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- W2034754377 abstract "Four chemically related compounds (two benzofurans, one thianaphthene and one indolyl derivative) have been compared with aspirin and indomethacin in their ability to inhibit prostaglandin (PG) synthesis in vitro by microsomes of bull seminal vesicles with tritiated arachidonate as substrate. Two of these substances [L 8027:3-(2-isopropyl indolyl)-3 pyridyl ketone and L 8109:(5-chloro-3-methyl-2-benzo [b] thienyl) acetic acid] inhibit the synthesis and show marked anti-inflammatory action in the usual pharmacological tests; however, there is no strict correlation, the most powerful inhibitor being the least active anti-inflammatory agent. A benzofuran derivative with a low anti-inflammatory action, but distinctly fibrinolytic [L 2197:2-ethyl-3-(4-hydroxybenzoyl) benzofuran] does not inhibit PG synthesis. A powerful fibrinolytic agent (L 7035:2-isopropyl-3-isonicotinoyl benzofuran), practically devoid of anti-inflammatory action, is a more active inhibitor of PG synthesis than aspirin. It seems that the PG synthetase system of the seminal vesicles does not react in vitro to inhibitors in the same way as that responsible for PG synthesis in tissues damaged by carrageenan or the Freund adjuvant. Such a discrepancy might be due to differences in the tissue distribution of the inhibitors and this could explain the lack of correlation between the in vivo and the in vitro potencies of drugs like L 8027 and L 8109. Localization of L 7035, on the other hand, would be such that the anti-aggregating properties can fully develop, while the inflamed sites remain out of reach of the drug." @default.
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- W2034754377 date "1975-05-01" @default.
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- W2034754377 title "Correlation between anti-inflammatory properties and inhibition of prostaglandin biosynthesis in vitro" @default.
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- W2034754377 doi "https://doi.org/10.1016/0006-2952(75)90195-1" @default.
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