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Open Access Articles- Top Results for Tifluadom

Tifluadom

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Tifluadom
200px
Systematic (IUPAC) name
N-[(5-(2-fluorophenyl)- 1-methyl- 2,3-dihydro- 1,4-benzodiazepin-2-yl) methyl] thiophene- 3-carboxamide
Clinical data
oral, unknown
Identifiers
83386-35-0 7pxN
None
PubChem CID 115208
IUPHAR ligand 1667
ChemSpider 103084 7pxY
UNII TF8X866L0I 7pxY
KEGG D02694 7pxY
ChEMBL CHEMBL169703 7pxY
Chemical data
Formula C22H20FN3OS
393.477 g/mol
 14pxN (what is this?)  (verify)

Tifluadom[1] is a benzodiazepine derivative with an unusual activity profile. Unlike most benzodiazepines, tifluadom has no activity at the GABAA receptor, but instead is a selective agonist for the κ-opioid receptor.[2] In accordance, it has potent analgesic[3] and diuretic[4] effects in animals, and also has sedative effects and stimulates appetite.[5][6]

While tifluadom has several effects which might have potential uses in medicine such as analgesia and appetite stimulation, κ-opioid agonists tend to produce undesirable effects in humans such as dysphoria and hallucinations, and so these drugs tend to only be used in scientific research. Dysphoric effects are similar to those seen when using other κ-opioid receptor agonists like pentazocine and salvinorin A.

See also

References

  1. US Patent 4325957
  2. 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.
  3. 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.
  4. Leander JD. Kappa opioid agonists and antagonists: effects on drinking and urinary output. Appetite. 1984 Mar;5(1):7-14.
  5. 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.
  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.


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