Tropisetron
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(IUPAC) ime | |||
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(1R,5S)-8-metil-8-azabiciklo[3.2.1]oktan-3-il 1metil-indol-3-karboksilat | |||
Klinički podaci | |||
Robne marke | Navoban | ||
AHFS/Drugs.com | Internacionalno ime leka | ||
Identifikatori | |||
CAS broj | 89565-68-4 | ||
ATC kod | A04AA03 | ||
PubChem[1][2] | 72165 | ||
ChemSpider[3] | 16736476 | ||
UNII | 6I819NIK1W ![]() | ||
KEGG[4] | D02130 ![]() | ||
ChEMBL[5] | CHEMBL496980 ![]() | ||
Hemijski podaci | |||
Formula | C17H20N2O2 | ||
Mol. masa | 284,353 g/mol | ||
SMILES | eMolekuli & PubHem | ||
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Sinonimi | ICS 205-930 | ||
Farmakokinetički podaci | |||
Bioraspoloživost | ~60–80% | ||
Vezivanje za proteine plazme | 71% | ||
Metabolizam | Hepatički (CYP3A4, CYP1A2, CYP2D6) | ||
Poluvreme eliminacije | 6–8 sata | ||
Izlučivanje | Renalno, fekalno | ||
Farmakoinformacioni podaci | |||
Trudnoća | X(AU) | ||
Pravni status | Samo na recept (S4) (AU) POM (UK) | ||
Način primene | Oralno, IV |
Tropisetron (INN) je serotoninski 5-HT3 antagonist koji se prvenstveno koristi kao antiemetik za tretman mučnine i povraćanja nakon hemoterapije. On je eksperimentalno takođe korišten kao analgetik kod obolelih od fibromialgije.[6]
Farmakologija[uredi - уреди | uredi izvor]
Tropisetron deluje kao selektivni 5-HT3 antagonist i α7-nikotinski agonist.[7][8]
Reference[uredi - уреди | uredi izvor]
- ↑ 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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.
- ↑ 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. PMID 20331846. doi:10.1186/1758-2946-2-3.
- ↑ 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. PMID 21948594. doi:10.1093/nar/gkr777.
- ↑ Muller, W.; T. Stratz (2004). "Local treatment of tendinopathies and myofascial pain syndromes with the 5-HT3 receptor antagonist tropisetron". Scand J Rheumatic Suppl. 119 (119): 44–48. PMID 15515413. Pristupljeno 2007-05-17.
- ↑ Macor JE, Gurley D, Lanthorn T, Loch J, Mack RA, Mullen G, Tran O, Wright N, Gordon JC (February 2001). "The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist". Bioorganic & Medicinal Chemistry Letters 11 (3): 319–21. PMID 11212100. doi:10.1016/S0960-894X(00)00670-3.
- ↑ Cui R, Suemaru K, Li B, Kohnomi S, Araki H (May 2009). "Tropisetron attenuates naloxone-induced place aversion in single-dose morphine-treated rats: role of alpha7 nicotinic receptors". European Journal of Pharmacology 609 (1–3): 74–7. PMID 19374878. doi:10.1016/j.ejphar.2008.12.051.
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