selegiline / Generic mfg. 
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  • ||||||||||  selegiline / Generic mfg., rasagiline / Generic mfg.
    Review, Journal, IO biomarker:  Rasagiline and selegiline modulate mitochondrial homeostasis, intervene apoptosis system and mitigate α-synuclein cytotoxicity in disease-modifying therapy for Parkinson's disease. (Pubmed Central) -  Mar 27, 2021   
    Selegiline and rasagiline, inhibitors of type B monoamine oxidase, have been proved to exhibit potent neuroprotective function: regulation of mitochondrial apoptosis system, maintenance of mitochondrial function, increased expression of genes coding antioxidant enzymes, anti-apoptotic Bcl-2 and pro-survival NTFs, and suppression of oligomerization and aggregation of α-synuclein and the toxicity in cellular and animal experiments. However, the present available pharmacological therapy starts too late to reverse disease progression, and future disease-modifying therapy should include also non-pharmacological complementary therapy during the prodromal stage.
  • ||||||||||  selegiline / Generic mfg.
    Preclinical, Journal:  Blocking Astrocytic GABA Restores Synaptic Plasticity in Prefrontal Cortex of Rat Model of Depression. (Pubmed Central) -  Mar 6, 2021   
    The tonic inhibition can be reduced by either blocking astrocytic intracellular Ca signaling or by reducing astrocytic GABA through inhibition of the synthesizing enzyme MAO-B with Selegiline. Blocking GABA synthesis also restores the impaired synaptic plasticity in the FSL prefrontal cortex, providing a new antidepressant mechanism of Selegiline.
  • ||||||||||  Trivastal (piribedil) / Servier
    Clinical, Journal:  Pathological gambling in a patient on piribedil: A case report. (Pubmed Central) -  Feb 24, 2021   
    This case further emphasizes the importance of monitoring and controlling Parkinson symptoms after drug reduction or withdrawal. Anticipation of this risk strengthens the significance of detailed medical history-taking and targeted clinical management.
  • ||||||||||  methamphetamine / Generic mfg., selegiline / Generic mfg.
    Journal:  Detection of l-Methamphetamine and l-Amphetamine as Selegiline Metabolites. (Pubmed Central) -  Feb 12, 2021   
    Consistent with previous studies, our results indicated that the ratio of amphetamine to methamphetamine was 0.27, which was in the range of selegiline ingestion. Furthermore, we confirmed l-methamphetamine and l-amphetamine by chiral derivatization using (R)-(-)-α-methoxy-α-(trifluoromethyl) phenylacetyl chloride.
  • ||||||||||  selegiline / Generic mfg.
    Preclinical, Journal:  Effect of Combined Electroacupuncture and Selegiline Treatment in Alzheimer's Disease: An Animal Model. (Pubmed Central) -  Dec 29, 2020   
    In addition, mice treated with a combination of SEL and EA did not demonstrate a direct modulation of insoluble Aβ but demonstrated greater glucose metabolism. Our findings demonstrated that SEL combined with EA treatment was associated with better cognitive functioning due to inhibition of neuroinflammation and increased glucose metabolism relative to the comparative groups in a mouse model with AD.
  • ||||||||||  Journal:  Theacrine, a purine alkaloid from kucha, protects against Parkinson's disease through SIRT3 activation. (Pubmed Central) -  Dec 20, 2020   
    Our findings demonstrated that SEL combined with EA treatment was associated with better cognitive functioning due to inhibition of neuroinflammation and increased glucose metabolism relative to the comparative groups in a mouse model with AD. Theacrine prevents apoptosis of dopaminergic neurons through directly activating SIRT3 which deacetylating SOD2 and restoring mitochondrial functions.
  • ||||||||||  selegiline / Generic mfg.
    Preclinical, Journal:  Protective effect of selegiline on cigarette smoke-induced oxidative stress and inflammation in rat lungs in vivo. (Pubmed Central) -  Dec 17, 2020   
    Selegiline attenuated CS-induced elevation of pro-inflammatory mediators (CINC-1, MCP-1 and IL-6) and restored CS-induced reduction of anti-inflammatory mediator IL-10 in BAL, which was driven through MAPK and NF-κB. Inhibition of MAO-B may provide a promising therapeutic strategy for CS-mediated oxidative stress and inflammation in acute CS-exposed rat lungs.
  • ||||||||||  [VIRTUAL] Levodopa Dose Equivalency for Opicapone and Safinamide () -  Sep 20, 2020 - Abstract #MDSCongress2020MDS Congress_1073;    
    After comparison with other COMTi, tolcapone and entacapone, the conversion factor for opicapone 50 mg should be “levodopa dose x 0,4 LED”.In the two RCT of safinamide the combine improvement in ON time without troublesome dyskinesias was 0,63 h, placebo time discounted. The LED proposed for opicapone 50 mg is “total levodopa dose x 0,4 mg LED” and for safinamide 50 or 100 mg is “100 mg LED”.
  • ||||||||||  selegiline / Generic mfg.
    Journal:  Biopharmaceutical Potential of Selegiline Loaded Chitosan Nanoparticles in the Management of Parkinson's Disease. (Pubmed Central) -  Aug 31, 2020   
    Significant decrease in lipid peroxidation and nitrite concentration; increase in reduced glutathione and catalase enzyme levels were obtained due to antioxidant characteristics of SH, which turned to be useful to treat Parkinson's disease. Selegiline loaded chitosan nanoparticles form an effective non-invasive drug delivery systemof direct nose to brain targeting in Parkinson's disease.
  • ||||||||||  selegiline / Generic mfg., rasagiline / Generic mfg.
    Journal:  Computational Insight into the Mechanism of the Irreversible Inhibition of Monoamine Oxidase Enzymes by the Antiparkinsonian Propargylamine Inhibitors Rasagiline and Selegiline. (Pubmed Central) -  Aug 8, 2020   
    The calculated Δ G energies confirm SEL binds better due to its bigger size and flexibility allowing it to optimize hydrophobic C-H···π and π···π interactions with residues throughout both of enzyme's cavities, particularly with FAD, Gln206 and four active site tyrosines, thus overcoming a larger ability of RAS to form hydrogen bonds that only position it in less reactive orientations for the hydride abstraction. Offered results elucidate structural determinants affecting the affinity and rates of the inhibition reaction that should be considered to cooperate when designing more effective compounds devoid of untoward effects, which are of utmost significance and urgency with the growing prevalence of brain diseases.
  • ||||||||||  rivastigmine / Generic mfg., quetiapine / Generic mfg.
    [VIRTUAL] Prolonged Therapy of Dementia with Lewy Bodies with Quaternary Ammonium Anti-Muscarinic/High-Dose Cholinesterase Inhibitor (QAAM/HDCI) () -  Aug 2, 2020 - Abstract #AAIC2020AAIC_3342;    
    The results show that prolonged symptomatic, cognitive and functional improvement of dementia with Lewy Bodies is possible with the high-level inhibition of central nervous system cholinesterase achievable when rivastigmine is combined with glycopyrrolate. The discussion correlates these observations with current experimental, clinical and epidemiological evidence regarding the mechanism and treatment of this, and other, neurodegenerative diseases.
  • ||||||||||  Journal:  Drugs for Depression. (Pubmed Central) -  May 13, 2020   
    Phosphodiesterase inhibitors may prevent and treat AD. No abstract available
  • ||||||||||  selegiline / Generic mfg.
    Journal:  Newly developed reversible MAO-B inhibitor circumvents the shortcomings of irreversible inhibitors in Alzheimer's disease. (Pubmed Central) -  Apr 29, 2020   
    Although short-term treatment with irreversible MAO-B inhibitors, such as selegiline, improves cognitive deficits in AD patients, long-term treatments have shown disappointing results...We have developed a potent, highly selective, and reversible MAO-B inhibitor, KDS2010 (IC = 7.6 nM; 12,500-fold selectivity over MAO-A), which overcomes the disadvantages of the irreversible MAO-B inhibitor. Long-term treatment with KDS2010 does not induce compensatory mechanisms, thereby significantly attenuating increased astrocytic GABA levels and astrogliosis, enhancing synaptic transmission, and rescuing learning and memory impairments in APP/PS1 mice.
  • ||||||||||  pramipexole IR / Generic mfg., selegiline / Generic mfg.
    Clinical, Journal, Combination therapy:  Pramipexole and Selegiline Combination Therapy in a Case of Treatment-Resistant Depression. (Pubmed Central) -  Apr 22, 2020   
    Long-term treatment with KDS2010 does not induce compensatory mechanisms, thereby significantly attenuating increased astrocytic GABA levels and astrogliosis, enhancing synaptic transmission, and rescuing learning and memory impairments in APP/PS1 mice. No abstract available
  • ||||||||||  Xadago (safinamide) / Zambon, US WorldMeds, Meiji Seika, Valeo Pharma, Eisai, selegiline / Generic mfg.
    Journal:  Design, synthesis and biological evaluation of novel human monoamine oxidase B inhibitors based on a fragment in an X-ray crystal structure. (Pubmed Central) -  Mar 12, 2020   
    Among them, compound A3 demonstrated very high potency and isoform selectivity against hMAO-B, 11 and 13 times more potent (IC = 3 nM) and 23.64 and 6.8 times more selective than the marked drugs, selegiline and safinamide. However, the endeavors to modify the polar 3-one group of isatin, that is in a hydrophobic environment in the binding site of hMAO-B, to small nonpolar hydrophobic groups did not bring about improved hMAO-B inhibitors, which may challenge our understanding of molecular interactions and molecular recognition in biological systems.
  • ||||||||||  selegiline / Generic mfg.
    Journal:  Discovery of novel 2,3-dihydro-1H-inden-1-amine derivatives as selective monoamine oxidase B inhibitors. (Pubmed Central) -  Feb 24, 2020   
    Compounds L4 (IC = 0.11 μM), L8 (IC = 0.18 μM), L16 (IC = 0.27 μM) and L17 (IC = 0.48 μM) showed similar MAO-B inhibitory activity as Selegiline. Moreover, L4, L16 and L17 also exhibited comparable selectivity with Selegiline, indicating that L4, L16 and L17 could be promising selective MAO-B inhibitors for further study.
  • ||||||||||  rasagiline / Generic mfg.
    Journal:  Different generations of type-B monoamine oxidase inhibitors in Parkinson's disease: from bench to bedside. (Pubmed Central) -  Feb 22, 2020   
    Three inhibitors of type-B monoamine oxidase (MAOB), selegiline, rasagiline, and safinamide, are used for the treatment of Parkinson's disease (PD)...Safinamide is the prototype of a new generation of multi-active MAOB inhibitors, which includes the antiepileptic drug, zonisamide...Among all antiparkinsonian agents, MAOB inhibitors are those with the greatest neuroprotective potential because of inhibition of dopamine metabolism, induction of neurotrophic factors, and, in the case of safinamide, inhibition of glutamate release. The recent development of new experimental animal models that more closely mimic the progressive neurodegeneration associated with PD will allow to test the hypothesis that MAOB inhibitors may slow the progression of PD.
  • ||||||||||  selegiline / Generic mfg.
    Journal, Monotherapy:  Long-Term Selegiline Monotherapy for the Treatment of Early Parkinson Disease. (Pubmed Central) -  Feb 22, 2020   
    The recent development of new experimental animal models that more closely mimic the progressive neurodegeneration associated with PD will allow to test the hypothesis that MAOB inhibitors may slow the progression of PD. Long-term monotherapy with selegiline (10 mg/d) was effective and well tolerated in patients with early PD in this 56-week study.
  • ||||||||||  topiramate / Generic mfg., selegiline / Generic mfg.
    Journal:  A Proteotranscriptomic-Based Computational Drug-Repositioning Method for Alzheimer's Disease. (Pubmed Central) -  Feb 19, 2020   
    Of these, four drugs classified into the nervous system group of Anatomical Therapeutic Chemical (ATC) system are voltage-gated sodium channel blockers (bupivacaine, topiramate) and monamine oxidase inhibitors (selegiline, iproniazid), and their mechanism of action was inferred from a potential anti-AD drug perspective. Our approach suggests a shortcut to discover new efficacy of drugs for AD.
  • ||||||||||  selegiline / Generic mfg.
    Journal:  Adjuvant potential of selegiline in treating acute toxicity of aluminium phosphide in rats. (Pubmed Central) -  Jan 17, 2020   
    In conclusion, selegiline treatment can ameliorate the AlP-induced cardiac and gastrointestinal injuries in rats via boosting redox status and mitochondrial function with no significant effect on survival. We suggest that using selegiline, apart from other clinical treatments, may improve the quality of treatment process for AlP toxicity.