Tifluadom
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(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 ![]() | ||
ChEMBL[5] | CHEMBL169703 ![]() | ||
Hemijski podaci | |||
Formula | C22H20FN3OS | ||
Mol. masa | 393.477 g/mol | ||
SMILES | eMolekuli & PubHem | ||
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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.
- ↑ 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.
- ↑ 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.
- ↑ 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 21948863.
- ↑ 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.
- ↑ 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.
- ↑ Leander JD. Kappa opioid agonists and antagonists: effects on drinking and urinary output. Appetite. 1984 Mar;5(1):7-14.
- ↑ 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.
- ↑ 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.