Rasagilin

Rasagilin
(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	3052776
DrugBank	DB01367
ChemSpider	2314553
UNII	003N66TS6T
KEGG	D02562
ChEMBL	CHEMBL887
Hemijski podaci
Formula	C12H13N
Mol. masa	171,238 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C12H13N/c1-2-9-13-12-8-7-10-5-3-4-6-11(10)12/h1,3-6,12-13H,7-9H2/t12-/m1/s1 ; Key: RUOKEQAAGRXIBM-GFCCVEGCSA-N
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

↑ 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. edit
↑ 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. edit
↑ 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. edit
↑ 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

Povezano

Spoljašnje veze

	Portal Medicina
	Portal Hemija

Rasagiline bound to proteins in the PDB

[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. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. 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. DOI:10.1186/1758-2946-2-3. PMID 20331846. 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. DOI:10.1093/nar/gkr777. PMID 21948594. 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.

[pmid18547126-7] 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. DOI:10.2165/00023210-200822070-00003. PMID 18547126.

[pmid16366596-8] 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.

[9] Lakhan SE (2007). „From a Parkinson's disease expert: Rasagiline and the Future of Therapy”. Molecular Neurodegeneration 2: 13.

[PrescribingInformation-10] „Prescribing Information”. Teva Neurosciences. 2005-06. Arhivirano iz originala na datum 2007-01-19. Pristupljeno 20. 3. 2007.

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]

[9]

[10]