Tropisetron

Tropisetron
(IUPAC) ime
	(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	72165
ChemSpider	16736476
UNII	6I819NIK1W
KEGG	D02130
ChEMBL	CHEMBL496980
Hemijski podaci
Formula	C17H20N2O2
Mol. masa	284,353 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C17H20N2O2/c1-19-11-6-7-12(19)9-13(8-11)21-17(20)15-10-18-16-5-3-2-4-14(15)16/h2-5,10-13,18H,6-9H2,1H3/t11-,12+,13+ ; Key: ZNRGQMMCGHDTEI-ITGUQSILSA-N
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

Tropisetron deluje kao selektivni 5-HT₃ antagonist i α₇-nikotinski agonist.^[7]^[8]

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
↑ 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. DOI:10.1016/S0960-894X(00)00670-3. PMID 11212100.
↑ 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. DOI:10.1016/j.ejphar.2008.12.051. PMID 19374878.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[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

[pain-6] 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.

[pmid11212100-7] 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. DOI:10.1016/S0960-894X(00)00670-3. PMID 11212100.

[pmid19374878-8] 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. DOI:10.1016/j.ejphar.2008.12.051. PMID 19374878.

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