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Tifluadom



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  ?
PubChem 115208
Chemical data
Formula C22H20FN3OS 
Mol. mass 393.477 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

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Legal status
Routes  ?


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]

Additional recommended knowledge

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.


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.
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Tifluadom". A list of authors is available in Wikipedia.
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