Selegilin
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| (IUPAC) ime | |||
|---|---|---|---|
| (R)-N-metil-N-(1-fenilpropan-2-il)prop-1-in-3-amin | |||
| Klinički podaci | |||
| Robne marke | Eldepryl | ||
| AHFS/Drugs.com | Monografija | ||
| MedlinePlus | a697046 | ||
| Identifikatori | |||
| CAS broj | 14611-51-9 [14611-52-0] (HCl) | ||
| ATC kod | N04BD01 QN06 | ||
| PubChem[1][2] | 26757 | ||
| DrugBank | DB01037 | ||
| ChemSpider[3] | 24930 | ||
| UNII | 2K1V7GP655 
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| KEGG[4] | D03731
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| ChEBI | CHEBI:9086
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| ChEMBL[5] | CHEMBL972
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| Hemijski podaci | |||
| Formula | C13H17N | ||
| Mol. masa | 187,281 g/mol | ||
| SMILES | eMolekuli & PubHem | ||
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| Farmakokinetički podaci | |||
| Bioraspoloživost | 4,4% (oralno, na prazan stomak), 20% (oralno, nakon jela), 18% (flaster) | ||
| Vezivanje za proteine plazme | 90% | ||
| Metabolizam | jetra | ||
| Poluvreme eliminacije | 1,5 sata (oralno, jedna doza), 9 sata (oralno, hronično) | ||
| Izlučivanje | urin | ||
| Farmakoinformacioni podaci | |||
| Trudnoća | ? | ||
| Pravni status | samo na recepat (SAD) | ||
| Način primene | Oralno, transdermalno, bukalno | ||
Selegilin (Anipril, L-deprenil, Eldepril, Emsam, Zelapar. Jumex) je lek koji se koristio za tretman ranih stupnjeva Parkinsonove bolesti, depresije i senilne demencije. Pri normalnim kliničkim dozama on je selektivni ireverzibilni MAO-B inhibitor. Međutim, u većim dozama on gubi svoju specifičnost i takođe je inhibir MAO-A. Dijetarne restrikcije su uobičajene za MAOI tretmane, ali je utvrđeno da one nisu neophodne pri primeni niskih doza.[6] Isto i važi i za standarne doze kad se lek primenjuje putem transdermalnog flastera.[7] Selegilin pripada klasi lekova koji se nazivaju fenetilamini. Selegilin je metamfetaminski derivat sa propargilnom grupom vezanom za atom azota.
Hemija[uredi - уреди | uredi kôd]
Selegilin, N-metil-N-(2-propinil)-2-metil-1-feniletil-2-amin, se sintetiše putem alkilacije (–)-metamfetamina koristeći propargil bromid.[8][9][10][11]
Reference[uredi - уреди | uredi kôd]
- ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. http://www.sciencedirect.com/science/article/pii/S1359644610007737.
- ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
- ↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. http://www.jcheminf.com/content/2/1/3.
- ↑ Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H. http://onlinelibrary.wiley.com/doi/10.1002/%28SICI%291097-0061%28200004%2917:1%3C48::AID-YEA2%3E3.0.CO;2-H/full.
- ↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.
- ↑ Amsterdam, J. D. (2003). „A double-blind, placebo-controlled trial of the safety and efficacy of selegiline transdermal system without dietary restrictions in patients with major depressive disorder”. Journal of Clinical Psychiatry 64 (2): 208–14. DOI:10.4088/JCP.v64n0216. PMID 12633131.
- ↑ Cascade EF, Kalali AH (June 2007). „EMSAM: The First Year”. Psychiatry 2007. http://www.psychiatrymmc.com/emsam-the-first-year/. Pristupljeno 2009-11-30.
- ↑ J. Knoll, E. Sanfai, DE 1568277 (1966).
- ↑ J. Hermann Nee Voeroes, Z. Ecsery, G. Sabo, L. Arvai, L. Nagi, O. Orban, E. Sanfai, 4564706 SAD patent 4564706 (1986)
- ↑ B. Brunova, M. Ferenc, EP 344675 (1989)
- ↑ Fowler, Joanna S. (1977). „2-Methyl-3-butyn-2-ol as an acetylene precursor in the Mannich reaction. A new synthesis of suicide inactivators of monoamine oxidase”. The Journal of Organic Chemistry 42 (15): 2637–7. DOI:10.1021/jo00435a026. PMID 874623.
Literatura[uredi - уреди | uredi kôd]
- Nicholas C. Price, Lewis Stevens (1999). Fundamentals of Enzymology: The Cell and Molecular Biology of Catalytic Proteins (Third izd.). USA: Oxford University Press. ISBN 019850229X. http://books.google.com/books/about/Fundamentals_of_enzymology.html?id=8uvwAAAAMAAJ.
- Eric J. Toone (2006). Advances in Enzymology and Related Areas of Molecular Biology, Protein Evolution (Volume 75 izd.). Wiley-Interscience. ISBN 0471205036. http://books.google.com/books/about/Advances_in_Enzymology_and_Related_Areas.html?id=Pmh8yToeuloC.
- Branden C, Tooze J.. Introduction to Protein Structure. New York, NY: Garland Publishing. ISBN: 0-8153-2305-0. http://www.garlandscience.com/textbooks/0815323042.asp?type=reviews.
- Irwin H. Segel. Enzyme Kinetics: Behavior and Analysis of Rapid Equilibrium and Steady-State Enzyme Systems (Book 44 izd.). Wiley Classics Library. ISBN 0471303097. http://books.google.com/books/about/Enzyme_Kinetics.html?id=T60oAAAAYAAJ.
- Robert A. Copeland (2013). Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide for Medicinal Chemists and Pharmacologists (2nd izd.). Wiley-Interscience. ISBN 111848813X. http://books.google.com/books/about/Evaluation_of_Enzyme_Inhibitors_in_Drug.html?id=l2rMy8QNUk0C.
- Gerhard Michal, Dietmar Schomburg (2012). Biochemical Pathways: An Atlas of Biochemistry and Molecular Biology (2nd izd.). Wiley. ISBN 0470146842. http://books.google.com/books/about/Biochemical_pathways.html?id=081qAAAAMAAJ.
Vidi još[uredi - уреди | uredi kôd]
Spoljašnje veze[uredi - уреди | uredi kôd]
- Deprenyl (Selegiline) Can Slow Parkinson's Disease Safely According to the British Medical Journal
- FDA Approves Emsam (Selegiline) as First Drug Patch for Depression
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