Trifluoperazin

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Trifluoperazin
(IUPAC) ime
10-[3-(4-metilpiperazin-1-il)propil]-
2-(trifluorometil)-10H-fenotiazin
Klinički podaci
AHFS/Drugs.com Monografija
MedlinePlus a682121
Identifikatori
CAS broj 117-89-5
ATC kod N05AB06
PubChem[1][2] 5566
DrugBank DB00831
ChemSpider[3] 5365
UNII 214IZI85K3 YesY
ChEBI CHEBI:45951 YesY
ChEMBL[4] CHEMBL422 YesY
Hemijski podaci
Formula C21H24F3N3S 
Mol. masa 407,497
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Metabolizam Hepatički
Poluvreme eliminacije 10–20 sata
Farmakoinformacioni podaci
Trudnoća C(AU) C(US)
Pravni status POM (UK) -only (SAD)
Način primene oralno, IM

Trifluoperazin (Eskazinil, Eskazin, Jatroneural, Modalina, Stelazin, Terfluzin, Trifluoperaz, Triftazin) je tipični antipsihotik iz fenotiazinske hemijske klase.

Farmakologija[uredi - уреди | uredi kôd]

Trifluoperazin je centralni simpatolitik,[5] antagonist dopaminskog receptora,[6][7] sa minimalnim antiholinergičnim dejstvom.[8]

Hemija[uredi - уреди | uredi kôd]

Trifluoperazin (2-trifluorometil-10-[3-(4-metil-1-piperazinil)propil]fenotazin) se sintetiše na sličan način kao i prohlorperazin. Alkilacija se izvodi koristeći 2-trifluorometilfenotazin-4-metil-1-piperazinilpropilhlorid kao supstrat.[9][10][11][12][13]

Reference[uredi - уреди | uredi kôd]

  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. http://www.sciencedirect.com/science/article/pii/S1359644610007737.  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. http://www.jcheminf.com/content/2/1/3.  edit
  4. 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
  5. Huerta-Bahena J, Villalobos-Molina R, García-Sáinz JA (January 1983). „Trifluoperazine and chlorpromazine antagonize alpha 1- but not alpha2- adrenergic effects”. Molecular Pharmacology 23 (1): 67–70. PMID 6135146. http://molpharm.aspetjournals.org/cgi/pmidlookup?view=long&pmid=6135146. Pristupljeno 2009-06-21. 
  6. Seeman P, Lee T, Chau-Wong M, Wong K (June 1976). „Antipsychotic drug doses and neuroleptic/dopamine receptors”. Nature 261 (5562): 717–9. Bibcode 1976Natur.261..717S. DOI:10.1038/261717a0. PMID 945467. 
  7. Creese I, Burt DR, Snyder SH (1996). „Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs”. The Journal of Neuropsychiatry and Clinical Neurosciences 8 (2): 223–6. PMID 9081563. http://neuro.psychiatryonline.org/cgi/content/abstract/8/2/223. Pristupljeno 2009-06-21. 
  8. Ebadi, Manuchair S (1998). „Trifluoperazine Hydrochloride”. CRC desk reference of clinical pharmacology (illustrated izd.). CRC Press. ISBN 978-0-8493-9683-0. http://books.google.co.uk/books?id=-EAxShTKfGAC&lpg=PA580&dq=trifluoperazine%20anticholinergic. Pristupljeno 2009-06-21. 
  9. Craig, P.; Nodiff, E.; Lafferty, J.; Ullyot, G. (1957). „Notes - New Trifluoromethylphenothiazine Derivatives”. Journal of Organic Chemistry 22 (6): 709. DOI:10.1021/jo01357a618. 
  10. G.E. Ullyot, U.S. Patent 2.921.069 (1960).
  11. Sharma, H.; Banerjee, S.; Sharma, V.; Mital, R. (1968). „Phenothiazines Exhibiting Lesser Extraparamidal Manifestations”. Journal of Medicinal Chemistry 11 (6): 1244. DOI:10.1021/jm00312a600. PMID 5680054. 
  12. P.N. Craig, G.E. Ullyot, DE 1165034  (1956).
  13. B.H. Chung, F. Zimalkowski, Arch. Pharm., 317, 323 (1984).

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