Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 27, 1997 - Issue 11
34
Views
4
CrossRef citations to date
0
Altmetric
Research Article

In vitro metabolic transformations of 2,4- dipyrrolidinylp yrimidine : a chemical probe for P450-mediated oxidation of tirilazad mesylate

, , , , , & show all
Pages 1131-1145 | Published online: 22 Sep 2008

References

  • ANDERSON, D. K., BRAUGHLER, J. M., HALL, E. D., WATERS, T. R., MCCALL, J. M. and MEANS, E. D., 1988, Effect of treatm ent with U-74006F on neurologicaloutcome following experimentalmodel of spinal cord injury. Journal of Neurosurgery, 96, 562–567.
  • BERNARD, T., 1995a, Monooxygenase-catalyzed nitrogen oxidations. In Biochemistry of Redox Reactions, edited by B. Testa and J. Caldwell (New York: Academic), pp. 164–202.
  • BERNARD, T., 1995, Monooxygenase-catalyzed N-C cleavage. In Biochemistry of Redox Reactions, edited by B. Testa and J. Caldwell (New York: Academic), pp. 203–234.
  • BRAUGHLER, J. M., BURTON, P. S., CHASE, R. L., PREGENZER, J. G., JACOBSON, E. J., VANDOORNICK, F. K. J., TUSTIN, J. M., AR, D. E. and BUNDY, G. L., 1988, Novel membranelocalized inhibitors of iron-dependent lipid peroxidation. Biochemical Pharmacology, 37, 3853–3860.
  • BRAUGHLER J. M., HALL, E. D JACOBSON, E. J., MCCALL, J. M. and MEANS, E. D., 1989, The 21-aminosteroids: potent inhibitors of lipid peroxidationfor the treatment of central nervous system trauma and ischemia. Drugs Future, 14, 143–152.
  • FLEISHAKER, J. C., PETERS, G. R. and CATHCART, K. S., 1993a, Evaluation of the pharmacokinetics and tolerability of tirilazad mesylate, a 21-aminosteroid free radical scavenger: I. Single dose administration. jourria/ of Clinical Pharmacology, 13, 175–181.
  • FLEISHAKER J. C., PETERS, G. R., CATHCART, K. S. and STEENWYK, R. C., 1993b, Evaluation of the pharmacokinetics and tolerability of tirilazad mesylate, a 21-aminosteroid free radical scavenger: II. Multiple dose administration. Journal of Clinical Pharmacology, 33, 182–190.
  • HALL, E. D., YONKERS, P. A., McCALL, J. M. and BRAUGHLER, J. M., 1988a, Effects of the 21-aminosteroid U-74006F on experimental head injury in mice. Journal of Neurosurgery, 68, 456–461.
  • HALL, E. D., BERRY, K. P. and BRAUGHLER, J. M., 1988b, The 21-aminosteroid lipid peroxidation inhibitor U -74006F protects against cerebral ischemia in gerbils. Stroke, 19, 997–1002.
  • HOLSZTYNSKA, E. J. and DOMINO, E. F., 1986, Biotransform ations of phencyclidine.Drug Metabolism Reviews, 16, 285–320.
  • KANAMURA, K., WEIR, B. K. A., FINDALY, J. M., GRACE, M. and MACDONALD, R. L., 1990, A dosage study of the effect of the 21-aminosteroid U-74006F on chronic cerebral vasospasm in a primate model. Neurosurgery, 27, 29–38.
  • KASSELL, N. F., HALEY, E. L. and ALVES, W.,1993, Phase II trial of tirilazad in aneurysm alsubarachnoid hemorrhage. Canadian Journal of Neurological Science, 20 (suppl. 1), S29.
  • KYEREMATEN, G. A. and VESELL, E. S., 1991, Metabolism of nicotine. Drug Metabolism Review, 33, 3–41.
  • MARET, G., TESTA, B., JENNER, P., TAYAR, N. E. and CARRUPT, P.-A., 1990, The MPTP story: MAO activates tetrahydropyridine d eriv atives to toxins causing p arkinso nism Drug Metabolism Reviews, 22, 291–332.
  • MASUMOTO, H., OHTA, S. and HIROBE, M., 1991, Application of chemical cytochrome P-450 model systems to studies on drug metabolism .IV. Mechanism of piperidinemetabolismpathwaysvia an iminium intermediate.Drug Metabolism and Disposition, 19, 768–780.
  • ORTIZ DE MONTELLANO, P. R., 1989, CytochromeP-450 catalysis: radical interm ediatesand dehydration reactions. TiPS, 10, 354–359.
  • ORTIZ DE MONTELLANO, P. R. and STEARNS, R. A., 1989, Radical intermediates in the cytochrome P-450-catalyzed oxidation of aliphatic hydrocarbons. Drug Metabolism Reviews, 20, 183–191.
  • STOTHERS, J. B., 1972, Carbon-13 NMR Spectroscopy (New York: Academic).
  • STREEPER, R. T., PEARSON, P. G., ZHAO, Z., MIZSAK, S. A. and VRBANAC, J. J., 1997, Synthesis of deuterium labeled 2,4-dipyrrolidinylpyrimidineas a chemicalprobe for P450 mediated oxidation of tirilazad mesylate. journa/ of Labelled Compounds and Radiopharmacolo gy (under revision).
  • WIENKERS, L. C., STEENWYK, R. C., MIZSAK, S. A. and PEARSON, P. G., 1995, In vitro metabolism of tirilazad mesylate in male and female rats. Contribution of cytochrome P4502C11 and d4-5a-reductase. Drug Metabolism and Disposition, 23, 383–392.
  • WIENKERS, L. C., STEENWYK, R. C., SANDERS, P. E., and PEARSON, P. G., 1996, Biotransformation of tirilazad in human: 1. Cytochrome P450 3A-mediated hydroxylation of tirilazad mesylate in human liver microsomes. journa/ of Pharmacology and Experimental Therapeutics, 277, 982–990.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.