Etoperidon

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Etoperidon
(IUPAC) ime
2-[3-[4-(3-hlorofenil)piperazin-1-il]
propil]-4,5-dietil-1,2,4-triazol-3-on
Klinički podaci
Identifikatori
CAS broj 52942-31-1
ATC kod N06AB09
PubChem[1][2] 40589
ChemSpider[3] 37083
UNII KAI6MVO39Z YesY
Hemijski podaci
Formula C19H28ClN5O 
Mol. masa 377,911 g/mol
SMILES eMolekuli & PubHem
Sinonimi ST-1191
Farmakoinformacioni podaci
Trudnoća ?
Pravni status Prescription only
Način primene Oralno

Etoperidon (Aksiomin, Centren, Depracer, Etonin, Etoran, Staf, Tropen, klopradon, tozalinon) je antidepresiv iz fenilpiperazinske klase koji je uveden u upotrebu u Evropi 1977.[4][5] On prvenstveno deluje kao antagonist nekoliko receptora u sledećem redosledu potencije: 5-HT2A receptor (36 nM) > α1-adrenergički receptor (38 nM) > 5-HT1A receptor (85 nM) > α2-adrenergički receptor (570 nM);[6] on ima zanemarljiv afinitet za blokiranje sledećih receptora: D2 receptor (2.300 nM) > H1 receptor (3,100 nM) > mACh receptori (>35.000 nM).[6] Pored blokiranja receptora, etoperidon isto tako ima slab afinitet za monoaminske transportere kao i za: serotoninski transporter (890 nM) > norepinefrinski transporter (20.000 nM) > dopaminski transporter (52.000 nM).[7]

Reference[uredi - уреди | uredi izvor]

  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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  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. PMID 20331846. doi:10.1186/1758-2946-2-3.  edit
  4. C. R Ganellin; D. J Triggle; F.. Macdonald (1997). Dictionary of pharmacological agents. CRC Press. str. 859. ISBN 978-0-412-46630-4. http://books.google.com/books?id=DeX7jgInYFMC&pg=PA859. pristupljeno 27 November 2011. 
  5. Index nominum 2000: international drug directory. Taylor & Francis US. 2000. str. 421. ISBN 978-3-88763-075-1. http://books.google.com/books?id=5GpcTQD_L2oC&pg=PA421. pristupljeno 27 November 2011. 
  6. 6,0 6,1 Cusack B, Nelson A, Richelson E. (1994). "Binding of Antidepressants to Human Brain Receptors: Focus on Newer Generation Compounds.". Psychopharmacology (Berl). 114 (4): 559–565. PMID 7855217. doi:10.1007/BF02244985. 
  7. Tatsumi M, Groshan K, Blakely RD, Richelson E. (1997). "Pharmacological Profile of Antidepressants and Related Compounds at Human Monoamine Transporters.". Eur J Pharmacol. 340 (2-3): 249–258. PMID 9537821. doi:10.1016/S0014-2999(97)01393-9. 

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