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Effects of 4-hydroxyantipyrine and Its 4-O-sulfate on Antipyrine as Biodistribution Promoter

Effects of 4-hydroxyantipyrine and Its 4-O-sulfate on Antipyrine as Biodistribution Promoter

Y Ohkawa, M Matsumura, Y Kurosaki, M Kurumi, K Sasaki, T Nakayama

Biol Pharm Bull. 2001 May;24(5):529-34.

PMID: 11379775

Abstract:

The effects of 4-hydroxyantipyrine (4-OH), a major metabolite of antipyrine, and its 4-O-sulfate (4-S) on the pharmacokinetics of antipyrine were investigated in rats. Plasma elimination of intravenously administered antipyrine was significantly decelerated under a steady-state concentration of 4-OH but not under that of 4-S. Tissue-to-plasma concentration ratio (Kp) of antipyrine under its steady-state concentration was significantly increased in the brain and heart by the concomitant use of 4-OH, while similar use of 4-S had no effect. The enhancement of the blood-brain barrier (BBB) permeability of antipyrine caused by the concomitant use of 4-OH was believed to be concerned with the increase of the Kp value of antipyrine in the brain. These results suggested that 4-OH could be used as a biodistribution promoter.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1672635	4-Hydroxyantipyrine		1672-63-5	Price

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