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. 1974 Apr;1(2):119–127. doi: 10.1111/j.1365-2125.1974.tb00220.x

Thiopurinol

Comparative enzyme inhibition and protein binding studies with allopurinol, oxipurinol and 6-mercaptopurine

B M Dean, D Perrett, H A Simmonds, R Grahame
PMCID: PMC1402452  PMID: 22454898

Abstract

1 The metabolites of thiopurinol have been investigated in intact human and pig erythrocytes using [6-14C]-thiopurinol, high voltage electrophoresis and automated cation exchange chromatography.

2 Pre-incubation of human erythrocytes in vitro with thiopurinol increased the formation of hypoxanthine from [8-14C]-inosine and simultaneously reduced IMP synthesis.

3 Reduced inosine formation, following one week of thiopurinol therapy, has also been observed in vitro using the intact red cells from three patients suffering from gout.

4 Binding of thiopurinol, and to lesser extents of 6-mercaptopurine, uric acid, oxipurinol and allopurinol, has been demonstrated electrophoretically to human and pig serum proteins.

5 Thiopurinol is shown to have a greater binding capacity for purified human serum albumin than uric acid or 6-mercaptopurine at varying substrate and albumin concentrations covering the physiological range. Under these conditions the binding of uric acid is reduced in the presence of thiopurinol.

6 A comparison of the distribution of thiopurinol, 6-mercaptopurine, allopurinol and oxipurinol in whole blood has revealed that allopurinol and oxipurinol are not irreversibly bound to cellular proteins; whereas 30% and 13% of the total cellular uptake was irreversibly bound in the case of thiopurinol and 6-mercaptopurine respectively at substrate levels of 1 nmol per μl blood.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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