Rasagilin

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Rasagilin
(IUPAC) ime
(R)-N-(prop-2-inil)-2,3-dihidro-1H-inden-1-amin
Klinički podaci
Robne marke Azilect
AHFS/Drugs.com Monografija
MedlinePlus a606017
Identifikatori
CAS broj 1875-50-9
ATC kod N04BD02
PubChem[1][2] 3052776
DrugBank DB01367
ChemSpider[3] 2314553
UNII 003N66TS6T YesY
KEGG[4] D02562 YesY
ChEMBL[5] CHEMBL887 YesY
Hemijski podaci
Formula C12H13N 
Mol. masa 171,238 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Bioraspoloživost 36%
Vezivanje za proteine plazme 88 – 94%
Metabolizam Hepatički (CYP1A2 posredovano)
Poluvreme eliminacije 3 sata
Izlučivanje Renalno i fekalno
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status Prescription only
Način primene Oralno

Rasagilin (Azilect, AGN 1135) je ireverzibilni inhibitor monoaminske oksidaze[6] koji se koristi kao monoterapija za ranu Parkinsonovu bolest, ili kao pomoćna terapija u odmaklim slučajevima.[7] On je više od jednog reda veličine selektivan za MAO tip B u odnosu na tip A.[8]

Inicijalna istraživanja su urađena na Tehnionu, izraelskom institutu za tehnologiju,[9] a razvoj leka je izvelo preduzeće Teva.[10]

Reference[uredi - уреди | uredi izvor]

  1. 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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  edit
  2. 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. 
  3. 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. PMID 20331846. doi:10.1186/1758-2946-2-3.  edit
  4. 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. 
  5. 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. PMID 21948594. doi:10.1093/nar/gkr777.  edit
  6. Oldfield V, Keating GM, Perry CM (2007). "Rasagiline: a review of its use in the management of Parkinson's disease". Drugs 67 (12): 1725–47. PMID 17683172. 
  7. Gallagher DA, Schrag A (2008). "Impact of newer pharmacological treatments on quality of life in patients with Parkinson's disease". CNS Drugs 22 (7): 563–86. PMID 18547126. doi:10.2165/00023210-200822070-00003. 
  8. Binda C; Hubálek F; Li M et al. (2005). "Binding of Rasagiline-related Inhibitors to Human Monoamine Oxidases: A Kinetic and Crystallographic Analysis". Journal of Medical Chemistry 48 (26): 8148–54. PMC 2519603. PMID 16366596. doi:10.1021/jm0506266. 
  9. Lakhan SE (2007). "From a Parkinson's disease expert: Rasagiline and the Future of Therapy". Molecular Neurodegeneration 2: 13. 
  10. "Prescribing Information". Teva Neurosciences. 2005-06. Arhivirano iz originala 19. 1. 2007.. http://web.archive.org/web/20070119131737/http://www.tevaneuro.com/upload/Prescribing_Information.pdf. pristupljeno 20. 3. 2007.. 

Literatura[uredi - уреди | uredi izvor]

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