Tetrabenazin

Tetrabenazin
(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	6018
DrugBank	DB04844
ChemSpider	5796
UNII	Z9O08YRN8O
KEGG	D08575
ChEMBL	CHEMBL117785
Hemijski podaci
Formula	C19H27NO3
Mol. masa	317,427 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C19H27NO3/c1-12(2)7-14-11-20-6-5-13-8-18(22-3)19(23-4)9-15(13)16(20)10-17(14)21/h8-9,12,14,16H,5-7,10-11H2,1-4H3 ; Key: MKJIEFSOBYUXJB-UHFFFAOYSA-N
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)

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]

Farmakologija

Tetrabenazin deluje prvenstveno kao VMAT-inhibitor,^[9] te promoviše ranu metaboličku degradaciju monoamina, posebno neurotransmitera dopamina.

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
↑ „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

	Portal Medicina
	Portal Hemija

NIMH Repository data sheet Arhivirano 2007-03-10 na Wayback Machine-u
"Tetrabenazine" Arhivirano 2010-07-18 na Archive.is-u

[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] „1st US drug for Huntington's disease wins approval”. Arhivirano iz originala na datum 2020-02-13. Pristupljeno 2014-04-05.

[7] Doctor spent decades getting tetrabenazine to market

[8] Specialty TrendsRx Availability Alert:Xenazine® (tetrabenazine)

[GZ_2006-9] 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.

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