Synthesis and biological activities of leukotriene F4 and leukotriene F4 sulfone |
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| Authors: | D Denis S Charleson A Rackham TR Jones AW Ford-Hutchinson A Lord M Cirino Y Girard M Larue J Rokach |
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| Institution: | 1. Departments of Pharmacology Merck Frosst Canada Inc., P.O. Box 1005, Pointe Claire - Dorval, Quebec H9R 4P8, Canada;7. Medical Chemistry Merck Frosst Canada Inc., P.O. Box 1005, Pointe Claire - Dorval, Quebec H9R 4P8, Canada |
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| Abstract: | Leukotriene F4 (LTF4 and LTF4 sulfone have been synthesized and their biological activities determined in the guinea pig.
LFT4 displayed comparable activity to LTD4 on guinea pig trachea and parenchyma but was less active on the ileum. When injected intravenously into the guinea pig, LTF4 induced a bronchoconstriction (ED50 16 μg Kg−1) which was blocked by indomethacin and FPL-55712 and was 50–100 X less potent than LTD4 in this assay. LTF4 sulfone was approximately 2–5 times less active than LTF4
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. When injected into guinea pig skin with PGE2 (100 ng); LTF4 and LTF4 sulfone (10–1000 ng) induced changes in vascular permeability. The order of potency in this assay was LTE4 sulfone = LTD4 = LTD4 sulfone > LTE4 > LTF4 = LTF4 sulfone. |
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| Keywords: | Correspondence |
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