Tetrabenazin
(Preusmjereno sa stranice MKJIEFSOBYUXJB-UHFFFAOYSA-N)
Tetrabenazin (Nitoman, Ksenazin) je lek za simptomatički tretman hiperkinetikog poremećaja kretanja. FDA je augusta 2008. odobrila njegovu upotrebu za tretman horeje vezane za Hantingtonovu bolest.[6] Ovo jedinjenje je poznato od 1950-tih. Inicijativu za FDA odobrenje je predvodio Josef Janković.[7][8]
-Tetrabenazine_Structural_Formulae.png)
| |||
| |||
| (IUPAC) ime | |||
|---|---|---|---|
| (SS,RR)-3-Izobutil-9,10-dimetoksi-1,3,4,6,7,11b-heksahidro-pirido[2,1-a]izohinolin-2-on | |||
| Klinički podaci | |||
| Robne marke | Ksenazin | ||
| AHFS/Drugs.com | Potrošačka informacije o leku | ||
| Identifikatori | |||
| CAS broj | 58-46-8 | ||
| ATC kod | N07XX06 | ||
| PubChem[1][2] | 6018 | ||
| DrugBank | DB04844 | ||
| ChemSpider[3] | 5796 | ||
| UNII | Z9O08YRN8O 
| ||
| KEGG[4] | D08575
| ||
| ChEMBL[5] | CHEMBL117785
| ||
| Hemijski podaci | |||
| Formula | C19H27NO3 | ||
| Mol. masa | 317,427 g/mol | ||
| SMILES | eMolekuli & PubHem | ||
| |||
| Sinonimi | Ro-1-9569 | ||
| Farmakokinetički podaci | |||
| Bioraspoloživost | Niska | ||
| Vezivanje za proteine plazme | 82–85% | ||
| Metabolizam | Hepatički (CYP2D6-posredovano) | ||
| Izlučivanje | Renalno i fekalno | ||
| Farmakoinformacioni podaci | |||
| Trudnoća | ? | ||
| Pravni status | ℞-only (US) | ||
| Način primene | Oralno (tablete, 25 mg) | ||
Farmakologija uredi
Tetrabenazin deluje prvenstveno kao VMAT-inhibitor,[9] te promoviše ranu metaboličku degradaciju monoamina, posebno neurotransmitera dopamina.
Reference uredi
- ↑ 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.
- ↑ „1st US drug for Huntington's disease wins approval”. Arhivirano iz originala na datum 2020-02-13. Pristupljeno 2014-04-05.
- ↑ Doctor spent decades getting tetrabenazine to market
- ↑ Specialty TrendsRx Availability Alert:Xenazine® (tetrabenazine)
- ↑ Zheng G, Dwoskin LP, Crooks PA (2006). „Vesicular monoamine transporter 2: role as a novel target for drug development”. AAPS J 8 (4): E682–92. DOI:10.1208/aapsj080478. PMC 2751365. PMID 17233532.
Spoljašnje veze uredi
- NIMH Repository data sheet Arhivirano 2007-03-10 na Wayback Machine-u
- "Tetrabenazine" Arhivirano 2010-07-18 na Archive.is-u