Replacing 14C with stable isotopes in drug metabolism studies

Drug Metabolism and Disposition

Volumn 24, Issue 7, 1996, Pages 697-701

  Abramson, Fred P ^a   Teffera, Yohannes ^a   Kusmierz, Josef ^a   Steenwyk, Rick C ^b   Pearson, Paul G ^b  

^a GEORGE WASHINGTON UNIVERSITY SCHOOL OF MEDICINE AND HEALTH SCIENCES   (United States)

^b PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CARBON 13; CARBON 14; DRUG METABOLITE; METHYLTESTOSTERONE; NITROGEN 15; RADIOISOTOPE; TIRILAZAD; CARBON; NITROGEN; PREGNANE DERIVATIVE; SCAVENGER;

ANIMAL EXPERIMENT; ARTICLE; BILE; BRAIN PROTECTION; CONTROLLED STUDY; DOSE RESPONSE; DRUG METABOLISM; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; INTRAVENOUS DRUG ADMINISTRATION; ISOTOPE LABELING; MASS SPECTROMETRY; MONKEY; NONHUMAN; PRIORITY JOURNAL; STROKE; SUBARACHNOID HEMORRHAGE; ANIMAL; CHEMISTRY; DOG; MACACA; MALE; METABOLISM; METHODOLOGY;

ANIMALS; BILE; CARBON ISOTOPES; CARBON RADIOISOTOPES; DOGS; FREE RADICAL SCAVENGERS; MACACA FASCICULARIS; MALE; MASS SPECTROMETRY; NITROGEN ISOTOPES; PREGNATRIENES;

EID: 0029657872     PISSN: 00909556     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (17)

1. A. P. Alvares and W. B. Pratt: Pathways of drug metabolism. In "Principles of Drug Action, The Basis of Pharmacology", 3rd ed. (W. P. Pratt and P. Taylor, eds.), pp. 365-422. Churchill Livingstone, New York, 1990.
2. T. A. Baillie: The use of stable isotopes in pharmacological research. Pharmacol. Rev. 33, 81-132 (1983).
3. I. A. Blair: Mass spectrometry in drug disposition and pharmacokinetics. In "Handbook of Experimental Pharmacology" (P. G. Welling and L. P. Balant, eds.), vol. 110, pp. 41-84. Springer-Verlag, Berlin, 1994.
4. F. P. Abramson: CRIMS: chemical reaction interface mass spectrometry. Mass Spectrom. Rev. 13, 341-356 (1994).
5. Y. Teffera, F. P. Abramson, M. McLean, and M. Vestal: Development of an isotope selective high performance liquid chromatography detector using chemical reaction interface mass spectrometry. J. Chromatogr. Biomed. B Appl. 620, 89-96 (1993).
6. Y. Teffera and F. P. Abramson: Application of HPLC/CRIMS for the analysis of conjugated metabolites: a demonstration using deuterated acetaminophen. Biol. Mass Spectrom. 23, 776-783 (1994).
7. J. M. Braughler, E. D. Hall, E. J. Jacobson, J. M. McCall, and E. D. Means: The 21-aminosteroids: potent inhibitors of lipid peroxidation for the treatment of central nervous system trauma and ischemia. Drugs Future 14, 143-152 (1989).
8. E. D. Hall, P. A. Yonkers, J. M. McCall, J. M. Braughler, and E. D. Hall: Effects of the 21-aminosteroid U-74006F on experimental head injury in mice. J. Neurosurg. 68, 456-461 (1988).
9. K. Kanamura, B. K. A. Weir, J. M. Findaly, M. Grace, and R. L. MacDonald: A dosage study of the effect of the 21-aminosteroid U-74006F on chronic cerebral vasospasm in a primate model. Neurosurgery 27, 29-38 (1990).
10. E. D. Hall, K. P. Berry, J. M. Braughler, and E. D. Hall: The 21-aminosteroid lipid peroxidation inhibitor U-74006F protects against cerebral ischemia in gerbils. Stroke 19, 997-1002 (1988).
11. J. C. Fleishaker, G. R. Peters, and K. S. Cathcart: Evaluation of the pharmacokinetics and tolerability of tirilazad mesylate, a 21-aminosteroid free radical scavenger. I. Single dose administration. J. Clin. Pharmacol. 33, 175-181 (1993).
12. 14C]-tirilazad to rabbit, dog, monkey, and human. Pharm. Res. 9, (Suppl.) S312 (1992).
13. L. C. Wienkers, R. C. Steenwyk, P. E. Sanders, and P. G. Pearson: Biotransformation of tirilazad in humans: 1. Cytochrome P450 3A-mediated hydroxylation of tirilazad mesylate in human liver microsomes. J. Pharmacol. Exp. Ther., 277, 982-990 (1996).
14. J. C. Fleishaker, P. G. Pearson, L. C. Wienkers, L. K. Pearson, and G. R. Peters: Biotransformation of tirilazad in humans: 2. Effects of ketoconazole on tirilazad clearance and oral bioavailability. J. Pharmacol. Exp. Ther., 277, 991-998 (1996).
15. M. McLean, M. L. Vestal, Y. Teffera, and F. P. Abramson: Element and isotope specific detection for HPLC using CRIMS. J. Chromatogr. A, 732, 189-199 (1996).
16. H. Song, J. Kusmierz, F. Abramson, and M. McLean: Implementation of the CRIMS technique on a Hewlett-Packard MSD. J. Am. Soc. Mass Spectrom. 5, 765-771 (1994).
17. 15N) labeling and continuous-flow isotope-ratio mass spectrometry as an alternative to radioactive labeling methods. J. Clin. Pharmacol. 33, 246-252 (1993).