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Tifluadom

Tifluadom
IUPAC ime
N-[(5-(2-fluorophenyl)- 1-methyl- 2,3-dihydro- 1,4-benzodiazepin-2-yl) methyl] thiophene- 3-carboxamide
Klinički podaci
Način primeneoralno
Identifikatori
CAS broj83386-35-0 ДаY
ATC kodnone
PubChemCID 115208
IUPHAR/BPS1667
ChemSpider103084 ДаY
KEGGD02694 ДаY
ChEMBLCHEMBL169703 ДаY
Hemijski podaci
FormulaC22H20FN3OS
Molarna masa393.477 g/mol
  • O=C(NCC1N(c3ccccc3C(=N/C1)\c2ccccc2F)C)c4ccsc4
  • InChI=1S/C22H20FN3OS/c1-26-16(13-25-22(27)15-10-11-28-14-15)12-24-21(17-6-2-4-8-19(17)23)18-7-3-5-9-20(18)26/h2-11,14,16H,12-13H2,1H3,(H,25,27) ДаY
  • Key:NPGABYHTDVGGJK-UHFFFAOYSA-N ДаY

Tifluadom je benzodiazepinski derivat. Za razliku od većine benzodiazepina, tifluadom ne deluje kao GABAA agonist, nego je selektivni agonist κ-opioidnog receptora.[1] Tifluadom je potentan analgetik[2] i diuretik[3] životinja. On je takođe sedativ i stimuliše apetit.[4][5]

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.

  1. ^ 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.
  2. ^ 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.
  3. ^ Leander JD. Kappa opioid agonists and antagonists: effects on drinking and urinary output. Appetite. 1984 Mar;5(1):7-14.
  4. ^ 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.
  5. ^ 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.

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Tifluadom
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