Summary
In plasma of mice injected with adenine-9-β-D-arabinofuranoside monophosphate (ara-AMP) coupled to human lactosaminated serum albumin (L-HSA) some of the ara-AMP molecules are enzymatically released, whereas others remain linked to L-HSA. Evidence has been obtained that ara-AMP is not deaminated when it is conjugated to L-HSA, in contrast to the free drug which is rapidly metabolized to its hypoxanthine derivative.
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Acknowledgments. This work was supported by Consiglio Nazionale delle Ricerche, Progetto Finalizzato per il Controllo delle Malattie da Infezione, grant 830065052; ara-AMP was a gift from Dr M.L. Black, Warner-Lambert Co (Ann Arbor, MI). ara-HxMP was a gift from Dr R.W. Sidwell, ICN (Irvine, California). The excellent technical assistance of Mr Goffredo Nanetti is gratefully acknowledged.
The abbreviations used are: ara-AMP, adenine-9-β-D-arabinofuranoside 5-monophosphate; ara-HxMP, hypoxanthine-9-β-D-arabinofuranoside 5-monophosphate; AF, asialofetuin; L-HSA, human lactosaminated serum albumin; L-HSA-ara-AMP, conjugates of L-HSA with ara-AMP; L-[3H]HSA-ara-AMP, conjugates tritiated in the protein moiety; L-HSA-ara-[2,83H]AMP and L-HSA-ara-[23H] AMP, conjugates tritiated in the adenine moiety of ara-AMP. The molar ratios lactose/HSA and ara-AMP/HSA are indicated by subscripts; for example L30-HSA-ara-AMP6.2 is a conjugate with a molar ratio of lactose/HSA of 30 and of ara-AMP/HSA of 6.2.
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Fiume, L., Bassi, B., Busi, C. et al. A study on the pharmacokinetics in mouse of adenine-9-β-D-arabinofuranoside-5-monophosphate conjugated with lactosaminated albumin. Experientia 41, 1326–1328 (1985). https://doi.org/10.1007/BF01952078
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DOI: https://doi.org/10.1007/BF01952078