A Trimmer
    Department of Neurology, University of Virginia School of Medicine, Charlottesville 22908, USA
    Neurodegeneration 5:233-9. 1996
    ..over two days produced a non-homogeneous loss of striatal dopamine transport sites and quantitatively reduced 3H-mazindol binding to similar degrees in p53-/- and wild type controls 2 and 3 weeks after starting MPTP...
  14. ncbi Expression of striatal preprotachykinin mRNA in symptomatic and asymptomatic 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-exposed monkeys is related to parkinsonian motor signs
    T V Wade
    Department of Pathology, Anatomy, and Cell Biology, Thomas Jefferson University, Philadelphia, Pennsylvania 19107, USA
    J Neurosci 21:4901-7. 2001
    Striatal preprotachykinin (PPT) gene expression and [(3)H]mazindol binding were examined in monkeys exposed to 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)...
  15. ncbi Three-dimensional quantitative structure-activity relationships of mazindol analogues at the dopamine transporter
    Santosh S Kulkarni
    Medicinal Chemistry Section, National Institute on Drug Abuse Intramural Research Program NIH, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    J Med Chem 45:4119-27. 2002
    A three-dimensional quantitative structure-activity relationship (3D-QSAR) study was performed on a series of mazindol analogues using the comparative molecular field analysis (CoMFA) method with their corresponding binding affinities for ..
  16. ncbi Differential sensitivity to NaCl for inhibitors and substrates that recognize mutually exclusive binding sites on the neuronal transporter of dopamine in rat striatal membranes
    A Tidjane Corera
    UMR C.N.R.S. 6036, IFRMP 23, , 22 Boulevard Gambetta, 76000, Rouen, France
    Neurosci Res 39:319-25. 2001
    Addition of NaCl (90--290 mM) to a 10 mM Na(+) medium did not significantly modify B(max) and K(d) values for [3H]mazindol binding to the dopamine neuronal transporter (DAT) studied on rat striatal membranes at 20 degrees C...
  17. ncbi 6-Hydroxydopamine-lesioning of the nigrostriatal pathway in rats alters basal ganglia mRNA for copper, zinc- and manganese-superoxide dismutase, but not glutathione peroxidase
    G Kunikowska
    Neurodegenerative Diseases Research Centre, Division of Pharmacology and Therapeutics, Guy's, King's and St Thomas' School of Biomedical Sciences, Hodgkin Building, King's College, London SE1 1UL, UK
    Brain Res 922:51-64. 2001
    ..the nigrostriatal pathway resulted in contralateral rotation to apomorphine and a marked loss of specific [(3)H]mazindol binding in the striatum (93%; P<0...
  18. ncbi Gamma-aminobutyric acidA and benzodiazepine receptor alterations in the rat brain after unilateral 6-hydroxydopamine lesions of the medial forebrain bundle
    T Araki
    Department of Clinical Pharmacology and Therapeutics, Tohoku University Graduate School of Pharmaceutical Science and Medicine, Aoba yama, Sendai, Japan
    Neurol Res 24:107-12. 2002
    ..rat brains were studied by receptor autoradiography using [3H]muscimol, [3H]flunitrazepam and [3H]mazindol binding, respectively...
  19. ncbi Periwound dopaminergic sprouting is dependent on numbers of wound macrophages
    P E Batchelor
    Departments of Medicine and Neurology, University of Melbourne, Austin and Repatriation Medical Centre, Heidelberg Victoria 3084, Australia
    Eur J Neurosci 15:826-32. 2002
    ..Quantification of this effect using [H3]-mazindol autoradiography confirmed that periwound sprouting was reduced significantly in the op/op mice compared with ..
  20. ncbi Discovery of substituted 3,4-diphenyl-thiazoles as a novel class of monoamine transporter inhibitors through 3-D pharmacophore search using a new pharmacophore model derived from mazindol
    Istvan J Enyedy
    Department of Internal Medicine, University of Michigan, Ann Arbor, MI 48109 0934, USA
    Bioorg Med Chem Lett 12:1775-8. 2002
    ..monoamine transporter inhibitors through a 3-D pharmacophore search using a new pharmacophore model derived from mazindol. The most potent compound (13) has K(i) values of 24 and 23 nM in binding to dopamine transporter and inhibition ..
  21. ncbi Chronic but not acute treatment with a metabotropic glutamate 5 receptor antagonist reverses the akinetic deficits in a rat model of parkinsonism
    Nathalie Breysse
    Laboratoire de Neurobiologie Cellulaire et Fonctionnelle, Centre National de la Recherche Scientifique, 13402 Marseille Cedex 20, France
    J Neurosci 22:5669-78. 2002
    ..p.). Altogether, these results suggest a specific role of mGluRs in the regulation of extrapyramidal motor functions and a potential therapeutic value for mGluR5 antagonists in the treatment of Parkinson's disease...
  22. ncbi Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter
    William J Houlihan
    Charles A Dana Research Institute, Drew University, Hall of Sciences, Madison, NJ 07940, USA
    J Med Chem 45:4097-109. 2002
    A series of mazindol (2) and homomazindol (3) analogues with a variety of electron-donating and electron-withdrawing groups in the pendant aryl group and the benzo ring C, as well as H, methoxy, and alkyl groups replacing the hydroxyl ..
  23. ncbi Methamphetamine- and 1-methyl-4-phenyl- 1,2,3, 6-tetrahydropyridine-induced dopaminergic neurotoxicity in inducible nitric oxide synthase-deficient mice
    Y Itzhak
    Department of Psychiatry and Behavioral Sciences, University of Miami School of Medicine, Miami, Florida 33136, USA
    Synapse 34:305-12. 1999
    ..Moreover, in contrast to nNOS deficiency, iNOS deficiency did not affect METH-induced behavioral sensitization...
  24. ncbi Studies on the striatal dopamine uptake system of weaver mutant mice and effects of ventral mesencephalic grafts
    L C Triarhou
    Department of Pathology and Laboratory Medicine Laboratory of Cellular and Molecular Neuropathology, Indiana University School of Medicine, Indianapolis 46202
    Neurochem Res 19:1349-58. 1994
    ..Assays of [3H]DA uptake in striatal synaptosomal fractions in vitro and autoradiography of [3H]mazindol binding in brain sections were carried out in wild-type mice (+/+) and in the two hemispheres of homozygous ..
  25. ncbi Alterations in dopamine and serotonin uptake systems in the striatum of the weaver mutant mouse
    E H Stotz
    Department of Psychiatry Institute of Psychiatric Research, Indiana University School of Medicine, Indianapolis
    J Neural Transm Gen Sect 97:51-64. 1994
    ..The dopamine uptake system was also investigated in all three genotypes via the binding of [3H] mazindol. Synaptosomal uptake of [3H] serotonin was increased by 79% in the dorsal portion of the wv/wv striatum compared ..
  26. ncbi Neurochemical effects of chronic dietary and repeated high-level acute exposure to chlorpyrifos in rats
    Stephanie Padilla
    Neurotoxicology Division, US Environmental Protection Agency, Research Triangle Park, North Carolina 27711, USA
    Toxicol Sci 88:161-71. 2005
    ..These data indicate that, although chronic feeding with or without intermittent spiked dosages with CPF produces substantial biochemical changes in a dose- and tissue-related manner, there are no persistent biochemical changes...
  27. ncbi Recognition of benztropine by the dopamine transporter (DAT) differs from that of the classical dopamine uptake inhibitors cocaine, methylphenidate, and mazindol as a function of a DAT transmembrane 1 aspartic acid residue
    Okechukwu T Ukairo
    Division of Pharmaceutical Sciences, Duquesne University, Mellon Hall, Room 453, 600 Forbes Ave, Pittsburgh, PA 15282, USA
    J Pharmacol Exp Ther 314:575-83. 2005
    ....
  28. ncbi Genetic interdependence of adenosine and dopamine receptors: evidence from receptor knockout mice
    J L Short
    Department of Pharmacology, Faculty of Medicine, Monash University, Clayton, Victoria 3800, Australia
    Neuroscience 139:661-70. 2006
    ..These data are consistent with the existence of functional interactions between dopaminergic and purinergic systems in these reward and motor-related brain regions...
  29. ncbi L-DOPA-induced dyskinesia in adult rats with a unilateral 6-OHDA lesion of dopamine neurons is paralleled by increased c-fos gene expression in the subthalamic nucleus
    Jean Jacques Soghomonian
    Department of Anatomy and Neurobiology, Boston University School of Medicine, 715 Albany Street, Boston, MA 02118, USA
    Eur J Neurosci 23:2395-403. 2006
    ..These results suggest that altered cell signaling in the STN is involved in some of the behavioral effects induced by systemic L-DOPA administration...
  30. ncbi The dopamine agonist piribedil with L-DOPA improves attentional dysfunction: relevance for Parkinson's disease
    Nathalie Turle-Lorenzo
    Laboratoire de Neurobiologie de la Cognition, UMR 6155 Centre National de la Recherche Scientifique Université de Provence, Case C, 3 Place Victor Hugo, 13331 Marseille Cedex 3, France
    J Pharmacol Exp Ther 319:914-23. 2006
    ....
  31. ncbi Dopaminergic innervation of the human striatum in Parkinson's disease
    Michelle Porritt
    Department of Medicine, University of Melbourne, Parkville, Victoria, Australia
    Mov Disord 20:810-8. 2005
    ..This suggests that the impact of disease in these areas is more profound than was thought previously...
  32. ncbi Inhibiting BDNF expression by antisense oligonucleotide infusion causes loss of nigral dopaminergic neurons
    M J Porritt
    Department of Medicine, University of Melbourne, Level 7, Lance Townsend Building, Austin Health, Studley Road, Heidelberg, Vic 3084 Australia
    Exp Neurol 192:226-34. 2005
    ..00001) and dopamine uptake site density measured by (3)H-mazindol autoradiography is reduced by 34% (P < or = 0.005)...
  33. ncbi Differential effects of prolonged high frequency stimulation and of excitotoxic lesion of the subthalamic nucleus on dopamine denervation-induced cellular defects in the rat striatum and globus pallidus
    Jean Jacques Bacci
    Laboratoire Interactions Cellulaires Neurodégénérescence et Neuroplasticité, CNRS, 13402 Marseille Cedex 20, France
    Eur J Neurosci 20:3331-41. 2004
    ....
  34. ncbi Alterations in striatal neuropeptide mRNA produced by repeated administration of L-DOPA, ropinirole or bromocriptine correlate with dyskinesia induction in MPTP-treated common marmosets
    B C Tel
    Neurodegenerative Disease Research Centre, Guy s, King s and St Thomas School of Biomedical Sciences, King s College, SE1 1UL, London, UK
    Neuroscience 115:1047-58. 2002
    ..The equivalent marked losses of specific [3H]mazindol binding in the striatum of all drug treatment groups confirmed the identical nature of the nigral cell loss ..
  35. ncbi Enhanced dopamine uptake in the striatum following repeated restraint stress
    Benjamin J Copeland
    The Neuroscience Program, Division of Molecular Neuropsychopharmacology, The Ohio State University College of Medicine and Public Health, Columbus, Ohio 43210, USA
    Synapse 57:167-74. 2005
    ..DAT) was found to be concomitantly increased in the midbrain, as was the binding of the transporter ligand mazindol to DAT in the nucleus accumbens and caudate-putamen...
  36. ncbi Pharmacotherapy for obesity
    Lisa L Ioannides-Demos
    Department of Epidemiology and Preventive Medicine, Monash University, Melbourne, Australia
    Drugs 65:1391-418. 2005
    ..and has included thyroid hormone, amphetamines, phentermine, amfepramone (diethylpropion), phenylpropanolamine, mazindol, fenfluramines and, more recently, sibutramine and orlistat...
  37. ncbi Long-term pharmacotherapy for obesity in elderly patients: a retrospective evaluation of medical records from a specialized obesity outpatient clinic
    Nídia Celeste Horie
    Obesity Outpatient Clinic for the Elderly, Department of Geriatrics, Hospital das Clinicas, Faculdade de Medicina da Universidade de São Paulo USP, Sao Paulo, Brazil
    Drugs Aging 27:497-506. 2010
    ..The medicines prescribed were sibutramine, orlistat, fluoxetine, sertraline, topiramate, fenproporex, mazindol and amfepramone, alone or in combinations, concomitantly or sequentially...
  38. ncbi Use of sibutramine and other noradrenergic and serotonergic drugs in the management of obesity
    D H Ryan
    Pennington Biomedical Research Center, Baton Rouge, LA, USA
    Endocrine 13:193-9. 2000
    ..of older weight loss medications approved for short-term use (benzphetamine, phendimetrazine, diethylpropion, mazindol, and phentermine), as well as over-the-counter adrenergic drugs (phenylpropanolamine and ephedrine); recent ..
  39. ncbi Failure of neuroprotection by embryonic striatal grafts in a double lesion rat model of striatonigral degeneration (multiple system atrophy)
    Z Puschban
    Neurological Research Laboratory, Department of Neurology, University Hospital Innsbruck, Austria
    Exp Neurol 164:166-75. 2000
    ..Brains were then processed to dopamine reuptake ([(3)H]mazindol), dopamine D1 ([(3)H]SCH23390), and D2 ([(3)H]spiperone) receptor autoradiography...
  40. ncbi Pharmacokinetics of radiotracers in human plasma during positron emission tomography
    P Cumming
    McConnell Brain Imaging Centre, Montreal Neurological Institute, Montreal, Canada
    Synapse 34:124-34. 1999
    ..Pretreatment with mazindol, a dopamine uptake inhibitor, was without effect on peripheral metabolism of [(11)C]-(S)-nicotine...
  41. ncbi Relationships among dopamine transporter affinities and cocaine-like discriminative-stimulus effects
    J L Katz
    Psychobiology Section, NIDA Intramural Research Program, National Institutes of Health, P O Box 5180, Baltimore, MD 21224, USA
    Psychopharmacology (Berl) 148:90-8. 2000
    ..The binding to the dopamine transporter by cocaine and many of its analogs has been reported to fit better using a two-site model than a one-site model...
  42. ncbi Treatment of obesity: an update on anti-obesity medications
    A Halpern
    Obesity and Metabolic Diseases Group, Endocrinology and Metabology Service, Clinics Hospital, University of Sao Paulo Medical School, Sao Paulo, Brazil
    Obes Rev 4:25-42. 2003
    ..fenfluramine, dexfenfluramine, phentermine, diethylpropion, fenproporex and sibutramine), tricyclic derivatives (mazindol), phenylpropanolamine derivatives (ephedrine, phenylpropanolamine), a phenylpropanolamine oxy-tri-fluor-phenyl ..
  43. ncbi Efficacy of central nervous system stimulant treatment for cocaine dependence: a systematic review and meta-analysis of randomized controlled clinical trials
    Xavier Castells
    Psychiatry Service, Hospital Universitari Vall d Hebron, Universitat Autonoma de Barcelona, Barcelona, Catalonia, Spain
    Addiction 102:1871-87. 2007
    ..To evaluate the efficacy of central nervous system (CNS) stimulants compared with placebo for the treatment of cocaine dependence...
  44. ncbi In vivo dopamine clearance rate in rat striatum: regulation by extracellular dopamine concentration and dopamine transporter inhibitors
    N R Zahniser
    Department of Pharmacology, University of Colorado Health Sciences Center, Denver, USA
    J Pharmacol Exp Ther 289:266-77. 1999
    ..However, mazindol and cocaine have been reported to "anomalously" increase DA clearance rate...
  45. ncbi The role of dopamine transporter in selective toxicity of manganese and rotenone
    Yoko Hirata
    Department of Biomolecular Science, Faculty of Engineering, Gifu University, 1 1 Yanagido, Gifu 501 1193, Japan
    Toxicology 244:249-56. 2008
    ..Dopamine transporter inhibitors, such as mazindol, nomifensine, or GBR12909, inhibited MPP+-induced DNA fragmentation but did not affect manganese- and rotenone-..
  46. ncbi Effects of cocaine, nicotine, dizocipline and alcohol on mice locomotor activity: cocaine-alcohol cross-sensitization involves upregulation of striatal dopamine transporter binding sites
    Y Itzhak
    Department of Biochemistry and Molecular Biology R 629, University of Miami School of Medicine, P O Box 016129, Miami, FL 33101, USA
    Brain Res 818:204-11. 1999
    ..Assessment of the densities of striatal dopamine transporter (DAT) sites (by [3H]mazindol binding) 11 days after the extinction of repeated treatment with either cocaine or ethanol revealed a significant ..
  47. ncbi A concise review on the therapeutics of obesity
    G A Bray
    Pennington Biomedical Research Center, Louisiana State University, Baton Rouge, Louisiana, USA
    Nutrition 16:953-60. 2000
    ..A number of peptides also affect food intake. The noradrenergic drugs phentermine, diethylpropion, mazindol, benzphetamine, and phendimetrazine are approved only for short-term use...
  48. ncbi Dopamine release is impaired in a mouse model of DYT1 dystonia
    Aygul Balcioglu
    MassGeneral Institute for Neurodegenerative Disease, Department of Neurology, Massachusetts General Hospital, Boston, Massachusetts, USA
    J Neurochem 102:783-8. 2007
    ..Pre-synaptic DA transporters were studied using in vitro autoradiography with [(3)H]mazindol, a ligand for the membrane DA transporter, and [(3)H]dihydrotetrabenazine, a ligand for the vesicular monoamine ..
  49. ncbi Enhancement of spinal monosynaptic reflexes with phenylethylamine and related drugs through descending noradrenergic neurons
    Y Hasebe
    Department of Toxicology and Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokyo, Japan
    J Pharmacobiodyn 12:241-5. 1989
    ..phenylethylamine (PEA) and related drugs, such as methamphetamine, phenelzine, methylphenidate, nomifensine and mazindol on the spinal monosynaptic reflex (MSR) were investigated in rats treated with 6-hydroxydopamine (6-OHDA) or 5,6-..
  50. pmc Cloning, expression, and localization of a chloride-facilitated, cocaine-sensitive serotonin transporter from Drosophila melanogaster
    L L Demchyshyn
    Department of Psychiatry, University of Toronto, ON, Canada
    Proc Natl Acad Sci U S A 91:5158-62. 1994
    ..both dSERT and hSERT revealed that antidepressants were 3- to 300-fold less potent on dSERT than on hSERT, while mazindol displayed approximately 30-fold greater potency for dSERT...
  51. ncbi Diabesity: are weight loss medications effective?
    Alfredo Halpern
    Medical School, University of Sao Paulo, Sao Paulo, Brazil
    Treat Endocrinol 4:65-74. 2005
    ..patients have been reviewed as well as cathecolaminergic agents (diethylpropion [amfepramone], fenproporex, mazindol, ephedrine-caffeine combination), serotoninergic drugs (fenfluramine, dexfenfluramine, fluoxetine), and other ..
  52. ncbi The interaction of methylphenidate and benztropine with the dopamine transporter is different than other substrates and ligands
    Dalit E Dar
    National Institute on Drug Abuse, Intramural Research Program, National Institutes of Health, Baltimore, MD 21224, USA
    Biochem Pharmacol 70:461-9. 2005
    ..Different patterns of pharmacological activity emerged. GBR 12909, cocaine, and mazindol each showed reduced affinity for the Y251A and the Y273A mutants, but their affinity for the S356,359A mutant was ..
  53. ncbi Strain differences in the distribution of dopamine transporter sites in rat brain
    Xilu Jiao
    Department of Pharmacology and Toxicology, University of the Sciences in Philadelphia, Box 118, 600 South 43rd Street, Philadelphia, PA 19104, USA
    Prog Neuropsychopharmacol Biol Psychiatry 27:913-9. 2003
    ..DAT sites were labeled with [3H]-GBR12935 (1 nM), and mazindol (50 microM) was used to define nonspecific binding...
  54. ncbi Postnatal development of striatal dopamine function. II. Effects of neonatal 6-hydroxydopamine treatments on D1 and D2 receptors, adenylate cyclase activity and presynaptic dopamine function
    W C Broaddus
    Department of Neurological Surgery, University of Virginia School of Medicine, Charlottesville 22908
    Brain Res Dev Brain Res 52:273-7. 1990
    ..c. treatment and was reduced by 40-50% with both treatment regimens. [3H]mazindol binding, a marker for presynaptic terminal DA transport sites, was reduced 30-40% by multiple i.s. or i.c...
  55. ncbi Cloning, pharmacological characterization, and chromosome assignment of the human dopamine transporter
    B Giros
    Department of Cell Biology, Howard Hughes Medical Institute Laboratories, Duke University Medical Center, Durham, North Carolina 27710
    Mol Pharmacol 42:383-90. 1992
    ..norepinephrine, gamma-aminobutyric acid, and serotonin), antidepressants (amitriptyline, bupropion, desipramine, mazindol, nomifensine, and nortriptyline), and various uptake inhibitors (mazindol, GBR 12783, GBR 12909, and amfonelic ..
  56. ncbi Differential recovery of sensorimotor function in GM1 ganglioside-treated vs. spontaneously recovered MPTP-treated cats: partial striatal dopaminergic reinnervation vs. neurochemical compensation
    J S Schneider
    Department of Pathology, Anatomy and Cell Biology, Thomas Jefferson University, 1020 Locust Street, 521 JAH, Philadelphia, PA 19107, USA
    Brain Res 813:82-7. 1998
    ..GM1-treated cats also had significant increases in striatal [3H]mazindol binding compared to spontaneously recovered cats...
  57. ncbi The human dopamine transporter forms a tetramer in the plasma membrane: cross-linking of a cysteine in the fourth transmembrane segment is sensitive to cocaine analogs
    Hanne Hastrup
    Center for Molecular Recognition, Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, New York 10032, USA
    J Biol Chem 278:45045-8. 2003
    ..The cocaine analog MFZ 2-12 and other DAT inhibitors, including benztropine and mazindol, protected Cys243 against cross-linking...
  58. ncbi Substrates and inhibitors display different sensitivity to expression level of the dopamine transporter in heterologously expressing cells
    Nianhang Chen
    Department of Psychiatry, Millhauser Laboratories, New York University School of Medicine, New York, New York 10016, USA
    J Neurochem 101:377-88. 2007
    ..potency in inhibiting [(3)H]DA uptake for cocaine, CFT, benztropine, and its analog JHW025, GBR 12909 and mazindol; their potency in inhibiting [(3)H]CFT binding was unaffected...
  59. ncbi Regional pre- and postsynaptic sympathetic system in the failing human heart--regulation of beta ARK-1
    M Ungerer
    Medizinische Klinik der Technischen Universität München, Klinikum rechts der Isar, Ismaningerstr 22, 81675, Munich, Germany
    Eur J Heart Fail 2:23-31. 2000
    ..The goal of the present study was to correlate markers of presynaptic sympathetic innervation with local measurement of the postsynaptic beta-adrenergic system in failing human hearts...
  60. ncbi Autoradiographic quantification of neurochemical markers of serotonin, dopamine and opioid systems in rat brain mesolimbic regions following chronic St John's wort treatment
    Feng Chen
    Department of Pharmacology, Faculty of Medicine, Monash University, Wellington Road, PO Box 13E, 3800, Clayton, Victoria, Australia
    Naunyn Schmiedebergs Arch Pharmacol 367:126-33. 2003
    ..In contrast, SJW resulted in a region-specific alteration of [(3)H]mazindol binding to dopamine transporters, such as increased binding of [(3)H]mazindol in the olfactory tubercle and ..
  61. ncbi Characterization of the dopamine transporter gene expression and binding sites in cultured human amniotic epithelial cells
    Mohamed A Elwan
    Department of Inherited Metabolic Diseases, National Institute of Neuroscience, NCNP, Kodaira, Tokyo 187 8502, Japan
    Neurosci Lett 342:61-4. 2003
    ..Saturation binding studies using [3H]mazindol showed a high affinity DAT binding site with K(D) and B(max) values of 12.32+/-1.67 nM and 82.7+/-9...
  62. ncbi Lack of genotype effect on D1, D2 receptors and dopamine transporter binding in triple MOP-, DOP-, and KOP-opioid receptor knockout mice of three different genetic backgrounds
    Ji Hoon Yoo
    Faculty of Health and Medical Sciences, University of Surrey, Guildford, Surrey, GU2 7XH, United Kingdom
    Synapse 64:520-7. 2010
    ..radioligand binding to the D1 and D2 receptors and DAT labeled with [(3)H]SCH23390, [(3)H]raclopride, and [(3)H]mazindol, respectively in triple-opioid receptor knockout (KO) and WT maintained on C57BL/6 (B6) and 129/SvEvTac (129) as ..
  63. ncbi Differential region-specific regulation of α4β2* nAChRs by self-administered and non-contingent nicotine in C57BL/6J mice
    Athanasios Metaxas
    Faculty of Health and Medical Sciences, Division of Biochemical Sciences, University of Surrey, UK
    Addict Biol 15:464-79. 2010
    ..Cytisine-sensitive [(125)I]epibatidine binding, [³H]SCH23390, [³H]raclopride and [³H]mazindol were used to label nAChRs with α4β2* subtype properties, D1 and D2 dopaminergic receptors, and dopamine ..
  64. ncbi Pharmacological characterization and anatomical distribution of the dopamine transporter in the mouse cerebellum
    Foteini Delis
    Department of Neurobiology, University of Pittsburgh, Pittsburgh, Pennsylvania 15261, USA
    Cerebellum 7:242-51. 2008
    ..showed that [(3)H]GBR12935 binds to a specific binding site, sensitive to dopamine and low concentrations of mazindol. The affinity of dopamine for the cerebellar binding site was one order of magnitude lower than the affinity for ..
  65. ncbi The neurotoxic effects of 3,4-methylenedioxymethamphetamine (MDMA) and methamphetamine on serotonin, dopamine, and GABA-ergic terminals: an in-vitro autoradiographic study in rats
    Brian D Armstrong
    Department of Psychiatry and Biobehavioral Science, University of California at Los Angeles, NPI 760 Westwood Plaza Room 67 373, Los Angeles, CA 90024, USA
    Neurotoxicology 25:905-14. 2004
    ..implanted osmotic minipumps for a period of 5 days, and in-vitro autoradiography using [3H]-paroxetine, [3H]-mazindol, [3H]-methylspiperone, and [3H]-flunitrazepam, was performed on brain sections...
  66. ncbi Dopamine neurotransmission is involved in the attenuating effects of 5-HT3 receptor antagonist MDL 72222 on acute methamphetamine-induced locomotor hyperactivity in mice
    Ji Hoon Yoo
    Department of Pharmacology, College of Pharmacy, Sungkyunkwan University, Suwon 440 746, Republic of Korea
    Synapse 62:8-13. 2008
    ..receptor, and dopamine transporter (DAT) binding labeled with [3H]SCH23390 for D1, [3H]raclopride for D2, and [3H]mazindol for DAT binding in the mouse brains with acute MAP exposure or pretreatment of MDL 72222 with MAP...
  67. ncbi Does excessive daytime sleepiness contribute to explaining the association between obesity and ADHD symptoms?
    Samuele Cortese
    AP HP, Child and Adolescent Psychopathology Unit, Robert Debre Hospital, Paris VII University, Paris, France
    Med Hypotheses 70:12-6. 2008
    ..regard to the therapeutic implications, we suggest that wake-promoting agents with anorexigenic effect, such as mazindol, might be particularly indicated for the treatment of ADHD symptoms in obese patients, since they might address ..
  68. ncbi Decreased striatal D1 binding density following mesotelencephalic 6-hydroxydopamine injections: an autoradiographic analysis
    J F Marshall
    Department of Psychobiology, University of California, Irvine 92717
    Brain Res 493:247-57. 1989
    ..Those striatal regions that showed greater declines in D1 density correspondingly had the greater losses of [3H]mazindol binding after the denervation, suggesting that the decline of D1 binding is a postsynaptic consequence of the ..
  69. ncbi Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter
    W J Houlihan
    Charles A Dana Research Institute, Drew University, Madison, New Jersey 07940, USA
    J Med Chem 39:4935-41. 1996
    A series of halogenated (F, Cl, Br, I), pyrimido and diazepino homologs of mazindol were prepared and evaluated for their ability to displace [3H]WIN 35,428 binding and to inhibit uptake of [3H]dopamine (DA) in rat striatal tissue...
  70. ncbi Non-additivity of D2 receptor proliferation induced by dopamine denervation and chronic selective antagonist administration: evidence from quantitative autoradiography indicates a single mechanism of action
    G J LaHoste
    Department of Psychobiology, University of California, Irvine 92717
    Brain Res 502:223-32. 1989
    ..3H]Mazindol labelling of high-affinity DA uptake sites indicated that the extent of DA denervation was greater than 98% in ..
  71. ncbi Development of beta 1 and beta 2 adrenergic receptors in baboon brain: an autoradiographic study using [125I]iodocyanopindolol
    P A Slesinger
    Department of Neurology, Johns Hopkins University School of Medicine, Baltimore, Maryland 21205
    J Comp Neurol 273:318-29. 1988
    ..Autoradiograms of [125I]ICYP and [3H]mazindol binding show overlapping patches of labeling in the E180 striatum, suggesting a possible developmental ..
  72. ncbi Characterization of enhanced behavioral responses to L-DOPA following repeated administration in the 6-hydroxydopamine-lesioned rat model of Parkinson's disease
    B Henry
    Division of Neuroscience, School of Biological Sciences, University of Manchester, 1 124 Stopford Building, Manchester, M13 9PT, United Kingdom
    Exp Neurol 151:334-42. 1998
    ....
  73. ncbi GM1 enhances dopaminergic markers in the brain of aged rats
    V M Goettl
    Department of Pharmacology, College of Medicine and Public Health, Ohio State University, Columbus, OH 43210, USA
    Exp Neurol 183:665-72. 2003
    ..rats there is a diminished capacity to transport dopamine (DA), to bind the dopamine transporter (DAT) marker mazindol, to bind the vesicular monoamine transporter 2 (VMAT2) marker dihydrotetrabenazine, and to release DA under basal ..
  74. ncbi [Determination of fenfluramine, diethylpropion and mazindol in slimming foods by gas chromatography-mass spectrometry]
    Jiali Feng
    Hunan Provincial Center for Disease Control and Prevention, Changsha 410005, China
    Se Pu 22:228-30. 2004
    ..spectrometry (GC/MS) analytical method for three anorectics drugs, fenfluramine, diethylpropion and mazindol, illegally adulterated in slimming foods has been developed. They can be simultaneously identified and quantified...
  75. ncbi Transport of [3H]mazindol binding sites in mesostriatal dopamine axons
    S J O'Dell
    Department of Psychobiology, University of California, Irvine 92717
    Brain Res 460:402-6. 1988
    ..Such lesions produce accumulations of high-affinity dopamine uptake sites (as measured by [3H]mazindol binding) and acetylcholinesterase proximal to the injection, suggesting that at least a portion of the [3H]..
  76. ncbi Perinatal heptachlor exposure increases expression of presynaptic dopaminergic markers in mouse striatum
    W Michael Caudle
    Center for Neurodegenerative Disease, Emory University, Whitehead Biomedical Research Building 505, 615 Michael Street, Atlanta, GA 30322, USA
    Neurotoxicology 26:721-8. 2005
    ....
  77. ncbi Binding of [3H]mazindol to cardiac norepinephrine transporters: kinetic and equilibrium studies
    David M Raffel
    Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical School, 3480 Kresge III Building, Ann Arbor 48109 0552, USA
    Naunyn Schmiedebergs Arch Pharmacol 370:9-16. 2004
    ..The radioligand [3H]mazindol binds with high affinity to NET...
  78. ncbi Chronic high dose L-DOPA alone or in combination with the COMT inhibitor entacapone does not increase oxidative damage or impair the function of the nigro-striatal pathway in normal cynomologus monkeys
    L Lyras
    Neurodegenerative Disease Research Centre, Guy s, King s and St Thomas School of Biomedical Sciences, King s College, London, United Kingdom
    J Neural Transm 109:53-67. 2002
    ..of the nigro-striatal pathway was assessed by nigral tyrosine hydroxylase mRNA levels and specific [(3)H]mazindol binding to dopaminergic terminals in caudate-putamen...
  79. ncbi [Analysis and identification of illegal constituents in health food products implicitly advertizing tonic or slimming effect in the National Institute of Health Sciences in Japan]
    Yukihiro Goda
    Division of Pharmacognosy, Phytochemistry and Narcotics, National Institute of Health Sciences
    Yakugaku Zasshi 134:197-202. 2014
    ..In addition, phenolphthalein, fenfluramine, sibtramine, desdimethylsibtramine, orlistat, mazindol, Rhubarb, Senna Leaf, etc. have been found as illegal constituents...
  80. ncbi Dopaminergic involvement in the cocaine-induced up-regulation of benzodiazepine receptors in the rat caudate nucleus
    N Goeders
    Department of Pharmacology and Therapeutics, Louisiana State University Medical Center, Shreveport 71130
    Brain Res 515:1-8. 1990
    ..extent of the lesion was assessed by measuring dopaminergic and noradrenergic uptake sites visualized with [3H]mazindol, while [3H]Ro 15-1788 was used to estimate the number of benzodiazepine receptors...
  81. ncbi Pharmacology in health foods:merits and demerits of food with health claims for the prevention of metabolic syndrome
    Naoki Sakane
    Division of Preventive Medicine, Clinical Research Institute for Endocrine and Metabolic Disease, National Hospital Organization Kyoto Medical Center, Japan
    J Pharmacol Sci 115:476-80. 2011
    ..Many anti-obesity drugs have been associated with unintended therapeutic outcomes. Currently, only one drug (mazindol) is approved in Japan for short-term treatment of individuals with a BMI over 35 kg/m(2)...
  82. ncbi [Brazilian guidelines for the treatment of narcolepsy]
    Flavio Aloe
    Hospital das Clinicas, Universidade de Sao Paulo, SP, Brasil
    Rev Bras Psiquiatr 32:305-14. 2010
    ..Second-line choices for the treatment of excessive sleepiness are slow-release metylphenidate followed by mazindol. The first-line treatments of cataplexy are the antidepressants, reboxetine, clomipramine, venlafaxine, ..
  83. ncbi Efficacy of psychostimulant drugs for cocaine dependence
    Xavier Castells
    Department of Psychiatry, Hospital Universitari Vall d Hebron and Department of Pharmacology, Therapeutics and Toxicology, , Barcelona, Catalonia, Spain
    Cochrane Database Syst Rev 2:CD007380. 2010
    ..metabolized to a psychostimulant have been investigated: bupropion, dexamphetamine, methylphenidate, modafinil, mazindol, methamphetamine and selegiline. Psychostimulants did not reduce cocaine use (SMD 0.11, 95%CI: -0.07 to 0...
  84. pmc The roles of dopamine transport inhibition and dopamine release facilitation in wake enhancement and rebound hypersomnolence induced by dopaminergic agents
    John A Gruner
    Cephalon, Inc, West Chester, PA, USA
    Sleep 32:1425-38. 2009
    ..In these studies, DA-releasing and DAT-inhibiting agents and their interaction were systematically examined for their ability to increase wake and induce RHS...
  85. pmc Time-course of SKF-81297-induced increase in glutamic acid decarboxylase 65 and 67 mRNA levels in striatonigral neurons and decrease in GABA(A) receptor alpha1 subunit mRNA levels in the substantia nigra, pars reticulata, in adult rats with a unilateral 6
    N Yamamoto
    Department of Anatomy and Neurobiology, Boston University School of Medicine, 715 Albany Street, Room L1004, Boston, MA 02118, USA
    Neuroscience 154:1088-99. 2008
    ..They also suggest that the down-regulation of nigral GABA(A) receptors is linked to the increase in striatal GAD67 mRNA levels in the dopamine-depleted striatum...
  86. ncbi Dopamine D1 receptor behavioral responsitivity following selective lesions of the striatal patch compartment during development
    B S Neal
    Department of Psychiatry, University of Pennsylvania School of Medicine, Philadelphia 19104
    Brain Res Dev Brain Res 60:105-13. 1991
    ..Autoradiographs of [3H]mazindol binding to DA uptake sites (a measure of DA terminal density) showed a 'patchy' loss of approx...
  87. ncbi Effect of 6-hydroxydopamine on murine hematopoietic stem cells: enhanced cytotoxicity on megakaryocyte colony forming units
    B G Gordon
    Section of Pediatric Hematology Oncology and Bone Marrow Transplantation, University of Nebraska Medical Center, Omaha
    Life Sci 49:121-7. 1991
    ..b>Mazindol, a selective dopamine uptake inhibitor did not alter 6-OHDA effect on either CFU-Meg or CFU-GM...
  88. ncbi Effects of pitolisant, a histamine H3 inverse agonist, in drug-resistant idiopathic and symptomatic hypersomnia: a chart review
    Smaranda Leu-Semenescu
    National Reference Centre for Narcolepsy and Idiopathic Hypersomnia, France AP HP, hôpital universitaire Pitié Salpêtrière, Service des Pathologies du Sommeil, Paris, France Pierre and Marie Curie University, Centre de Recherche de l Institut du Cerveau et de la Moelle Epiniere, Inserm U 1127, CNRS UMR7225, Paris, France Electronic address
    Sleep Med 15:681-7. 2014
    ..by blocking presynaptic H3 histamine reuptake) in patients with idiopathic (IH) and symptomatic (SH) hypersomnia plus sleepiness refractory to available stimulants (modafinil, methylphenidate, mazindol, sodium oxybate, and d-amphetamine).
  89. ncbi Uptake and decarboxylation of L-3,4-dihydroxyphenylalanine in cultured monkey placenta amniotic epithelial cells
    M A Elwan
    Department of Inherited Metabolic Diseases, National Institute of Neuroscience, NCNP, Kodaira, Tokyo 187 8502, Japan
    Placenta 28:245-8. 2007
    ..Neither d-DOPA nor DA uptake blockers such as mazindol and GBR 12935 significantly affected l-DOPA uptake and hence DA levels...
  90. ncbi [3H]WIN 35,065-2: a ligand for cocaine receptors in striatum
    M C Ritz
    Neuroscience Branch, NIDA Addiction Research Center, Baltimore, Maryland
    J Neurochem 55:1556-62. 1990
    ..Pharmacological characterization suggests that [3H]WIN 35,065-2 binds to the dopamine transporter. Mazindol, GBR 12909, nomifensine, and (-)-cocaine are potent inhibitors of [3H]WIN 35,065-2 binding...
  91. ncbi Dysfunction of the cortico-basal ganglia-cortical loop in a rat model of early parkinsonism is reversed by metabotropic glutamate receptor 5 antagonism
    Abid Oueslati
    Interactions Cellulaires, Neurodégénérescence et Neuroplasticité, UMR 6186, CNRS Université de la Méditerranée, 31 Chemin Joseph Aiguier, 13402 Marseille Cedex 20, France
    Eur J Neurosci 22:2765-74. 2005
    ..These data suggest that the expression of akinetic deficits in early parkinsonism is associated with focused metabolic changes in the cortico-basal ganglia-cortical loop downstream of the striatum and pallidal complex...
  92. ncbi Dopamine uptake inhibitors block long-term neurotoxic effects of methamphetamine upon dopaminergic neurons
    G J Marek
    Department of Pharmacological and Physiological Sciences, University of Chicago, IL 60637
    Brain Res 513:274-9. 1990
    ..dopamine (DA) uptake inhibitors blocked MA-induced neostriatal depletions (amfonelic acid (AFA) much greater than mazindol (MAZ) greater than or equal to bupropion (BUP) greater than benztropine (BENZ)) was similar to their potency at ..
  93. ncbi Autoradiography of dopamine receptors and dopamine uptake sites in the spontaneously hypertensive rat
    K Kujirai
    Department of Neurology, Columbia University, College of Physicians and Surgeons, New York, NY 10032
    Brain Res Bull 25:703-9. 1990
    ..and D2 receptors by using [3H]SCH 23390 and [3H]spiperone binding, respectively, and DA uptake sites by using [3H]mazindol binding in spontaneously hypertensive rats (SHR) and Sprague-Dawley (SD) rats...
  94. ncbi Endothelin-1 inhibits the neuronal norepinephrine transporter in hearts of male rats
    Johannes Backs
    Department of Cardiology, University of Heidelberg, INF 410, D 69120 Heidelberg, Germany
    Cardiovasc Res 67:283-90. 2005
    ..An impairment of cardiac NE re-uptake by the neuronal NE transporter (NET) contributes to an increased NE net release in failing hearts. We hypothesized that both phenomena are caused by ET-1-mediated inhibition of NET...
  95. ncbi Acquired narcolepsy in an acromegalic patient who underwent pituitary irradiation
    Owen J Dempsey
    Department of Respiratory Medicine, Aberdeen Royal Infirmary, Grampian University Hospital Trust, Aberdeen, Scotland, UK
    Neurology 61:537-40. 2003
    ..Onset of narcolepsy is unusual at this age and the temporal relationship following radiotherapy suggests this treatment was implicated. His CSF hypocretin levels were normal, indicating other factors may be important in his narcolepsy...
  96. ncbi Discriminative stimulus effects of (-)-ephedrine in rats: analysis with catecholamine transporter and receptor ligands
    Lance R McMahon
    Department of Pharmacology and Toxicology, The University of Texas Medical Branch, Galveston, TX 77555 1031, USA
    Drug Alcohol Depend 70:255-64. 2003
    ..In the present study, the catecholamine reuptake inhibitors mazindol and nomifensine, the norepinephrine (NE) reuptake inhibitor desipramine, and the dopamine D(2)-like (e.g...
  97. pmc Dose-related neuroprotective effects of chronic nicotine in 6-hydroxydopamine treated rats, and loss of neuroprotection in alpha4 nicotinic receptor subunit knockout mice
    R E Ryan
    Department of Pharmaceutical Biology and Pharmacology, Victorian College of Pharmacy, Monash University, Parkville, Victoria 3052, Australia
    Br J Pharmacol 132:1650-6. 2001
    ..In both models of Parkinsonian-like damage, loss of striatal dopaminergic nerve terminals was assessed by [(3)H]-mazindol autoradiography...
  98. ncbi Synthesis and preliminary characterization of a high-affinity novel radioligand for the dopamine transporter
    A K Dutta
    Wayne State University, Department of Pharmaceutical Sciences, Detroit, Michigan, USA
    Synapse 39:175-81. 2001
    ..Thus, the pharmacological profile of [3H]O-972 indicated that DAT inhibitors, which include GBR 12909, mazindol, CFT, and cocaine, could potently displace this novel radioligand from monkey brain striatum tissue...
  99. ncbi Effects of 7-nitroindazole, an NOS inhibitor on methamphetamine-induced dopaminergic and serotonergic neurotoxicity in mice
    S F Ali
    Neurochemistry Laboratory, FDA, Jefferson, Arkansas 72079, USA
    Ann N Y Acad Sci 844:122-30. 1998
    ..acid (DOPAC), and homovanillic acid (HVA), respectively, and a 48% decrease in the number of [3H]mazindol binding sites in the striatum compared to control values...
  100. ncbi 1-Methyl-4-phenylpridinium (MPP+)-induced functional run-down of GABA(A) receptor-mediated currents in acutely dissociated dopaminergic neurons
    Jie Wu
    Division of Neurology, Barrow Neurological Institute, St Joseph s Hospital and Medical Center, Phoenix, AZ 85013, USA
    J Neurochem 83:87-99. 2002
    ..The MPP+-induced I(GABA) run-down can be prevented by a DA transporter inhibitor, mazindol, and can be mimicked by a metabolic inhibitor, rotenone...
  101. ncbi High performance liquid chromatographic determination of mazindol in human plasma
    A Kaddoumi
    Department of Analytical Research for Pharmacoinformatics, Graduate School of Pharmaceutical Sciences, Nagasaki University, Japan
    Analyst 126:1963-8. 2001
    ..convenient high performance liquid chromatographic method with UV detection is described for the determination of mazindol [5-(p-chlorophenyl)-2,5-dihydro-3H-imidazo[2,1-a]isoindol-5-ol] and its major metabolite, 2-(2-aminoethyl)-3-(p-..

Research Grants35

  1. DOPAMINE TRANSPORTER LIGANDS AS COCAINE MEDICATIONS
    Alexandros Makriyannis; Fiscal Year: 2002
    ..approach is based on evidence indicating that the known DAT inhibitors, cocaine, benztropine, GBR 12909 and mazindol interact with the DAT but have non-identical binding domains...
  2. Cocaine Withdrawal: A Window of Treatment Opportunity
    Tong Lee; Fiscal Year: 2009
    ..The present proposal emphasizes the use of a non-abused drug (e.g., mazindol or pergolide) to simulate daily acute cocaine withdrawal, which is subsequently targeted with a 5-HT3, 5-HT2A or ..
  3. RADIOLIGANDS FOR CENTRAL NORADRENERGIC UPTAKE SITES
    Shanaz Tejani Butt; Fiscal Year: 1992
    ..So far, studies have been done with labelled desipramine and more recently with labelled mazindol. Labelled desipramine is not an ideal ligand for labelling uptake sites associated with NE as it gives a high ..
  4. STIMULUS PROPERTIES OF ANXIOLYTICS IN HUMANS
    Chris Ellyn Johanson; Fiscal Year: 1991
    ..Further, stimulant drugs (e.g., mazindol) that were not self-administered in previous studies will be evaluated under similar conditions to determine ..
  5. COCAINE RECEPTORS AND ADDICTION
    MOHYEE ELDEFRAWI; Fiscal Year: 1993
    ..g. benztropine, nomifensine and mazindol) do not have the reinforcing properties of cocaine...
  6. INHIBITION OF DOPAMINE RELEASE BY COCAINE AND OTHER DRUG
    DOROTHY DEMBIEC COHEN; Fiscal Year: 1990
    Cocaine, nomifensine, mazindol, dita and desmethylimipramine (DMI) inhibit the K+-stimulated release of (3H-DA) from nerve terminals in the striatum.d The extent of inhibition is 40 -50%...
  7. DOPAMINE TRANSPORTER IMAGING IN COCAINE ABUSE
    DEAN WONG; Fiscal Year: 1999
    ..Two methods will be studied, one with unlabeled mazindol and IV unlabeled WIN 35,428 given prior to the second of two high specific activity [11/C] WIN 35,428 PET scans...
  8. Human Cocaine Discrimination
    CRAIG RUSH; Fiscal Year: 2006
    ..discriminative-stimulus and subjective effects of cocaine will be assessed alone and following pretreatment with mazindol, a dopamine uptake blocker (Exp. 1); fluphenazine, a D1-D2 dopamine receptor antagonist (Exp...
  9. LOCALIZED NEUROTOXICITY OF METHAMPHETAMINE AND COCAINE
    DAVID BRUNSWICK; Fiscal Year: 1990
    ..Norepinephrine uptake sites will be labelled using either 3H-desmethylimipramine or 3H-mazindol (measured as the difference in the binding in the absence and presence of desmethylimipramine)...
  10. DRUGS OF ABUSE--DOPAMINE RELEASE AND REUPTAKE
    JAMES SCHENK; Fiscal Year: 1999
    ..obtained with other inhibitors of dopamine transport, including but not limited to GBR- 12909, nomifensine, and mazindol. Kinetic observations observed in vitro will be compared to those observed in vivo using in vivo voltammetry...
  11. COCAINE: EFFECTS ON DOPAMINE RECEPTORS AND TRANSPORT
    James Wamsley; Fiscal Year: 1991
    ..of receptor/uptake site changes will be investigated using (3H)SCH 23390 (D1), (3H)sulpiride (D2), (3H)mazindol (uptake sites), as well as with (3H)cocaine itself...
  12. MESOTELENCEPHALIC INJURY AND REGIONAL DOPAMINE UPTAKE
    John Marshall; Fiscal Year: 1992
    ..rabbits, and humans have a higher density of dopamine uptake sites (determined by [3H]DA uptake kinetics or [3H]mazindol binding to the associated recognition site) in dorsal striatum than ventrally, with particularly low levels ..
  13. MAZINDOL ANALOGS AS COCAINE RECEPTOR ANTAGONISTS
    WILLIAM HOULIHAN; Fiscal Year: 1999
    ..be approached by a systematic structural modification using molecular modeling techniques, of the clinically used mazindol, a known inhibitor of the cocaine binding site with a poor dopamine uptake/cocaine binding ratio (1.04)...
  14. COCAINE ANTAGONISTS THROUGH 3D PHARMACOPHORE SEARCHING
    Shaomeng Wang; Fiscal Year: 2000
    ..Performance of biological evaluations of selected compounds3 that meet the pharmacophore requirements in the [ H]mazindol binding and [3H]DA uptake assays...
  15. DRUG ABUSE & BEHAVIORAL EXPERIENCE IN HUMANS
    Chris Ellyn Johanson; Fiscal Year: 1991
    ..Thus, in the present experiments, the ability of behavioral experience to modify effects of mazindol, a drug which has similar behavioral properties to amphetamine but is not abused, will also be determined...
  16. HEART IMAGING AGENTS--STRUCTURAL MECHANISTICS STUDY
    David Raffel; Fiscal Year: 2001
    ..Finally, [11C]- and [18F]-labeled polar derivatives of the psychostimulant methcathinone will be synthesized as potential NET markers and their in vitro NET affinities determined as the cloned human NET transporter. ..
  17. Psychostimulants and Alpha-1 Adrenoceptor Subtypes
    Paul Wellman; Fiscal Year: 2006
    ..These studies will advance our understanding of the behavioral functions of brain a l-AR subtypes and may lead to the identification of new drugs that inhibit eating without activating brain reinforcement systems. ..
  18. HEART IMAGING AGENTS--STRUCTURAL MECHANISTICS STUDY
    David Raffel; Fiscal Year: 2004
    ..Finally, [11C]- and [18F]-labeled polar derivatives of the psychostimulant methcathinone will be synthesized as potential NET markers and their in vitro NET affinities determined as the cloned human NET transporter. ..
  19. Heavy Metal and Drug Self-Administration: Mechanisms
    PAUL JEFFERSON WELLMAN; Fiscal Year: 2010
    ..e., lead contamination and cocaine use. Based on the available literature, there is reason to believe that environmental pollutants may increase vulnerability to drug addiction. ..
  20. DIETARY OBESITY
    George Bray; Fiscal Year: 2007
    ..We now propose these well founded, important and exciting studies which will provide critical new insights into anatomical, physiological and molecular mechanisms by which high levels of dietary fat induce obesity. ..
  21. Genetics of Opioid Dependence in a Hmong (Thai) Isolate
    Robert Malison; Fiscal Year: 2007
    ..Such studies, we believe, afford significant, perhaps uniquely powerful, advantages for identifying susceptibility loci for OD. [unreadable] [unreadable] [unreadable] [unreadable]..
  22. COCAINE SENSITIZATION AND THE DOPAMINE TRANSPORTER
    NANCY ZAHNISER; Fiscal Year: 2008
    ..abstract_text> ..
  23. Louisiana Clinical and Translational Science Center Planning Phase
    Donna Ryan; Fiscal Year: 2006
    ..In addition to activities serving Louisiana, the LA CaTS Center will serve as an incubator to foster the development of innovative tools and information technologies that can benefit the field. [unreadable] [unreadable] [unreadable]..
  24. Adolescent Exposure to Psychostimulants: Role of nNOS
    Yossef Itzhak; Fiscal Year: 2008
    ..Results of these studies would provide new information on mechanisms that underlie the development of hypersensitivity to these drugs from adolescence through adulthood. ..
  25. DOPAMINE TRANSPORTER AGENTS AGAINST COCAINE DEPENDENCE
    ALOKE DUTTA; Fiscal Year: 2007
    ..Compounds selected based on their in vitro activity will be tested for effects on locomotor activity and drug discrimination and self-administration studies to assess their potential in replacement therapy. ..
  26. Behavioral Sensitization and Parkinson's Disease
    Jean Jacques Soghomonian; Fiscal Year: 2006
    ....
  27. Pharmacotherapy for opioid and cocaine dependence
    Bruce Rounsaville; Fiscal Year: 2005
    ..4. To examine depression as a predictor of response. 5. To examine three month follow-up status after completing the treatment trial for continuation in treatment, abstinence from illicit drugs, and depressive symptoms. ..
  28. Substituted Amphetamines: NO-Dependent Mechanisms
    Yossef Itzhak; Fiscal Year: 2005
    ....
  29. Cellular mRNA Analysis in a Murine Huntington's Model
    SARAH AUGOOD; Fiscal Year: 2005
    ..Understanding transcriptional dysregulation at a cellular level may facilitate the search for novel therapeutics for HD and other polyglutamine diseases. ..
  30. Cocaine, Disulfiram & DBH: A Pharmacomechanistic Study
    Robert Malison; Fiscal Year: 2004
    ..abstract_text> ..
  31. MOR expressing neurons in pain and morphine analgesia
    RONALD WILEY; Fiscal Year: 2004
    ..Many valuable future experiments and clinical applications may be possible if dermorphin-saporin proves effective. ..
  32. ADVANCED TRAINING IN SPECT/PET NEURORECEPTOR IMAGING
    Robert Malison; Fiscal Year: 2003
    ..abstract_text> ..
  33. SPECT IMAGING OF DOPAMINE FUNCTION IN DAYTOP SUBJECTS
    Robert Malison; Fiscal Year: 2001
    ..abstract_text> ..
  34. Reconsolidation and extinction processes in the treatment of drug addiction
    Yossef Itzhak; Fiscal Year: 2010
    ..abstract_text> ..