Tifluadom

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Tifluadom
Tifluadom.svg
Systematic (IUPAC) name
N-[[5-(2-fluorophenyl)-1-methyl-2,3-dihydro-1,4-benzodiazepin-2-yl]methyl]thiophene-3-carboxamide
Clinical data
Routes of
administration		 unknown
Identifiers
CAS Number 83386-35-0 N
ATC code none
PubChem CID 115208
IUPHAR/BPS 1667
ChemSpider 103084 YesY
UNII TF8X866L0I YesY
KEGG D02694 YesY
ChEMBL CHEMBL169703 YesY
Chemical data
Formula C22H20FN3OS
Molar mass 393.477 g/mol
3D model (Jmol) Interactive image
 NYesY (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[edit]

  • Lufuradom
  • GYKI-52895, structural benzodiazepine which is a dopamine reuptake inhibitor without GABAergic function
  • GYKI-52,466, structural benzodiazepine which is an AMPAkine and glutamate antagonist without GABAergic function

References[edit]

  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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