[3H] Prostaglandin(PG) E2 efflux transport across the BBB in lipopolysaccharide(LPS)-treated mice was evaluated using in vivo brain efflux index method. The half-life of[ 3H] PGE2 administrated in the cerebral cortex of LPS-treated mice was 7. 7 times greater than that of saline-treated mice, suggesting that PGE2 efflux transport across the BBB is attenuated in inflammation. Moreover,[ 3H] PGE2 efflux transport in LPS-treated mice was inhibited by intravenous administration of cefmetazole. This result indicates that PGE2 efflux transport across the BBB is further attenuated by drug administration.