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| selegilineSummarySummary: A selective, irreversible inhibitor of Type B monoamine oxidase. It is used in newly diagnosed patients with Parkinson's disease. It may slow progression of the clinical disease and delay the requirement for levodopa therapy. It also may be given with levodopa upon onset of disability. (From AMA Drug Evaluations Annual, 1994, p385) The compound without isomeric designation is Deprenyl. Top Publications
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Neuroprotective actions of selegilineM Ebadi
Department of Pharmacology, Physiology, and Therapeutics, University of North Dakota School of Medicine and Health Sciences, Grand Forks, North Dakota 58203, USA
J Neurosci Res 67:285-9. 2002b>Selegiline, a selective inhibitor of monoamine oxidase-B (MAO-B), was one of the first adjunct therapies in clinical neurology...
Selegiline and oxidative stress in HIV-associated cognitive impairmentG Schifitto
University of Rochester, NY, USA
Neurology 73:1975-81. 2009To assess the effectiveness of the selegiline transdermal system (STS) in reversing HIV-induced metabolic brain injury (as measured by proton magnetic resonance spectroscopy [MRS]) and in decreasing oxidative stress, measured by CSF ..
A new low-dose formulation of selegiline: clinical efficacy, patient preference and selectivity for MAO-B inhibitionA Clarke
Scherer DDS, Swindon, United Kingdom
J Neural Transm 110:1257-71. 2003Three studies were performed using a fast dissolving formulation of selegiline hydrochloride designed for buccal absorption "Zydis Selegiline"...
Monoamine oxidase-inhibition and MPTP-induced neurotoxicity in the non-human primate: comparison of rasagiline (TVP 1012) with selegilineA Kupsch
Department of Neurology, Klinikum Grosshadern, Ludwig Maximilians University, and Institute of Physiology, Munchen, Federal Republic of Germany
J Neural Transm 108:985-1009. 2001..B (MAO-B) has been reported to be implicated in both MPTP-induced parkinsonism and Parkinson's disease, since selegiline (L-deprenyl), an irreversible MAO-B inhibitor, prevents MPTP-induced neurotoxicity in numerous species including ..
Contrasting neuroprotective and neurotoxic actions of respective metabolites of anti-Parkinson drugs rasagiline and selegilineOrit Bar Am
Eve Topf and US National Parkinson Foundation Center of Excellence for Neurodegenerative Diseases Research, Technion-Faculty of Medicine, Efron St PO Box 9697, Haifa 31096, Israel
Neurosci Lett 355:169-72. 2004The anti-Parkinson selective irreversible monoamine oxidase B inhibitor drugs, rasagiline and selegiline, have been shown to possess neuroprotective activities in cell culture and in vivo models...
The anti-Parkinsonian drug selegiline delays the nucleation phase of α-synuclein aggregation leading to the formation of nontoxic speciesCarolina A Braga
Instituto de Bioquimica Medica, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ 21941 590, Brazil
J Mol Biol 405:254-73. 2011..b>Selegiline (Sel) is a noncompetitive monoamino oxidase B inhibitor that has neuroprotective effects and has been ..
Selegiline in the treatment of attention deficit hyperactivity disorder in children: a double blind and randomized trialShahin Akhondzadeh
Roozbeh Psychiatric Hospital, Tehran University of Medical Sciences, South Kargar Avenue, Tehran 13334, Iran
Prog Neuropsychopharmacol Biol Psychiatry 27:841-5. 2003..b>Selegiline is a type B monoamine oxidase inhibitor (MAOI) that is metabolized to amphetamine and methamphetamine stimulant ..
Selegiline in comparison with methylphenidate in attention deficit hyperactivity disorder children and adolescents in a double-blind, randomized clinical trialMohammad Reza Mohammadi
Department of Psychiatry, Tehran University of Medical Sciences, Psychiatry and Clinical Psychology Research Center, Roozbeh Hospital, Tehran, Iran
J Child Adolesc Psychopharmacol 14:418-25. 2004OBJECTIVES: The aim of this study was to examine the selegiline treatment compared to methylphenidate (MPH) in children and adolescents with attention deficit hyperactivity disorder (ADHD)...
Selegiline protects against recognition memory impairment induced by neonatal iron treatmentMaria Noemia Martins de Lima
, Instituto de Geriatria e Gerontologia, , , 90619-900 Porto Alegre, RS, Brazil
Exp Neurol 196:177-83. 2005..The aim of the present study was to determine whether selegiline, a monoamine oxidase (MAO) inhibitor known for its neuroprotective properties, could protect rats against ..
Increased cell-cell adhesion, a novel effect of R-(-)-deprenylV Jenei
Institute of Biomolecular Chemistry, Chemical Research Center, Hungarian Academy of Sciences, Budapest, Hungary
J Neural Transm 112:1433-45. 2005..The effect of R-(-)-deprenyl was not reversible during a 24-hour recovery period. In summary, we described a new, MAO-B independent effect of R-(-)-deprenyl on cell-cell adhesion which can contribute to its neuroprotective function...
Metabolic transformation plays a primary role in the psychostimulant-like discriminative-stimulus effects of selegiline [(R)-(-)-deprenyl]Sevil Yasar
Division of Geriatric Medicine and Gerontology, Johns Hopkins University School of Medicine, Baltimore, MD 21224, USA
J Pharmacol Exp Ther 317:387-94. 2006l-Deprenyl [selegiline, (R)-(-)-deprenyl] is a selective inhibitor of monoamine oxidase B (MAO-B) used in the treatment of Parkinson's disease and proposed as an antidepressant and an aid for cigarette-smoking cessation and treatment of ..
(-)-D-Deprenyl attenuates apoptosis in experimental brain ischaemiaL Simon
National Institute of Psychiatry and Neurology, National Stroke Center, , H-1021, Budapest, Hungary
Eur J Pharmacol 430:235-41. 2001..D-Deprenyl treatment increased the number of GAP-43-positive cells. We conclude that (-)-D-deprenyl reduced the number of affected cells and induced neuronal plasticity...
Selegiline potentiates the effects of EGb 761 in response to ischemic brain injuryY S Kwon
Neurotoxicology Program, College of Pharmacy, Korea Institute of Drug Abuse, Kangwon National University, Chunchon 200-701, South Korea
Neurochem Int 45:157-70. 2004We evaluated whether combined treatment with selegiline, a selective MAO-B inhibitor, and EGb 761, a standard extract of Ginkgo biloba, has synergistic effects against ischemic reperfusion injury (IRI) in gerbils...
Orally disintegrating selegiline in Parkinson patients with dopamine agonist-related adverse effectsKelly E Lyons
University of Kansas Medical Center, Kansas City, KS 66160, USA
Clin Neuropharmacol 33:5-10. 2010To determine whether adding orally disintegrating selegiline (ODS) while decreasing dopamine agonist (DA) dosages would reduce DA-related adverse effects (AEs) of excessive daytime sleepiness (EDS), pedal edema, hallucinations, and ..
The multiple actions of selegilineManuchair Ebadi
Department of Pharmacology, Physiology, and Therapeutics, University of North Dakota, School of Medicine and Health Sciences, P.O. Box 9037, 501 North Columbia Road, Grand Forks, ND 58203, USA
Proc West Pharmacol Soc 45:39-41. 2002
Low dose (-)deprenyl is cytoprotective: it maintains mitochondrial membrane potential and eliminates oxygen radicalsL Simon
National Institute of Psychiatry and Neurology, National Stroke Center, Department of Vascular Neurology, Semmelweis University, Budapest H 1021 Hungary
Life Sci 78:225-31. 2005....
Orally disintegrating selegiline for the treatment of Parkinson's diseaseMatthias Lohle
Technische Universitat Dresden, Department of Neurology, Fetscherstrasse 74, 01307 Dresden, Germany
Expert Opin Pharmacother 9:2881-91. 2008The selective monoamine oxidase type B inhibitor selegiline is commonly administered as medical treatment to patients suffering from Parkinson's disease...
Comparison of neuroprotective and neurorestorative capabilities of rasagiline and selegiline against lactacystin-induced nigrostriatal dopaminergic degenerationWen Zhu
Department of Neurology, The 1st Affiliated Hospital of Sun Yat sen University, Guangzhou, China
J Neurochem 105:1970-8. 2008..Rasagiline and selegiline are selective and irreversible monoamine oxidase-B inhibitors that possess significant protective properties on ..
Freezing of gait in PD: prospective assessment in the DATATOP cohortN Giladi
Movement Disorders Division, Department of Neurology, Columbia-Presbyterian Medical Center, New York, NY, USA
Neurology 56:1712-21. 2001..Deprenyl, in the absence of L-dopa, was found to be an effective prophylactic treatment and should be considered for patients with PD who have an onset of gait difficulty...
Survival in Parkinson disease: thirteen-year follow-up of the DATATOP cohortC Marras
Division of Neurology, Toronto Western Hospital, University Health Network, University of Toronto, Ontario, Canada M5T 2S8
Neurology 64:87-93. 2005..To investigate predictors of survival in Parkinson disease (PD)...
Transdermal selegiline: targeted effects on monoamine oxidases in the brainLynn Wecker
Department of Pharmacology and Therapeutics, University of South Florida College of Medicine, Tampa, Florida 33612-4799, USA
Biol Psychiatry 54:1099-104. 2003..These studies determined whether the transdermal administration of selegiline has differential effects on MAOs in brain versus the gastrointestinal system...
Transdermal selegiline and intravenous cocaine: safety and interactionsElisabeth J Houtsmuller
Behavioral Pharmacology Research Unit, Johns Hopkins University School of Medicine, Bayview Medical Center, 5510 Nathan Shock Drive, Baltimore, MD 21224 6823, USA
Psychopharmacology (Berl) 172:31-40. 2004..b>Selegiline, a selective monoamine oxidase B inhibitor, indirectly modulates dopamine levels, and research suggests ..
A randomized controlled trial of oral selegiline plus nicotine skin patch compared with placebo plus nicotine skin patch for smoking cessationR Biberman
Division of Health, Maccabi Health Care Services, Sackler Medical Faculty, Tel Aviv University, Israel
Addiction 98:1403-7. 2003To compare the effect of oral selegiline plus nicotine patch with placebo plus nicotine patch on smoking cessation rates.
Effects of (-)deprenyl (selegiline) on acetylcholinesterase and Na(+),K(+)-ATPase activities in adult rat whole brainCharalambos Antoniades
Department of Experimental Physiology, Medical School, University of Athens, P.O. Box 65257, GR-154 01 Athens, Greece
Pharmacol Res 46:165-9. 2002..We conclude that (-)deprenyl is an indirect AChE inhibitor and Na(+),K(+)-ATPase stimulator in the rat brain (in vitro)...
Urinary excretion of selegiline N-oxide, a new indicator for selegiline administration in manM Katagi
Forensic Science Laboratory, Osaka Prefectural Police HQ, 1 3 18, Hommachi, Chuoku, Osaka 541 0053, Japan
Xenobiotica 32:823-31. 20021. The metabolism of selegiline (SG) has been studied by investigating the time-course of urinary excretion of SG and its metabolites using high-performance liquid chromatography-electrospray ionization mass spectrometry (LC-ESI MS) in ..
Transdermal selegiline in major depression: a double-blind, placebo-controlled, parallel-group study in outpatientsJ Alexander Bodkin
McLean Hospital, 115 Mill St. Belmont, MA 02478, USA
Am J Psychiatry 159:1869-75. 2002OBJECTIVE: The authors investigated the efficacy and safety of transdermal selegiline in adult outpatients with major depressive disorder...
A preliminary placebo-controlled trial of selegiline hydrochloride for smoking cessationTony P George
Program for Research in Smokers with Mental Illness (PRISM, New Haven, Connecticut 06519, USA
Biol Psychiatry 53:136-43. 2003..to be involved in nicotine dependence, we studied the safety and efficacy of the monoamine oxidase B inhibitor selegiline hydrochloride compared with placebo for smoking cessation in nicotine-dependent cigarette smokers...
Selegiline potentiates cocaine-induced increases in rodent nucleus accumbens dopamineWynne K Schiffer
Department of Neurobiology and Behavior, Stony Brook University, Stony Brook, New York 11794, USA
Synapse 48:35-8. 2003b>Selegiline has been proposed as a treatment for cocaine addiction and studies in humans suggest that it attenuates cocaine's reinforcing effects...
Daily transdermal administration of selegiline to guinea-pigs preferentially inhibits monoamine oxidase activity in brain when compared with intestinal and hepatic tissuesMichael Mawhinney
Department of Pharmacology, West Virginia University School of Medicine, Morgantown, WV 26506, USA
J Pharm Pharmacol 55:27-34. 2003b>Selegiline has been formulated in an acrylic polymer adhesive mixture to be employed as a constant release topical patch for daily transdermal administration...
A double-blind, placebo-controlled trial of the safety and efficacy of selegiline transdermal system without dietary restrictions in patients with major depressive disorderJay D Amsterdam
Depression Research Unit, Department of Psychiatry, University of Pennsylvania School of Medicine, Philadelphia, USA
J Clin Psychiatry 64:208-14. 2003The monoamine oxidase (MAO) inhibitor selegiline has demonstrated antidepressant efficacy superior to placebo...
Selegiline long-term effects on brain acetylcholinesterase, (Na+,K+)-ATPase activities, antioxidant status and learning performance of aged ratsHaris Carageorgiou
Department of Experimental Pharmacology, Medical School, University of Athens, Athens, Greece
Pharmacol Res 48:245-51. 2003The aim of this study was to investigate the effects of selegiline ((-)deprenyl), an irreversible inhibitor of monoaminoxidase-B (MAO-B): (a) on brain acetylcholinesterase (AChE), (Na(+),K(+))-ATPase and Mg(2+)-ATPase activities; (b) ..
Comparative studies on the cytochrome p450-associated metabolism and interaction potential of selegiline between human liver-derived in vitro systemsJarmo S Salonen
Orion Pharma Preclinical and Clinical R and D, Turku, Finland
Drug Metab Dispos 31:1093-102. 2003b>Selegiline was used as a model compound in a project aimed at comparing, evaluating, and integrating different in vitro approaches for the prediction of cytochrome p450 (p450)-catalyzed hepatic drug metabolism in humans (EUROCYP)...
A new formulation of selegiline: improved bioavailability and selectivity for MAO-B inhibitionA Clarke
Scherer DDS, Swindon, United Kingdom
J Neural Transm 110:1241-55. 2003..studies were conducted in healthy volunteers to compare the pharmacokinetic and pharmacodynamic profiles of selegiline hydrochloride in a new formulation designed for buccal absorption "Zydis Selegiline" (1...
Cardiovascular activity of rasagiline, a selective and potent inhibitor of mitochondrial monoamine oxidase B: comparison with selegilineZaid A Abassi
Department of Physiology and Biophysics, Technion Rappaport Faculty of Medicine and Rappaport Family Institute for Research in the Medical Sciences, Technion, Haifa, Israel
Br J Pharmacol 143:371-8. 2004b>Selegiline is used for treating Parkinson's disease...
Selegiline is a mechanism-based inactivator of CYP2A6 inhibiting nicotine metabolism in humans and miceEric C K Siu
Department of Pharmacology, University of Toronto, 1 King s College Circle, Room 4326, Toronto, Ontario, Canada
J Pharmacol Exp Ther 324:992-9. 2008b>Selegiline (l-deprenyl) is in clinical treatment trials as a potential smoking cessation drug. We investigated the affect of selegiline and its metabolites on nicotine metabolism...
Evaluation of the potential for pharmacodynamic and pharmacokinetic drug interactions between selegiline transdermal system and two sympathomimetic agents (pseudoephedrine and phenylpropanolamine) in healthy volunteersAlbert J Azzaro
Somerset Pharmaceuticals, Inc
J Clin Pharmacol 47:978-90. 2007b>Selegiline transdermal system is a recently approved monoamine oxidase inhibitor antidepressant...
Selegiline transdermal system: an examination of the potential for CYP450-dependent pharmacokinetic interactions with 3 psychotropic medicationsAlbert J Azzaro
Chief Scientific Officer, Somerset Pharmaceuticals, Inc, Rocky Point Center, 3030 North Rocky Point Drive, Suite 250, Tampa, FL 33607, USA
J Clin Pharmacol 47:146-58. 2007b>Selegiline transdermal system (STS) is a recently approved monoamine oxidase inhibitor antidepressant...
The path from anti Parkinson drug selegiline and rasagiline to multifunctional neuroprotective anti Alzheimer drugs ladostigil and m30Moussa B H Youdim
Eve Topf Centres of Excellence for Neurodegenerative Diseases Research, Technion Rappaport Family Faculty of Medicine and Department of Pharmacology, Haifa, Israel
Curr Alzheimer Res 3:541-50. 2006..has its origin in the anti Parkinson action of the selective monoamine oxidase (MAO) B inhibitor, l-deprenyl (selegiline ), a failed anti depressant in 1975...
Selegiline transdermal system for the treatment of major depressive disorder: an 8-week, double-blind, placebo-controlled, flexible-dose titration trialAlan D Feiger
Department of Psychiatry, University of Colorado School of Medicine, Denver, CO, USA
J Clin Psychiatry 67:1354-61. 2006This study investigated the efficacy, safety, and tolerability of the selegiline transdermal system (STS) administered in a dose range of 6 mg/24 hours to 12 mg/24 hours for treating major depressive disorder (MDD).
Tyramine pressor sensitivity during treatment with the selegiline transdermal system 6 mg/24 h in healthy subjectsAlbert J Azzaro
Somerset Pharmaceuticals, Inc, Tampa, Florida, USA
J Clin Pharmacol 46:933-44. 2006The oral tyramine pressor test was administered to healthy males during treatment with a selegiline transdermal system (STS; 6 mg/24 h)...
Amphetamine-induced locomotor activity is reduced in mice following MPTP treatment but not following selegiline/MPTP treatmentBrian D West
Neuroscience Drug Discovery, Merck Research Laboratories, P.O. Box 4, WP44E-200, West Point, PA 19486, USA
Pharmacol Biochem Behav 84:158-61. 2006..Further, the potential for use of this endpoint to evaluate putative therapeutics is exemplified by the amelioration of these effects following pre-treatment with the MAO-B inhibitor selegiline.
Double-blind, placebo-controlled trial of selegiline transdermal system (STS) for the treatment of cocaine dependenceAhmed Elkashef
National Institute on Drug Abuse NIDA, Division of Pharmacotherapies and Medical Consequences of Drug Abuse DPMCDA, MSC 9551 Bethesda, MD 20892, USA
Drug Alcohol Depend 85:191-7. 2006..b>Selegiline is an irreversible selective inhibitor of monoamine oxidase type B (MAO-B) which may affect cocaine addiction ..
Selegiline slows the progression of the symptoms of Parkinson diseaseS Palhagen
Department of Neurology, Karolinska University Hospital Huddinge, SE 141 86 Stockholm, Sweden
Neurology 66:1200-6. 2006To study the long-term effects of selegiline in monotherapy and in combination with levodopa in the early phase of Parkinson disease (PD).
Clomipramine and selegiline: do they influence impulse control?B Bert
Institute of Pharmacology and Toxicology, School of Veterinary Medicine, Freie Universitat Berlin, Berlin, Germany
J Vet Pharmacol Ther 29:41-7. 2006..The reduction of these undesirable actions is the focus of behaviour therapy. Clomipramine and selegiline have been approved for the treatment of separation anxiety in dogs, but there are anecdotal reports that they ..
A comprehensive assessment of the safety of intravenous methamphetamine administration during treatment with selegilineThomas F Newton
Department of Psychiatry and Biobehavioral Sciences, David Geffen School of Medicine at the University of California at Los Angeles, USA
Pharmacol Biochem Behav 82:704-11. 2005b>Selegiline (L-deprenyl) is a selective irreversible monoamine oxidase B inhibitor shown to be effective in the treatment of Parkinson's and Alzheimer's diseases...
Antidepressant-like effects of selegiline in the forced swim testSeiichiro Shimazu
Research Institute, Fujimoto Pharmaceutical Corporation, 1 3 40 Nishiotsuka, Matsubara, Osaka 580 0011, Japan
Eur Neuropsychopharmacol 15:563-71. 2005Although selegiline, a monoamine oxidase (MAO)-B inhibitor, is reported to exert antidepressant effects in depressant patients, evidence in rodents for effects of selegiline is quite limited...
Effects of selegiline alone or with donepezil on memory impairment in ratsKazue Takahata
Research Institute, Fujimoto Pharmaceutical Corporation, 1-3-40 Nishiotsuka, Matsubara, Osaka 580-0011, Japan
Eur J Pharmacol 518:140-4. 2005b>Selegiline, a monoamine oxidase-B inhibitor, is reported to improve memory and learning in dementia of Alzheimer's type. However, only a few studies have reported its use in animal models...
A multicenter trial of selegiline transdermal system for HIV-associated cognitive impairmentG Schifitto
Department of Neurology, Movement and Inherited Neurologic Disorders, Clinical Trials Coordination Center, 1351 Mount Hope Avenue, Suite 223, Rochester, NY 14620, USA
Neurology 69:1314-21. 2007..b>Selegiline is an MAO-B inhibitor with antioxidant and neurotrophic properties...
Therapeutic factors causing hallucination in Parkinson's disease patients, especially those given selegilineKeiko Kamakura
Third Department of Internal Medicine, National Defense Medical College, 3-2 Namiki, Tokorozawa, Saitama 359-8513, Japan
Parkinsonism Relat Disord 10:235-42. 2004b>Selegiline protects nigral dopaminergic neurons and is recommended for the treatment of patients in the early stage of Parkinson's disease (PD)...
Comparative study of the effects of isatin, an endogenous MAO-inhibitor, and selegiline on bradykinesia and dopamine levels in a rat model of Parkinson's disease induced by the Japanese encephalitis virusN Hamaue
The Research Institute of Personalized Health Sciences, Health Sciences University of Hokkaido, 061-0293 Ishikari-Tobetsu, Japan
Neurotoxicology 25:205-13. 2004..b>Selegiline [(-)-deprenil] was developed as a MAO-B inhibitor more than 30 years ago and widely used in the treatment of ..
Comparative neuroprotective effects of rasagiline and aminoindan with selegiline on dexamethasone-induced brain cell apoptosisShawna Tazik
Division of Neurobiology and Behavioral Research, Department of Psychiatry and Human Behavior G 109, University of Mississippi Medical Center, 2500N State Street, Jackson, MS 39216, USA
Neurotox Res 15:284-90. 2009..In this study, we have compared the ability of rasagiline (Azilect) and its main metabolite, R-aminoindan with selegiline (Deprenyl) in prevention of dexamethasone-induced brain cell death employing human neuroblastoma SH-SY5Y cells ..
Impact of sustained deprenyl (selegiline) in levodopa-treated Parkinson's disease: a randomized placebo-controlled extension of the deprenyl and tocopherol antioxidative therapy of parkinsonism trialIra Shoulson
University of Rochester Medical Center, Rochester, NY 14620, USA
Ann Neurol 51:604-12. 2002Deprenyl (selegiline) delays the need for levodopa therapy in patients with early Parkinson's disease, but the long-term benefits of this treatment remain unclear...
Effects of selegiline on fronto-temporal dementia: a neuropsychological evaluationRita Moretti
Int J Geriatr Psychiatry 17:391-2. 2002
Clinical pharmacokinetics and pharmacodynamics of selegiline. An updateI Mahmood
Division of Pharmaceutical Evaluation I, Food and Drug Administration, Rockville, Maryland, USA
Clin Pharmacokinet 33:91-102. 1997b>Selegiline is a selective inhibitor of monoamine oxidase-B (MAO-B) at a dose of 10 mg/day and is given to patients with Parkinson's disease as an adjunct to levodopa therapy...
Long-term persistence of symptomatic effect of selegiline in Parkinson's disease. A two-months placebo-controlled withdrawal studyA Negrotti
Istituto di Neurologia, , Italy
J Neural Transm 108:215-9. 2001Following a two-months of placebo-controlled withdrawal, the MAO-B inhibitor selegiline was found to maintain a long term significant mild to moderate symptomatic effect on bradykinesia and tremor at rest in nine patients with Parkinson's ..
Selegiline in the treatment of Alzheimer's disease: a long-term randomized placebo-controlled trial. Czech and Slovak Senile Dementia of Alzheimer Type Study GroupV Filip
Department of Psychiatry, Comenius University, Bratislava, Slovak Republic
J Psychiatry Neurosci 24:234-43. 1999To evaluate the efficacy and adverse effects of the type B monoamine oxidase inhibitor selegiline (also known as I-deprenyl) in the treatment of Alzheimer's disease.
Selegiline completely restores choline acetyltransferase activity deficits in simian immunodeficiency infectionE Koutsilieri
Clinical Neurochemistry, Department of Psychiatry, University of Wurzburg, Fuchsleinstr 15, 97080, Wurzburg, Germany
Eur J Pharmacol 411:R1-R2. 2001..We report now that selegiline, completely restores the reduced choline acetyltransferase activity which encourages for a meaningful anti-..
The influence of metabolism on the MAO-B inhibitory potency of selegilineD Haberle
Department of Pharmacodynamics Semmelweis University, H 1445 Budapest, Hungary
Curr Med Chem 9:47-51. 2002Deprenyl (selegiline), a propargylamine derivative of methylamphetamine, is a potent, irreversible inhibitor of monoamine-oxidase type B (MAO-B). The MAO-B inhibitory effects of various doses (0.1-0.25-0...
The effect of selegiline in the treatment of people with Alzheimer's disease: a meta-analysis of published trialsG K Wilcock
Department of Care of the Elderly, University of Bristol, UK
Int J Geriatr Psychiatry 17:175-83. 2002To evaluate the effect of selegiline in the treatment of patients with Alzheimer's disease, in terms of cognitive performance, functional ability, emotional state (including behaviour and mood) and global response...
Chronic daily administration of selegiline and EGb 761 increases brain's resistance to ischemia in miceI Unal
Department of Neurology, Faculty of Medicine and Institute of Neurological Sciences and Psychiatry, Hacettepe University, 06100, Ankara, Turkey
Brain Res 917:174-81. 2001..Acute administration of selegiline and EGb 761 have been shown to have anti-apoptotic and neuroprotective effects in experimental ischemia...
Transdermal selegiline in HIV-associated cognitive impairment: pilot, placebo-controlled studyN Sacktor
Department of Neurology, Johns Hopkins University School of Medicine, Baltimore, MD 21224, USA
Neurology 54:233-5. 2000..a pilot randomized, double-blind, placebo-controlled clinical trial of the transdermal administration of selegiline in HIV+ patients to obtain preliminary data to assess its safety, tolerability, and impact on HIV-associated ..
CYP2B6 and CYP2C19 as the major enzymes responsible for the metabolism of selegiline, a drug used in the treatment of Parkinson's disease, as revealed from experiments with recombinant enzymesM Hidestrand
Division of Molecular Toxicology, Institute of Environmental Medicine, Karolinska Institutet, 171 77 Stockholm, Sweden
Drug Metab Dispos 29:1480-4. 2001In view of conflicting data in the literature regarding the enzyme(s) responsible for metabolism of selegiline, a drug used in the treatment of Parkinson's disease, investigations were carried out in vitro using the human cytochrome P450 ..
Selegiline metabolism and cytochrome P450 enzymes: in vitro study in human liver microsomesP Taavitsainen
Department of Pharmacology and Toxicology, University of Oulu, Finland
Pharmacol Toxicol 86:215-21. 2000Although being a drug therapeutically used for a long time, the enzymatic metabolism of selegiline has not been adequately studied...
Effects of a tyramine-enriched meal on blood pressure response in healthy male volunteers treated with selegiline transdermal system 6 mg/24 hourLawrence F Blob
Somerset Pharmaceuticals, Tampa, FL 33607, USA
CNS Spectr 12:25-34. 2007..A selegiline transdermal system (STS) was developed to provide antidepressant concentrations of selegiline in the brain, ..
Selegiline in narcolepsyS E Roselaar
University Department of Neurology, King's College School of Medicine, London, England
Sleep 10:491-5. 1987We examined the effect of the specific monoamine oxidase-B (MAO-B) inhibitor selegiline (deprenyl, Eldepryl), 20-30 mg p.o. daily, in 21 subjects with the narcoleptic syndrome for 4 weeks...
Toxicokinetic evaluation of a selegiline transdermal system in the dogJ S Barrett
Somerset Pharmaceuticals, Tampa, FL, USA
Biopharm Drug Dispos 18:165-84. 1997The toxicology and toxicokinetics of a selegiline transdermal system (STS) were evaluated in a 3 month dog study of daily 24 h applications of placebo 4, 8, or 12 STSs in 32 male and 32 female beagle dogs...
Selegiline's neuroprotective capacity revisitedP Riederer
Clinical Neurochemistry, Clinic and Policlinic for Psychiatry and Psychotherapy, University of Wuerzburg, Germany
J Neural Transm 110:1273-8. 2003
Reexamination of the TEMPO StudyClifford W Shults
Arch Neurol 62:1320; author reply 1321. 2005
[Molecular mechanisms of the neuroprotective effect of (-)-deprenyl]Melinda Pálfi
Magyar Tudományos Akadémia, Neurokémiai Kutatócsoport, Budapest
Orv Hetil 147:1251-7. 2006..Data are accumulating about the relationship of these enzymes and propargyl compounds, but the real significance of this issue will only be established by future research...
Neuroprotection of MPTP-induced toxicity in zebrafish dopaminergic neuronsEnid T McKinley
Zygogen, 520 Kell Hall, 24 Peachtree Center Avenue, Atlanta, GA 30303, USA
Brain Res Mol Brain Res 141:128-37. 2005..Effects on swimming behavior and touch response that result from MPTP damage are partially ameliorated by both l-deprenyl and DAT knockdown...
[Role of R-(-)-deprenyl in adhesion of neuronal and non-neuronal cells]Veronika Jenei
Magyar Tudományos Akadémia, Kémiai Kutatóközpont, Biomolekuláris Kémiai Intézet, Budapest
Orv Hetil 146:601-6. 2005..The authors' results with S-(+)-deprenyl suggest that the sterical structure of the drug is an important factor of the observed effect, which is probably a consequence of an irreversible change in the cells...
Clinical pharmacology of rasagiline: a novel, second-generation propargylamine for the treatment of Parkinson diseaseJack J Chen
Movement Disorders Center, Loma Linda University, Loma Linda, CA, USA
J Clin Pharmacol 45:878-94. 2005..Rasagiline completely and selectively inhibits MAO-B with a potency 5 to 10 times greater than selegiline. Unlike the prototype propargylamine selegiline, which is metabolized to amphetamine derivatives, rasagiline is ..
A novel formulation of selegiline for the treatment of Parkinson's diseaseJames W Tetrud
The Parkinson's Institute, 1170 Morse Avenue, Sunnyvale, CA 94089, USA
Neurology 63:S2-6. 2004
Clinical trials of neuroprotection for Parkinson's diseasePeter A LeWitt
Departments of Neurology, Psychiatry and Behavioral Neuroscience, Wayne State University School of Medicine, The William Beaumont Hospital Research Institute, Royal Oak, Michigan, USA
Neurology 63:S23-31. 2004
A review of the mechanisms and role of monoamine oxidase inhibitors in Parkinson's diseaseMoussa B H Youdim
Department of Pharmacology, Technion-Bruce Rappaport Faculty of Medicine, Eve Topf and NPF Neurodegenerative Diseases Centers, Rappaport Family Research Institute, Haifa, Israel
Neurology 63:S32-5. 2004
Other pharmacological treatments for motor complications and dyskinesiasCheryl Waters
Division of Movement Disorders, Department of Neurology, Columbia University, 710 West 168th Street, New York, NY 10032, USA
Mov Disord 20:S38-44. 2005..Patients may also suffer from dyskinesias. Dyskinesias can be treated with small doses of liquefied levodopa-carbidopa, amantadine, and clozapine, an atypical neuroleptic...
Indolalkylamines derivatives as antioxidant and neuroprotective agents in an experimental model of Parkinson's diseaseElisenda Sanz
Departament de Bioquimca i Biologia Molecular, Facultad de Medicina, Institut de Neurociencies, , Campus Universitari de Bellaterra, Barcelona, Spain
Med Sci Monit 10:BR477-84. 2004..The antioxidant properties of PF 9601 N would explain its neuroprotective effect observed in SHSY5Y cells lesioned with dopamine...
Evidence-based medical review update: pharmacological and surgical treatments of Parkinson's disease: 2001 to 2004Christopher G Goetz
Department of Neurological Sciences, Department of Pharmacology, Rush University Medical Center, Chicago, Illinois 60612, USA
Mov Disord 20:523-39. 2005..b>Selegiline was reassigned as Non-efficacious for the prevention of dyskinesias. Other designations did not change...
Inhibition of methamphetamine-induced hyperlocomotion in mice by clorgyline, a monoamine oxidase-a inhibitor, through alteration of the 5-hydroxytriptamine turnover in the striatumN Kitanaka
Department of Pharmacology, Hyogo College of Medicine, 1-1 Mukogawa-cho, Nishinomiya, Hyogo 663-8501, Japan
Neuroscience 130:295-308. 2005..5-2 mg/kg (i.p.). In contrast, single or repeated pretreatment of selegiline (0.3 mg/kg, s.c.), a MAO-B inhibitor, had no effect on METH-induced hyperlocomotion...
Neural mechanisms underlying motor dysfunction as detected by the tail suspension test in MPTP-treated C57BL/6 miceAtsushi Mori
Research Unit for Neurological Diseases, Second Institute of New Drug Discovery, Otsuka Pharmaceutical Co, Ltd, Tokushima-city, Tokushima 771-0192, Japan
Neurosci Res 51:265-74. 2005..We concluded that the increase in immobility time in the TST was induced by the nigrostriatal dopaminergic degeneration and was thought to be a consequence of motor dysfunction in this mouse model of PD...
[Neuroprotective and neurorestorative therapy in Parkinson's disease]F J Jimenez-Jimenez
Departamento de Neurologia, Hospital Universitario Principe de Asturias, Alcalúa de Henares, Madrid, Espana
Rev Neurol 25:S185-93. 1997..This article reviews the current knowledge on the possible neuroprotective and restorative treatments in Parkinson's disease...
Recent advances in Parkinson's disease therapy: use of monoamine oxidase inhibitorsClaire Henchcliffe
Weill Medical College of Cornell University, Department of Neurology and Neuroscience, 428 East 72, Street, Suite 400, NY 10021, USA
Expert Rev Neurother 5:811-21. 2005..b>Selegiline is currently the most widely used monoamine oxidase-B inhibitor for Parkinson's disease, but has a low and ..
Effect of MAO-B inhibition against ischemia-induced oxidative stress in the rat brain. Comparison with a rational antioxidantMona Seif-el-Nasr
Department of Pharmacology, Faculty of Pharmacy, Cairo University, Cairo, Egypt
Arzneimittelforschung 58:160-7. 2008....
Rat striatal monoamine oxidase-B inhibition by l-deprenyl and rasagiline: its relationship to 2-phenylethylamine-induced stereotypy and Parkinson's diseaseM B H Youdim
Department of Pharmacology, Technion Faculty of Medicine, Eve Topf and US National Parkinson Foundation Centers for Neurodegenerative Diseases, The B Rappaport Family Medical Research Institute, 31096 Haifa, Israel
Parkinsonism Relat Disord 8:247-53. 2002Rats were injected intraperitoneally with varying doses of l-deprenyl (selegiline) followed 2h later by 30 mg kg(-1) 2-phenylethylamine (PEA), administered in the same way, and the stereotypic behavioural response elicited was assessed...
Selegiline reduces cisplatin-induced neuronal death in neuroblastoma cellsThomas Muller
Department of Neurology, St Josef Hospital, University of Bochum, Gudrunstr 56, 44791 Bochum, Germany
Neurol Res 30:417-9. 2008Long-term administration of the monoamine oxidase (MAO)-B inhibitor selegiline may reduce neuronal death based on preclinical findings and reduce progression of chronic neurodegeneration due to outcomes of long-term clinical trials in ..
Monoamine oxidase-B inhibition in the treatment of Parkinson's diseaseHubert H Fernandez
Movement Disorders Center, University of Florida, McKnight Brain Institute, Gainesville, FL 32610, USA
Pharmacotherapy 27:174S-185S. 2007..The two available MAO-B inhibitors approved for use in the United States, rasagiline and selegiline, each provide symptomatic relief as monotherapy and as adjunctive therapy, and have shown potential disease-..
Comprehensive review of rasagiline, a second-generation monoamine oxidase inhibitor, for the treatment of Parkinson's diseaseJack J Chen
Department of Pharmacotherapy and Outcomes Science, School of Pharmacy, Loma Linda University, Loma Linda, California 92350, USA
Clin Ther 29:1825-49. 2007..Rasagiline [N-propargyl-l(R)-aminoindan] is a second-generation propargylamine pharmacophore that selectively and irreversibly inhibits brain MAO-B and is specifically designed for the treatment of Parkinson's disease (PD)...
In vitro metabolism of the analgesic bicifadine in the mouse, rat, monkey, and humanDavid A Erickson
Department of Drug Metabolism, Covance Laboratories Inc, Madison, WI, USA
Drug Metab Dispos 35:2232-41. 2007..inhibited in human hepatic microsomes and mitochondria by the monoamine oxidase (MAO)-B-specific inhibitor selegiline. Clorgyline, a specific inhibitor of MAO-A, was less effective in inhibiting M12 formation...
Amine oxidases and their inhibitors: what can they tell us about neuroprotection and the development of drugs for neuropsychiatric disorders?Glen B Baker
J Psychiatry Neurosci 32:313-5. 2007
Rasagiline as a therapy for Parkinson's disease (PD)Neal Hermanowicz
Am J Geriatr Pharmacother 5:174-5; author reply 175-6. 2007
Community and long-term care management of Parkinson's disease in the elderly: focus on monoamine oxidase type B inhibitorsJack J Chen
Movement Disorders Center, Schools of Medicine and Pharmacy, Loma Linda University, Loma Linda, California 92350, USA
Drugs Aging 24:663-80. 2007..Monoamine oxidase type B (MAO-B) inhibitors can be used across the spectrum of disease severity, but selegiline (deprenyl), the prototype in this class, is characterised by low and erratic bioavailability of the parent drug ..
Monamine oxidase inhibitors: current and emerging agents for Parkinson diseaseHubert H Fernandez
Movement Disorders Center, Department of Neurology, McKnight Brain Institute University of Florida, Gainesville, FL 32610, USA
Clin Neuropharmacol 30:150-68. 2007..Data have been reported regarding the selective MAO-B inhibitors, rasagiline and selegiline, for the symptomatic treatment of Parkinson disease (PD)...
Antioxidant effects of selegiline in oxidative stress induced by iron neonatal treatment in ratsPatricia Budni
Laboratório de Fisiopatologia Experimental, Universidade do Extremo Sul Catarinense, Criciuma, Brazil
Neurochem Res 32:965-72. 2007..The aim of the present study was to evaluate the possible protective effect of selegiline, a monoamino-oxidase B (MAO-B) inhibitor used in pharmacotherapy of Parkinson's disease, against iron-induced ..
Monoamine oxidase inhibitory coumarins from the aerial parts of Dictamnus albusSeon Hwa Jeong
College of Pharmacy, Chungbuk National University, Cheongju 361 763, Korea
Arch Pharm Res 29:1119-24. 2006..5 and 0.6 microM, respectively) compared to MAO-A (IC50 1.3 and 34.6 microM, respectively). According to kinetic analyses derived by Lineweaver-Burk reciprocal plots, compounds 1 and 2 exhibited a competitive inhibition to MAO-B...
Effects of subchronic treatment with selegiline on L-DOPA-induced increase in extracellular dopamine level in rat striatumKouichi Adachi
Department of Neurology, Wakayama Medical University, Wakayama, Japan
J Pharmacol Sci 101:286-92. 2006b>Selegiline is used an adjunct to L-DOPA therapy. We investigated extracellular striatal dopamine (DA) level in awake rats treated with L-DOPA and/or selegiline using a microdialysis method. Rats given 10 mg/kg, i.p...
(-)-Trans-epsilon-viniferin, a polyphenol present in wines, is an inhibitor of noradrenaline and 5-hydroxytryptamine uptake and of monoamine oxidase activityMatilde Yáñez
Departamento de Farmacologia, Facultad de Farmacia, Universidad de Santiago de Compostela, Campus Universitario Sur, E 15782 Santiago de Compostela La Coruña, Spain
Eur J Pharmacol 542:54-60. 2006....
High-throughput screening for monoamine oxidase-A and monoamine oxidase-B inhibitors using one-step fluorescence assayHong-mei Guang
Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China
Acta Pharmacol Sin 27:760-6. 2006..71+/-0.03 and 0.75+/-0.03 in MAO-A-inhibitor and MAO-B-inhibitor HTS system, respectively. CONCLUSION: The established assays can be well applied to MAO-A and MAO-B inhibitor screening with high quality, precision and reproducibility...
Monoamine oxidase: isoforms and inhibitors in Parkinson's disease and depressive illnessMoussa B H Youdim
Department of Pharmacology and Technion Bruce Rappaport Faculty of Medicine, Eve Topf and NPF Centers of Excellence for Neurodegenerative Diseases Research and Teaching, Haifa, Israel
Br J Pharmacol 147:S287-96. 2006..These aspects of MAO and its inhibition and some indication of how this important area of pharmacology and therapeutics might develop in the future are summarized in this review...
[A comparison of the pharmacology of (-)-deprenyl to N-methylpropargylamine-1-aminoindane (J-508) and rasagiline, the desmethyl-analogue of J-508]Ildiko Miklya
Semmelweis Egyetem, AOK, Farmakológiai és Farmakoterápiás Intézet, Budapest
Neuropsychopharmacol Hung 10:15-22. 2008..Thus, rasagiline can not be a substitute for (-)-deprenyl in therapy...
Preclinical evidence for neuroprotection with monoamine oxidase-B inhibitors in Parkinson's diseasePeter Jenner
Neurodegenerative Diseases Research Centre, Guy's, King's and St Thomas' School of Biomedical Sciences, King's College, London, United Kingdom
Neurology 63:S13-22. 2004
[Parkinson's disease]K Miyoshi
Hyogo Institute for Aging Brain and Cognitive Disorders
Nippon Rinsho 59:1570-3. 2001..Serotonin reuptake inhibitors and selegiline are recommended for the treatment of depression in parkinsonian patients.
Research Grants
- CARDIOVASCULAR DISEASE PREVENTION TRAINING PROGRAMStephen Fortmann; Fiscal Year: 2007..and improving quality of life in persons over 65, behavioral maintenance treatment in smoking cessation, selegiline for smoking cessation, retail tobacco marketing effects on adolescent smoking initiation, pro- and anti-smoking ..
- RADIOTRACER RANDD IN NUCLEAR MEDICINE AND NEUROSCIENCESJoanna Fowler; Fiscal Year: 2000....
- PARKINSON DISEASE NEUROPROTECTION CLINICAL TRIAL CENTERBala Manyam; Fiscal Year: 2005..disease, not yet requiring symptomatic treatment and unexposed to prior treatment with levodopa/dopamine agonist/selegiline (within four months). 3)...
- Selegiline for Smoking CessationMARC POTENZA; Fiscal Year: 2007..In support of this hypothesis, in preliminary studies, we have shown that the selective MAO-B inhibitor selegiline hydrochloride (10 mg/day) significantly increases smoking abstinence rates compared to placebo...
- Selegiline for Smoking CessationTony George; Fiscal Year: 2006..In support of this hypothesis, in preliminary studies, we have shown that the selective MAO-B inhibitor selegiline hydrochloride (10 mg/day) significantly increases smoking abstinence rates compared to placebo...
- Selegiline for Treatment of Cannabis DependenceBRENT MOORE; Fiscal Year: 2005..b>Selegiline, a monoamine oxidase-B inhibitor, increases dopamine activity in mesolimbic and other brain regions involved in ..
- NEUROLOGIC AIDS RESEARCH CONSORTIUMDavid Clifford; Fiscal Year: 2007..Complete and analyze A5090 testing the safety and efficacy of transdermal selegiline for HIV- associated motor cognitive disorder; 2...
- Parkinson's Disease Neuroprotection Clinical Trial: Clinical CenterBurton Scott; Fiscal Year: 2007..At this time, only selegiline (Eldrepyl), a selective monoamine oxidase-B (MAO-B) inhibitor has been approved by the US Food & Drug ..
- Norepinephrine and Nerve Growth Factor in Heart FailureChang Seng Liang; Fiscal Year: 2004..Superoxide dismutase and selegiline, which have been shown to prevent cardiac sympathetic nerve abnormalities in heart failure, will be used to ..
- Selegiline Patch for Treatment of Nicotine DependenceJoel Killen; Fiscal Year: 2007..Primary aim: To conduct the first randomized controlled trial of the efficacy of selegiline patch (STS) for the treatment of nicotine dependence...
