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Tifluadom
Systematic (IUPAC) name
N-[(5-(2-fluorophenyl)- 1-methyl- 2,3-dihydro- 1,4-benzodiazepin-2-yl) methyl] thiophene- 3-carboxamide
Identifiers
CAS number 83386-35-0
ATC code none
PubChem 115208
Chemical data
Formula C 22H20FN3OS 
Mol. mass 393.477 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes oral, unknown

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

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 Salvia Divinorum..

See also

References

  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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