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tifluadom
Tifluadom〔US Patent 4325957〕 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.〔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.〕 In accordance, it has potent analgesic〔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.〕 and diuretic〔Leander JD. Kappa opioid agonists and antagonists: effects on drinking and urinary output. ''Appetite''. 1984 Mar;5(1):7-14.〕 effects in animals, and also has sedative effects and stimulates appetite.〔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.〕〔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.〕
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==
* Lufuradom
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