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Rotigotin

Izvor: Wikipedija

Rotigotin transdermalni flaster
(IUPAC) ime
(S)-6-[propil(2-tiofen-2-iletil)amino]-5,6,7,8- tetrahidronaftalen-1-ol
Klinički podaci
AHFS/Drugs.com Mikromedeks, detaljne potrošačke informacije
MedlinePlus a607059
Identifikatori
CAS broj 92206-54-7
ATC kod N04BC09
PubChem[1][2] 57537
DrugBank DB05271
ChemSpider[3] 51867
UNII 87T4T8BO2E DaY
ChEMBL[4] CHEMBL1303 DaY
Hemijski podaci
Formula C19H25NOS 
Mol. masa 315,474 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Bioraspoloživost 37% (transdermalno)
Vezivanje za proteine plazme 92%
Metabolizam Hepatički (CYP-posredovano)
Poluvreme eliminacije 5–7 sati
Izlučivanje Urin (71%), Fekalije (23%)
Farmakoinformacioni podaci
Trudnoća ?
Pravni status Prescription only
Način primene Transdermalni flaster

Rotigotin (Neupro) je neergolinski dopaminski agonist koji se koristi za lečenje Parkinsonove bolesti i sindroma nemirnih nogu (RLS) u Evropi i SAD-u.[5][6] On se formuliše kao jednodnevni transdermalni flaster koji omogućava spor i konstantan unos leka tokom 24 časovnog perioda.[5][5]

Poput drugih dopaminskih agonista, za rotigotin je pokazano da poseduje antidepresivne efekte i da može da bude koristan u lečenju depresije.[7]

Hemija

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Rotigotin je analogan sa 7-OH-DPAT i UH-232. Sva tri jedinjenja su derivati aminotetralina. Ova jedinjenja imaju sličnu strukturu sa dopaminom, što uslovljava njihovu farmakologiju.

Jedan od mogućih sintetičkih puteva je:[8]

Farmakologija

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Rotigotin poseduje slediće in vitro profile vezivanja za receptore:[9]

Reference

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  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. 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
  5. 5,0 5,1 5,2 Chen JJ, Swope DM, Dashtipour K, Lyons KE (December 2009). „Transdermal rotigotine: a clinically innovative dopamine-receptor agonist for the management of Parkinson's disease”. Pharmacotherapy 29 (12): 1452–67. DOI:10.1592/phco.29.12.1452. PMID 19947805. 
  6. Davies S (September 2009). „Rotigotine for restless legs syndrome”. Drugs of Today (Barcelona, Spain : 1998) 45 (9): 663–8. DOI:10.1358/dot.2009.45.9.1399952. PMID 19956807. 
  7. Bertaina-Anglade V, La Rochelle CD, Scheller DK (October 2006). „Antidepressant properties of rotigotine in experimental models of depression”. European Journal of Pharmacology 548 (1-3): 106–14. DOI:10.1016/j.ejphar.2006.07.022. PMID 16959244. 
  8. Cusack, N. J.; Peck, J. V.; Drugs Future 1993, 18, 1005.
  9. Scheller D, Ullmer C, Berkels R, Gwarek M, Lübbert H (January 2009). „The in vitro receptor profile of rotigotine: a new agent for the treatment of Parkinson's disease”. Naunyn-Schmiedeberg's Archives of Pharmacology 379 (1): 73–86. DOI:10.1007/s00210-008-0341-4. PMID 18704368. 

Povezano

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Spoljašnje veze

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Portal Medicina
Portal Hemija

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Rotigotin
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