The response to selegiline was assessed in ten (2 females, 8 males) idiopathic parkinsonian patients with the wearing off response. Selegiline was compared to placebo in each patient in a double blind crossover study carried out over ten months. After 16 weeks of therapy selegiline significantly prolonged response to levodopa, extending response to 3 hours (p less than 0.05) in most patients and to 4 hours (p less than 0.001) in some patients. Baseline scores (zero time: 12 hours after their previous dose of medication) were also significantly better after selegiline therapy (p less than 0.05). Selegiline did not improve peak response (1 hour after medication) to levodopa indicating that these patients were on optimum therapy prior to receiving selegiline. Adverse effects (nausea (2), dyskinesia (2), fear reaction (1) and postural dizziness (1] occurred in 5 patients during the trial.
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http://dx.doi.org/10.1111/j.1600-0404.1989.tb01791.x | DOI Listing |
J Med Chem
January 2025
Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.
Monoamine oxidase-B (MAO-B), predominantly exists on the outer mitochondrial membrane of astrocytes, serves as a crucial biomarker for reactive astrocytes during neuroinflammatory responses and various neurodegenerative diseases. In this study, we synthesized a series of fluorinated coumarin derivatives and evaluated their structure-activity relationship and subtype selectivity for MAO-B. Following this, the preclinical bioevaluation containing positron emission tomography (PET) imaging and autoradiography studies led to the identification of the novel PET tracer, [F], which demonstrated high affinity for MAO-B (IC = 0.
View Article and Find Full Text PDFMolecules
September 2024
Department Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University of Sofia, 1000 Sofia, Bulgaria.
Neurodegenerative diseases such as Parkinson's and Alzheimer's continue to be some of the most significant challenges in modern medicine. Recent research related to the molecular mechanisms of parkinsonism has opened up new approaches to antiparkinsonian therapy. In response to this, we present the evaluation of the potential neuroprotective and MAOA/MAOB inhibitory effects of newly synthesized hydrazones, containing a pyrrole moiety in the carboxyl fragment of the structure.
View Article and Find Full Text PDFChem Biol Drug Des
September 2024
Division of Pharmacology, Institute of Pharmaceutical Research, GLA University, Mathura, India.
Parkinson's disease (PD) stands as the second most common neurological disorder after Alzheimer's disease, primarily affecting the elderly population and significantly compromising their quality of life. The precise etiology of PD remains elusive, but recent research has shed light on potential factors, including the formation of α-synuclein aggregates, oxidative stress, neurotransmitter imbalances, and dopaminergic neurodegeneration in the substantia nigra pars compacta (SNpc) region of the brain, culminating in motor symptoms such as bradykinesia, akinesia, tremors, and rigidity. Monoamine oxidase (MAO) is an essential enzyme, comprising two isoforms, MAO-A and MAO-B, responsible for the oxidation of monoamines such as dopamine.
View Article and Find Full Text PDFEur J Clin Nutr
March 2024
Department of Surgery, Brigham and Women's Hospital, Boston, MA, USA.
Monoamine oxidase inhibitors (MAOIs) prevent the breakdown of tyramine in the body, and can cause a sudden increase in blood pressure with significant tyramine build up. This phenomenon, when it occurs, is known as tyramine pressor response. It is unknown if tyrosine administered in parenteral nutrition (PN) leads to tyramine build-up with concomitant use of MAOIs.
View Article and Find Full Text PDFInt J Mol Sci
August 2023
Department of Pharmacology and Pharmacotherapy, Semmelweis University, Nagyvarad ter 4, 1089 Budapest, Hungary.
Selegiline and rasagiline are two selective monoamine oxidase B (MAO-B) inhibitors used in the treatment of Parkinson's disease. In their clinical application, however, differences in L-dopa-sparing potencies have been observed. The aim of this study was to find neurochemical and behavioral explanations for the antiparkinsonian effects of these drugs.
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