Effects of 4-hydroxyantipyrine and its 4-O-sulfate on antipyrine as biodistribution promoter

Y. Ohkawa; M. Matsumura; Y. Kurosaki; M. Kurumi; Kenji Sasaki; T. Nakayama

doi:10.1248/bpb.24.529

Effects of 4-hydroxyantipyrine and its 4-O-sulfate on antipyrine as biodistribution promoter

Y. Ohkawa, M. Matsumura, Y. Kurosaki, M. Kurumi, Kenji Sasaki, T. Nakayama

Research output: Contribution to journal › Article › peer-review

8 Citations (Scopus)

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 (K_p) 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 K_p value of antipyrine in the brain. These results suggested that 4-OH could be used as a biodistribution promoter.

Original language	English
Pages (from-to)	529-534
Number of pages	6
Journal	Biological and Pharmaceutical Bulletin
Volume	24
Issue number	5
DOIs	https://doi.org/10.1248/bpb.24.529
Publication status	Published - 2001

Keywords

4-hydroxyantipyrine
4-hydroxyantipyrine O-sulfate
Antipyrine
Biodistribution promoter
Concomitant use
Drug/metabolite interaction

ASJC Scopus subject areas

Pharmacology
Pharmaceutical Science

Access to Document

10.1248/bpb.24.529

Cite this

@article{448bf462f2e341c5a5a1cffef7a72f74,

title = "Effects of 4-hydroxyantipyrine and its 4-O-sulfate on antipyrine as biodistribution promoter",

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.",

keywords = "4-hydroxyantipyrine, 4-hydroxyantipyrine O-sulfate, Antipyrine, Biodistribution promoter, Concomitant use, Drug/metabolite interaction",

author = "Y. Ohkawa and M. Matsumura and Y. Kurosaki and M. Kurumi and Kenji Sasaki and T. Nakayama",

year = "2001",

doi = "10.1248/bpb.24.529",

language = "English",

volume = "24",

pages = "529--534",

journal = "Biological and Pharmaceutical Bulletin",

issn = "0918-6158",

publisher = "Pharmaceutical Society of Japan",

number = "5",

}

TY - JOUR

T1 - Effects of 4-hydroxyantipyrine and its 4-O-sulfate on antipyrine as biodistribution promoter

AU - Ohkawa, Y.

AU - Matsumura, M.

AU - Kurosaki, Y.

AU - Kurumi, M.

AU - Sasaki, Kenji

AU - Nakayama, T.

PY - 2001

Y1 - 2001

N2 - 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.

AB - 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.

KW - 4-hydroxyantipyrine

KW - 4-hydroxyantipyrine O-sulfate

KW - Antipyrine

KW - Biodistribution promoter

KW - Concomitant use

KW - Drug/metabolite interaction

UR - http://www.scopus.com/inward/record.url?scp=0034980745&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0034980745&partnerID=8YFLogxK

U2 - 10.1248/bpb.24.529

DO - 10.1248/bpb.24.529

M3 - Article

C2 - 11379775

AN - SCOPUS:0034980745

SN - 0918-6158

VL - 24

SP - 529

EP - 534

JO - Biological and Pharmaceutical Bulletin

JF - Biological and Pharmaceutical Bulletin

IS - 5

ER -

Effects of 4-hydroxyantipyrine and its 4-O-sulfate on antipyrine as biodistribution promoter

Abstract

Keywords

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this