Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 30, 2000 - Issue 9
44
Views
4
CrossRef citations to date
0
Altmetric
Research Article

Human hepatic metabolism of a novel 2-carboxyindole glycine antagonist for stroke: in vitro-in vivo correlations

, , &
Pages 843-856 | Published online: 22 Sep 2008

References

  • BORDI, F., PIETRA, C., ZIVIANI, L. and REGGIANI, A., 1997, The glycine antagonist GV150526 protects somatosensory evoked potentials and reduces the infarct area in the MCAo model of focal is chemia in the rat. Experimental Neurology, 145, 425–433.
  • BRADFORD, M., 1976, A rapid and sensitive method for the quantitation of microgram of quantity of protein utilizing the principle of dye binding. Analytical Biochemistry, 72, 248–254.
  • CHIAMULERA, C., COSTA, S. and REGGIANI, A., 1990, Effect of NMDA- and strychnine-insensitive glycine site antagonists on NMDA-mediated convulsions and learning. Psychopharmacology,, 102, 551.
  • COLLINRIDGE, G. L. and BLISS, T. V. P., 1987, NMDA receptors — their role in long term potentiation. Trends Neuroscknces, 10, 288–293.
  • COLLINRIDGE, G. L. and WATKINS, J. C., 1994, The NMDA Receptor, 2nd edn (Oxford: Oxford University Press).
  • EBNER, T. and BURCHELL, B., 1993, Substrate specificities of two stably expressed human liver UDP - glucuronosyl transferases of the UGT1 gene family. Drug Metabolism and Disposition, 21,50–55.
  • GAVIRAGHI, G., DI FABIO, R., CUGOLA, A., DONATI, D., FERIANI, E., TRIST, D. G. and REGGIANI, A., 1996, Novel glycine antagonists as potent neuroprotective agents. Pharmacochemistry Library, 28, 81–95.
  • GOLDSTEIN, J. A. and DE MORAIS, S. M. F., 1994, Biochemistry and molecular biology of the human CYP2C subfamily. Pharmacokinetics, 4, 285–299.
  • GORROD, J. W., TEMPLE, D. J. and BECKETT, A., 1975, The metabolism of N-ethyl-N-methylaniline by rabbit liver microsomes: the measurement of metabolites by gas—liquid chromatography. Xenobiotica, 5, 453–462.
  • HOKE, J. F., DYKER, A. G., MCALLISTER, A. M. and LEES, K. R., 1998, Pharmacokinetics of GV150526 following multiple intravenous doses in acute stroke patients. Abstract, 6th European Stroke Conference, Amsterdam, The Netherlands.
  • HOUSTON, J. B. and CARLILE, D. J., 1997, Prediction of hepatic clearance from microsomes, hepatocytes, and liver slices. Drug Metabolism Reviews, 29, 891–922.
  • IWATSUBO, T., HIROTA, T., 00IE, T., SUZUKI, H., SHIMADA, H., CHIBA, K., ISHIZAKI, T., GREEN, C. E., TYSON, C. A. and SUGIYAMA, Y., 1997, Prediction of in vivo drug metabolism in the human liver from in vitro metabolism data. Pharmacology and Therapeutics, 73, 147–171.
  • IYER, K. R. and SINZ, M. W., 1999, Characterisation of Phase I and Phase II hepatic drug metabolism activities in a panel of human liver preparations. Chemico-Biological Interactions, 118, 151–169.
  • JIN, C. J., MINERS, J. 0., LILLYWHITE, K. J. and MACKENZIE, P. I., 1993, Complementary deoxy-ribonucleic acid cloning and expression of a human liver uridine disphosphate-glucuronosyl-transferase glucuronidating carboxylic acid-containing drugs. Journal of Pharmacology and Experimental Therapeutics, 264, 475–479.
  • KRUMDIECK, C. L., Dos SANTOS, J. E. and Ho, K. J., 1980, A new instrument for the rapid preparation of tissue slices. Analytical Biochemistry, 104, 118–123.
  • LUDDEN, L. K., LUDDEN, T. M., COLLINS, J. M., PENTIKIS, H. S. and STRONG, J. M., 1997, Effect of albumin on the estimation, in vitro, of phenytoin lima. and Km values: implications for clinical correlations. Journal of Pharmacology and Experimental Therapeutics, 282, 391–396.
  • MULDER, G. J., COUGHTRIE, M. H. W. and BURCHELL, B., 1990, Glucuronidation. In G. J. Mulder (ed.), Conjugation Reactions in Drug Metabolism (London: Taylor & Francis), pp. 51–107.
  • OBACH, R. S., 1997, Nonspecific binding to microsomes: impact on scale-up of in vitro intrinsic clearance to hepatic clearance as assessed through examination of warfarin, imipramine, and propranolol. Drug Metabolism and Disposition, 42, 1359–1369.
  • OMURA, T. and SATO, R., 1962, A new cytochrome in liver microsomes. Journal of Biological Chemistry, 237, 1375–1376.
  • RADOMINSKA-PANDYA, A., CZERNIK, P. J. and LITTLE, J. A. 1999, Structural and functional studies of UDP-glucuronosyltransferases. Drug Metabolism Reviews, 31, 817–899.
  • RETTI, A. E., WIENKERS, L. C., GONZALEZ, F. J., TRAGER, W. F. and KORZEKWA, R., 1994, Impaired (S)-warfarin metabolism catalyzed by the R144C allelic variant of CYP2C9. Pharmacokinetics, 4, 39–42.
  • RITTER, J. K., CHEN, F., YHEUN, Y. S., LUBET, R. A. and OWENS, I. S., 1992, Two human liver cDNAs encode UDP-glucuronosyl transferascs with 2 log differences in activity towards parallel substrates including hyodeoxycholic acid and certain estrogen derivatives. Biochemistry, 212, 3409–3414.
  • ROGAWSKI, M. A., 1992, The NMDA receptor, NMDA antagonists and epilepsy therapy. Drugs, 44, 279–292.
  • SACCHETTI, M. L., TONI, M., FIORELLI, M., ARGENTIN°, C. and FIESCHI, C., 1997, The concept of combination therapy in acute ischemic stroke. Neurology, 49, S70–74.
  • SMITH, P. C., HASEGAWA, J., LANGENDIJK, P. N. and BENET, L. Z., 1985, Stability of acyl glucuronides in blood, plasma, and urine: studies with zomepirac. Drug Metabolism and Disposition, 13, 110–112.
  • SPAHN-LAGGUTH, M. and BENET, L. Z., 1992, Acyl-glucuronides revisited: IS the glucuronidation process a toxification as well as a detoxification mechanism? Drug Metabolism Reviews, 24, 5–48.
  • VERONESE, M. E., MACKENZIE, P. I., DOECKE, C. J., McMANus, M. E., MINERS, J. 0. and BIRKETT, D. J., 1991, Tolbutamide and phenytoin hydroxylations by cDNA-expressed human liver cyto-chrome P4502C9. Biochemical and Biophysical Research Communications, 175, 1112–1118.
  • WILKINSON, G. R., 1987, Clearance approaches in pharmacology. Pharmacological Reviews, 39, 1–47.

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.