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Chemical Compound Review

Tifluadom     N-[[6-(2-fluorophenyl)-2- methyl-2,5...

Synonyms: titfluadom, dl-Tifluadom, AGN-PC-00MDCU, CHEMBL169703, SureCN142030, ...
 
 
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Disease relevance of C11797

  • The hyperphagia induced by tifluadom was antagonized by naloxone, suggesting that the effect was mediated by an action at opiate receptors [1].
  • In adrenal demedullated rats, tifluadom induced initial arrest of heart was not affected but the subsequent bradycardia was blocked [2].
 

Psychiatry related information on C11797

  • Administration of the kappa-opiates tifluadom (2.5 mg/kg i.p.) or ketazocine (5 mg/kg i.p.) caused a marked initial decrease in locomotor activity lasting about 15-20 min, followed by an increase in locomotor activity at about 40 min after drug administration [3].
 

High impact information on C11797

  • The influence of oral (p.o.) administration of kappa-(U-50488, tifluadom) and mu- (morphine, DAGO) opioid substances on gastric emptying of liquids and solids in a standard canned dog food meal was evaluated using a double-radiolabeled technique in dogs fitted with gastric cannulas [4].
  • Cholecystokinin-A receptor ligands based on the kappa-opioid agonist tifluadom [5].
  • The kappa opioid agonists U50,488, bremazocine, ethylketazocine and tifluadom and the opioid antagonist naltrexone were examined alone and in combination with morphine in a squirrel monkey shock titration procedure, before and during chronic morphine administration [6].
  • During tests of substitution, the selective kappa-opioid agonists bremazocine, U50, 488 and tifluadom substituted for the bremazocine stimulus, whereas the less selective kappa-opioid agonists ethylketocyclazocine, levallorphan, proxorphan and nalorphine substituted for the fentanyl stimulus [7].
  • In order to determine the functional significance of the increased density of brain kappa opioid receptors in SHR rats, the effect of the kappa receptor agonists, tifluadom, U-50,488H and bremazocine, on two known actions associated with kappa receptors, namely analgesia and diuresis, were determined in SHR and normotensive rats [8].
 

Chemical compound and disease context of C11797

 

Biological context of C11797

  • Tifluadom-induced diuresis in rats. Evidence for an opioid receptor-mediated central action [11].
  • Tifluadom inhibited the binding of [3H]MeTRH with an IC50 value of 1.88 microM [12].
  • Levorphanol, tifluadom, bremazocine and MR 2034 produced dose-related decreases in minute volume, tidal volume and respiratory frequency [13].
  • The effects of the kappa agonists bremazocine, ethylketazocine, tifluadom and U-50,488 were examined in rhesus monkeys with four experimental procedures: urinary output was measured in normally hydrated monkeys; muscle relaxation and stupor were observed; and the time it took monkeys to withdraw their tails from warm water was evaluated [14].
  • Finally, using another kappa agonist, tifluadom, we showed that the effect on food intake is stereospecific [15].
 

Anatomical context of C11797

 

Associations of C11797 with other chemical compounds

 

Gene context of C11797

  • The influence of tifluadom on cholecystokinin-induced antinociception [22].
  • Scatchard analysis indicated the inhibition of CCK binding by tifluadom was competitive in nature [18].
  • An ethological analysis of the effects of tifluadom on social encounters in male albino mice [23].
  • In this study we found that the ob/ob mouse was mildly resistant to the ability of three kappa agonists, viz, butorphanol, tifluadom, and ketocyclazocine to induce food intake [24].
 

Analytical, diagnostic and therapeutic context of C11797

References

  1. Effects of tifluadom on food consumption compared with chlordiazepoxide and kappa agonists in the rat. Cooper, S.J., Moores, W.R., Jackson, A., Barber, D.J. Neuropharmacology (1985) [Pubmed]
  2. Cardiovascular responses to kappa opioid agonists in intact and adrenal demedullated rats. Gulati, A., Bhargava, H.N. Eur. J. Pharmacol. (1988) [Pubmed]
  3. The effects of tifluadom and ketazocine on behaviour, dopamine turnover in the basal ganglia and local cerebral glucose utilization of rats. Beck, T., Krieglstein, J. Brain Res. (1986) [Pubmed]
  4. Opposite effects of kappa-opioid agonists on gastric emptying of liquids and solids in dogs. Gue, M., Fioramonti, J., Honde, C., Pascaud, X., Junien, J.L., Bueno, L. Gastroenterology (1988) [Pubmed]
  5. Cholecystokinin-A receptor ligands based on the kappa-opioid agonist tifluadom. Bock, M.G., DiPardo, R.M., Evans, B.E., Rittle, K.E., Whitter, W.L., Veber, D.F., Freidinger, R.M., Chang, R.S., Chen, T.B., Lotti, V.J. J. Med. Chem. (1990) [Pubmed]
  6. Agonist and antagonist activity of kappa opioids in the squirrel monkey: II. Effect of chronic morphine treatment. Craft, R.M., Dykstra, L.A. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  7. Discriminative stimulus effects of mu and kappa opioids in the pigeon: analysis of the effects of full and partial mu and kappa agonists. Picker, M.J., Dykstra, L.A. J. Pharmacol. Exp. Ther. (1989) [Pubmed]
  8. Kappa opioid receptor activity in spontaneously hypertensive rats. Bhargava, H.N., Gulati, A. J. Pharmacol. Exp. Ther. (1988) [Pubmed]
  9. Effects of the opioid benzodiazepine tifluadom and its optical isomers on spontaneous locomotor activity of mice. Ruhland, M., Zeugner, H. Life Sci. (1983) [Pubmed]
  10. Opioid benzodiazepine tifluadom and drug-induced hyperactivity in mice: lack of benzodiazepine-like effects. Sansone, M., Castellano, C., Pavone, F., Hano, J. Polish journal of pharmacology and pharmacy. (1985) [Pubmed]
  11. Tifluadom-induced diuresis in rats. Evidence for an opioid receptor-mediated central action. Shearman, G.T., Tolcsvai, L. Neuropharmacology (1986) [Pubmed]
  12. Inhibition of [3H][3-MeHis2]thyrotropin releasing hormone recognition sites in the rat brain by tifluadom, a kappa opiate receptor agonist. Das, S., Bhargava, H.N. Neuropharmacology (1987) [Pubmed]
  13. Effects of levorphanol and several kappa-selective opioids on respiration and behavior in rhesus monkeys. Howell, L.L., Bergman, J., Morse, W.H. J. Pharmacol. Exp. Ther. (1988) [Pubmed]
  14. Kappa opioids in rhesus monkeys. I. Diuresis, sedation, analgesia and discriminative stimulus effects. Dykstra, L.A., Gmerek, D.E., Winger, G., Woods, J.H. J. Pharmacol. Exp. Ther. (1987) [Pubmed]
  15. The kappa opioid receptor and food intake. Morley, J.E., Levine, A.S., Kneip, J., Grace, M., Zeugner, H., Shearman, G.T. Eur. J. Pharmacol. (1985) [Pubmed]
  16. Opioid inhibition of adenylate cyclase in the striatum and vas deferens of the rat. Bhoola, K.D., Pay, S. Br. J. Pharmacol. (1986) [Pubmed]
  17. Actions of opioids on the dorsal root potential of the isolated spinal cord preparation of the neonate rat. Briggs, I., Barnes, J.C. Neuropharmacology (1987) [Pubmed]
  18. Tifluadom, a kappa-opiate agonist, acts as a peripheral cholecystokinin receptor antagonist. Chang, R.S., Lotti, V.J., Chen, T.B., Keegan, M.E. Neurosci. Lett. (1986) [Pubmed]
  19. Stereoselectivity of kappa-opiate receptor ligands in inhibiting the binding of [3H][3-MeHis2]thyrotrophin releasing hormone to brain membranes. Bhargava, H.N., Das, S., Gulati, A. J. Pharm. Pharmacol. (1988) [Pubmed]
  20. Differential, postnatal ontogeny of opiate and benzodiazepine receptor subtypes in rat cerebral cortex: binding characteristics of tifluadom and brotizolam. Hill, H.F., Watanabe, Y., Shibuya, T. Jpn. J. Pharmacol. (1984) [Pubmed]
  21. Orally administered kappa but not mu opiate agonists enhance gastric emptying of a solid canned food meal in dogs. Gué, M., Fioramonti, J., Junien, J.L., Bueno, L. J. Pharm. Pharmacol. (1988) [Pubmed]
  22. The influence of tifluadom on cholecystokinin-induced antinociception. Gericke, M., Morgenstern, R., Ott, T. Eur. J. Pharmacol. (1990) [Pubmed]
  23. An ethological analysis of the effects of tifluadom on social encounters in male albino mice. Brain, P.F., Smoothy, R., Benton, D. Pharmacol. Biochem. Behav. (1985) [Pubmed]
  24. The kappa opioid receptor, ingestive behaviors and the obese mouse (ob/ob). Morley, J.E., Levine, A.S., Gosnell, B.A., Kneip, J., Grace, M. Physiol. Behav. (1983) [Pubmed]
  25. Effects of tifluadom on passive avoidance behaviour in DBA/2 mice. Pavone, F., Castellano, C. Behav. Brain Res. (1985) [Pubmed]
 
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