The Effect of the Lipid A Analog, E5531 on Fever Induced by Endotoxin from Escherichia coli

Yasuyuki ASAI; Yukio NOZU; Takayuki IKEUCHI; Ryuichi NARAZAKI; Kiyoshi IWAMOTO; Sumio WATANABE

doi:10.1248/bpb.22.432

Yasuyuki ASAI, Yukio NOZU, Takayuki IKEUCHI, Ryuichi NARAZAKI, Kiyoshi IWAMOTO, Sumio WATANABE

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Keywords: lipid A, endotoxin, limulus amebocyte lysate, fever, pyrogenicity

JOURNAL FREE ACCESS

1999 Volume 22 Issue 4 Pages 432-434

DOI https://doi.org/10.1248/bpb.22.432

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Abstract

E5531 is a specific lipid A antagonist and is expected to be a drug for the treatment of septic shock. The LAL (limulus amebocyte lysate) activity and pyrogenicity of E5531 were determined. The LAL activity of E5531 is large and confirmed that E5531 had a high affinity to the lipopolysaccharide receptor. The pyrogenic activity of E5531 is weak and the pyrogenic profile of E5531 is different from that of USP (United States Pharmacopoeia) reference standard endotoxin (ETX). E5531 suppressed the pyrogenicity of ETX in rabbits, indicating that E5531 in expected to be useful for the treatment of fever induced by ETX.

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