Tifluadom

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

Tifluadom is a benzodiazepine derivative with an unusual activity profile. Unlike most benzodiazepines, tifluadom has no activity as a GABA_A 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.

[edit] 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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