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Chemical Compound Review

Tirilazad     (8S,10R,13S,14S,16R,17S)-17- [2-[4-(2,6...

Synonyms: Tirilazadum, SureCN483318, CHEMBL1630578, AC1L2XOZ, LS-172108, ...
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Disease relevance of U 74006


High impact information on U 74006


Chemical compound and disease context of U 74006


Biological context of U 74006


Anatomical context of U 74006


Associations of U 74006 with other chemical compounds


Gene context of U 74006

  • Collectively, these data suggest that formation of U-89678, a circulating pharmacologically active metabolite, contributes to the total metabolic elimination of tirilazad in humans and that clearance of U-89678 is mediated primarily via CYP3A4 metabolism [26].
  • Hormonal effects on tirilazad clearance in women: assessment of the role of CYP3A [27].
  • Fibroblasts pre-incubated with tirilazad at a concentration of 30 muM show significantly less IL-6 in the extracellular medium after UVA exposure [28].
  • Treatment with antioxidants, superoxide dismutase (SOD) or tirilazad significantly improved the neurogenic vascular response while tirilazad treatment significantly alleviated thermal hyperalgesia [29].
  • METHODS: Tirilazad (a lipid peroxidase inhibitor) or FK and acYVAD-cmk (a caspase inhibitor), were added to embryonic porcine ventral mesencephalic tissue and viability was assessed in vitro [30].

Analytical, diagnostic and therapeutic context of U 74006

  • Improvement in high-energy phosphate recovery 17 minutes after starting tirilazad infusion during reperfusion is consistent with an early onset of a functionally significant oxygen radical injury [2].
  • Plasma tirilazad mesylate concentrations were determined by HPLC [14].
  • In both periods, 1.5 mg/kg tirilazad mesylate was administered (as 10-minute intravenous infusions) every 6 hours for 21 doses (5 days) [21].
  • The objective of the present study was to explore the effects of tirilazad mesylate on DA neuron survival in cultures of rat ventral mesencephalon and its capacity to promote the in vitro cell viability of embryonic rat and human mesencephalic tissue, treated and dissociated in the same way as in clinical trials [31].
  • METHODS: Using a double-blind study design, eight volunteers received tirilazad mesylate, and eight others received only vehicle [32].


  1. Novel inhibitors of iron-dependent lipid peroxidation for neurodegenerative disorders. Hall, E.D. Ann. Neurol. (1992) [Pubmed]
  2. Amelioration of impaired cerebral metabolism after severe acidotic ischemia by tirilazad posttreatment in dogs. Kim, H., Koehler, R.C., Hurn, P.D., Hall, E.D., Traystman, R.J. Stroke (1996) [Pubmed]
  3. Effects of tirilazad mesylate on vasospasm and phospholipid hydroperoxides in a primate model of subarachnoid hemorrhage. Suzuki, H., Kanamaru, K., Kuroki, M., Sun, H., Waga, S., Miyazawa, T. Stroke (1999) [Pubmed]
  4. Tirilazad treatment does not decrease early brain injury after transient focal ischemia in cats. Takeshima, R., Kirsch, J.R., Koehler, R.C., Traystman, R.J. Stroke (1994) [Pubmed]
  5. High-dose tirilazad for acute stroke (RANTTAS II). RANTTAS II Investigators. Haley, E.C. Stroke (1998) [Pubmed]
  6. Modulation of inflammation by reactive oxygen species: implications for aging and tissue repair. Khodr, B., Khalil, Z. Free Radic. Biol. Med. (2001) [Pubmed]
  7. A role for free radicals and nitric oxide in delayed recovery in aged rats with chronic constriction nerve injury. Khalil, Z., Khodr, B. Free Radic. Biol. Med. (2001) [Pubmed]
  8. A predictive risk model for outcomes of ischemic stroke. Johnston, K.C., Connors, A.F., Wagner, D.P., Knaus, W.A., Wang, X., Haley, E.C. Stroke (2000) [Pubmed]
  9. Combination drug therapy and mild hypothermia: a promising treatment strategy for reversible, focal cerebral ischemia. Schmid-Elsaesser, R., Hungerhuber, E., Zausinger, S., Baethmann, A., Reulen, H.J. Stroke (1999) [Pubmed]
  10. Comparative study of the effect of 21-aminosteroid and alpha-tocopherol on models of acute oxidative renal injury. Salahudeen, A.K., Wang, C., Kanji, V.K. Free Radic. Biol. Med. (1996) [Pubmed]
  11. Pharmacokinetic alterations after severe head injury. Clinical relevance. Boucher, B.A., Hanes, S.D. Clinical pharmacokinetics. (1998) [Pubmed]
  12. Effect of lipid peroxidation inhibition on retinal ganglion cell death. Levin, L.A., Clark, J.A., Johns, L.K. Invest. Ophthalmol. Vis. Sci. (1996) [Pubmed]
  13. Effects of nalmefene, CG3703, tirilazad, or dopamine on cerebral blood flow, oxygen delivery, and electroencephalographic activity after traumatic brain injury and hemorrhage. Dewitt, D.S., Prough, D.S., Uchida, T., Deal, D.D., Vines, S.M. J. Neurotrauma (1997) [Pubmed]
  14. Effect of age and gender on tirilazad pharmacokinetics in humans. Hulst, L.K., Fleishaker, J.C., Peters, G.R., Harry, J.D., Wright, D.M., Ward, P. Clin. Pharmacol. Ther. (1994) [Pubmed]
  15. Effect of the 21-aminosteroid tirilazad on cerebral pH and somatosensory evoked potentials after incomplete ischemia. Maruki, Y., Koehler, R.C., Kirsch, J.R., Blizzard, K.K., Traystman, R.J. Stroke (1993) [Pubmed]
  16. Protective effects of lazaroid U74389F (16-desmethyl tirilazad) on endrin-induced lipid peroxidation and DNA damage in brain and liver and regional distribution of catalase activity in rat brain. Bagchi, M., Ghosh, S., Bagchi, D., Hassoun, E., Stohs, S.J. Free Radic. Biol. Med. (1995) [Pubmed]
  17. Tirilazad pretreatment improves early cerebral metabolic and blood flow recovery from hyperglycemic ischemia. Maruki, Y., Koehler, R.C., Kirsch, J.R., Blizzard, K.K., Traystman, R.J. J. Cereb. Blood Flow Metab. (1995) [Pubmed]
  18. Tirilazad mesylate does not improve early cerebral metabolic recovery following compression ischemia in dogs. Helfaer, M.A., Kirsch, J.R., Hurn, P.D., Blizzard, K.K., Koehler, R.C., Traystman, R.J. Stroke (1992) [Pubmed]
  19. Effects of tirilazad mesylate on postischemic brain lipid peroxidation and recovery of extracellular calcium in gerbils. Hall, E.D., Pazara, K.E., Braughler, J.M. Stroke (1991) [Pubmed]
  20. Lazaroids. CNS pharmacology and current research. Clark, W.M., Hazel, J.S., Coull, B.M. Drugs (1995) [Pubmed]
  21. The effect of phenytoin on the pharmacokinetics of tirilazad mesylate in healthy male volunteers. Fleishaker, J.C., Hulst, L.K., Peters, G.R. Clin. Pharmacol. Ther. (1994) [Pubmed]
  22. Changes in membrane properties during energy depletion-induced cell injury studied with fluorescence microscopy. Wu, Y., Sun, F.F., Tong, D.M., Taylor, B.M. Biophys. J. (1996) [Pubmed]
  23. Lack of effect of postinjury treatment with methylprednisolone or tirilazad mesylate on the increase in eicosanoid levels in the acutely injured cat spinal cord. Hall, E.D., Yonkers, P.A., Taylor, B.M., Sun, F.F. J. Neurotrauma (1995) [Pubmed]
  24. Additive effects of caspase inhibitor and lazaroid on the survival of transplanted rat and human embryonic dopamine neurons. Hansson, O., Castilho, R.F., Kaminski Schierle, G.S., Karlsson, J., Nicotera, P., Leist, M., Brundin, P. Exp. Neurol. (2000) [Pubmed]
  25. Biotransformation of tirilazad in human: 2. Effect of ketoconazole on tirilazad clearance and oral bioavailability. Fleishaker, J.C., Pearson, P.G., Wienkers, L.C., Pearson, L.K., Peters, G.R. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  26. Biotransformation of tirilazad in human: 3. tirilazad A-ring reduction by human liver microsomal 5alpha-reductase type 1 and type 2. Wienkers, L.C., Steenwyk, R.C., Hauer, M.J., Fleishaker, J.C., Pearson, P.G. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  27. Hormonal effects on tirilazad clearance in women: assessment of the role of CYP3A. Fleishaker, J.C., Pearson, L.K., Pearson, P.G., Wienkers, L.C., Hopkins, N.K., Peters, G.R. Journal of clinical pharmacology. (1999) [Pubmed]
  28. Tirilazad amelioriates extracellular effects of photooxidative stress by sealing the membrane of UVA irradiated human dermal fibroblasts. Schneider, L.A., Dissemond, J., Schwamborn, E., Wlaschek, M., Brenneisen, P., Scharffetter-Kochanek, K. European journal of dermatology : EJD (2006) [Pubmed]
  29. Free radicals contribute to the reduction in peripheral vascular responses and the maintenance of thermal hyperalgesia in rats with chronic constriction injury. Khalil, Z., Liu, T., Helme, R.D. Pain (1999) [Pubmed]
  30. Effects of immunosuppressive treatment on host responses against intracerebral porcine neural tissue xenografts in rats. Wennberg, L., Czech, K.A., Larsson, L.C., Mirza, B., Bennet, W., Song, Z., Widner, H. Transplantation (2001) [Pubmed]
  31. Tirilazad mesylate improves survival of rat and human embryonic mesencephalic neurons in vitro. Othberg, A., Keep, M., Brundin, P., Lindvall, O. Exp. Neurol. (1997) [Pubmed]
  32. The effect of tirilazad mesylate (U74006F) on cerebral oxygen consumption, and reactivity of cerebral blood flow to carbon dioxide in healthy volunteers. Olsen, K.S., Videbaek, C., Agerlin, N., Krøll, M., Bøge-Rasmussen, T., Paulson, O.B., Gjerris, F. Anesthesiology (1993) [Pubmed]
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