Rasagilin
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| (IUPAC) ime | |||
|---|---|---|---|
| (R)-N-(prop-2-inil)-2,3-dihidro-1H-inden-1-amin | |||
| Klinički podaci | |||
| Robne marke | Azilect, Azipron | ||
| 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 
| ||
| KEGG[4] | D02562
| ||
| ChEMBL[5] | CHEMBL887
| ||
| Hemijski podaci | |||
| Formula | C12H13N | ||
| Mol. masa | 171,238 g/mol | ||
| SMILES | eMolekuli & PubHem | ||
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| 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, Azipron, 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 | uredi kod]
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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. DOI:10.2165/00023210-200822070-00003. PMID 18547126.
- ↑ Binda C, Hubálek F, Li M i dr.. (2005). „Binding of Rasagiline-related Inhibitors to Human Monoamine Oxidases: A Kinetic and Crystallographic Analysis”. Journal of Medical Chemistry 48 (26): 8148–54. DOI:10.1021/jm0506266. PMC 2519603. PMID 16366596.
- ↑ Lakhan SE (2007). „From a Parkinson's disease expert: Rasagiline and the Future of Therapy”. Molecular Neurodegeneration 2: 13.
- ↑ „Prescribing Information”. Teva Neurosciences. 2005-06. Arhivirano iz originala na datum 2007-01-19. Pristupljeno 20. 3. 2007.
Literatura[uredi | uredi kod]
Vidi još[uredi | uredi kod]
Spoljašnje veze[uredi | uredi kod]
- Rasagiline bound to proteins in the PDB