Tifluadom

Izvor: Wikipedija
Prijeđi na navigaciju Prijeđi na pretragu
Tifluadom
(IUPAC) ime
N-[(5-(2-fluorophenyl)- 1-methyl- 2,3-dihydro- 1,4-benzodiazepin-2-yl) methyl] thiophene- 3-carboxamide
Klinički podaci
Identifikatori
CAS broj 83386-35-0
ATC kod nije dodeljen
PubChem[1][2] 115208
ChemSpider[3] 103084
KEGG[4] D02694 DaY
ChEMBL[5] CHEMBL169703 DaY
Hemijski podaci
Formula C22H20FN3OS 
Mol. masa 393.477 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status
Način primene oralno

Tifluadom je benzodiazepinski derivat. Za razliku od većine benzodiazepina, tifluadom ne deluje kao GABAA agonist, nego je selektivni agonist κ-opioidnog receptora.[6] Tifluadom je potentan analgetik[7] i diuretik[8] životinja. On je takođe sedativ i stimuliše apetit.[9][10]

Dok tifluadom ima više efekata koji potencijalno mogu da nađu medicinsku primenu, kao što su analgezija i stimulacija apetita, on je κ-opioidni agonist i stoga je sklon ispoljavanju nepoželjnih nuspojava kod ljudi, kao što su disforija i halucinacije. Lekovi iz ove grupe se uglavnom koriste u naučnim istraživanjima. Njegovi disforični efekti su slični drugim agonistima κ-opioidnih receptora, npr. pentazocinu i Salvia divinorum.

Vidi još[uredi | uredi kod]

Reference[uredi | uredi kod]

  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. Romer D, Buscher HH, Hill RC, Maurer R, Petcher TJ, Zeugner H, Benson W, Finner E, Milkowski W, Thies PW. Unexpected opioid activity in a known class of drug. Life Sciences. 1982 Sep 20-27;31(12-13):1217-20.
  7. Genovese RF, Dykstra LA. Tifluadom's effects under electric shock titration and tail-immersion procedures in squirrel monkeys. Life Sciences. 1986 Nov 10;39(19):1713-9.
  8. Leander JD. Kappa opioid agonists and antagonists: effects on drinking and urinary output. Appetite. 1984 Mar;5(1):7-14.
  9. Jackson HC, Sewell RD. The role of opioid receptor sub-types in tifluadom-induced feeding. Journal of Pharmacy and Pharmacology. 1984 Oct;36(10):683-6.
  10. Dykstra LA, Gmerek DE, Winger G, Woods JH. Kappa opioids in rhesus monkeys. I. Diuresis, sedation, analgesia and discriminative stimulus effects. Journal of Pharmacology and Experimental Therapeutics. 1987 Aug;242(2):413-20.

Spoljašnje veze[uredi | uredi kod]