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Molecular Pharmacology, Vol 14, 366-369, Copyright © 1978 by the American Society for Pharmacology and Experimental Therapeutics

Inhibition of Drug Metabolism by a Prodrug: 9-beta-D-Arabinofuranosyladenine 5'-Valerate as an Inhibitor of Adenosine Deaminase

ROBERT A. LIPPER 1, SUSAN M. MACHKOVECH 1, JOHN C. DRACH 1, and WILLIAM I. HIGUCHI 1

1 College of Pharmacy and Dental Research Institute, The University of Michigan, Ann Arbor, Michigan 48109

9-beta-D-Arabinofuranosyladenine 5'-valerate (ara-A-5'-valerate), a bioreversible derivative or prodrug of the antiviral agent 9-beta-D-arabinofuranosyladenine (ara-A), was shown to be a competitive inhibitor of calf intestinal adenosine deaminase (adenosine aminohydrolase, EC 3.5.4.4). With ara-A as the substrate, apparent Km and Ki values were 110 µM and 11 µM, respectively, at 37°. Ara-A-5'-valerate is not subject to adenosine deaminase-catalyzed deamination, and it is more water-soluble and more lipophilic than ara-A.

Note:
ACKNOWLEDGMENTS We thank Drs. D. C. Baker, A. J. Giazko, and T. H. Haskell of Warner-Lambert/Parke-Davis Pharmaceutical Research Division for their generosity in supplying compounds used in these studies.

Submitted on August 8, 1977
Accepted on September 21, 1977






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